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Molecular Target for Screening: G-Protein-Coupled Receptors

Newark, DE. August, 2010 – Press Release – TimTec, LLC. – Molecular Target for Screening:  G-Protein-Coupled Receptors, ActiTarg-G

G-Protein-Coupled Receptors are the largest gene families in the human genome and, rightfully so, have become the leading molecular target in 2008. In 2009 SBS April meeting in Lille, France, followed-up with screening trends report stating that  “GPCRs are expected to replace protein kinases as the most common molecular target used by HTS laboratories.”

GPCRs are the largest family of cell surface receptors being integral to the number of cellular and physiological functions, including light sensing, smell, appetite control, insulin secretion, and blood pressure modulation. These receptors generally have a seven-membrane spanning alpha-helical topography, and while these receptors are similar in overall structure and function, they differ in key amino acid residues. The potential for this super family of receptors to reveal small molecule modulators of a significant biological function has been responsible for the focus of intense drug discovery efforts.

TimTec GPCR Ligands library is called ActiTarg-G. It currently counts 2,300 molecules available in various formatting options, and can be delivered in vials or in 96 or 384-well plates.  ActiTarg-G is the set of diverse molecules that contain chemical lattices present in compounds reported in the technical or patent literature to possess GPCR-ligand properties.

Contact Information to schedule free consultation:

TimTec LLC

Harmony Business Park A-301

Newark DE 19711

Tel 302 292 8500

Fax 302 292 8520

info@timtec.net

Web: http://www.timtec.net/news/timtec-news/actitarg-g-gpcr-ligandshtml.html

About TimTec

TimTec LLC is a privately held company located in Newark Delaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds and collections, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.

http://www.timtec.net/

Nine U.S. Health Research Centers to Receive $255 Million

Nine health research centers have received funds to develop ways to reduce the time it takes for clinical research to become treatments for patients. The funds were awarded as part of the Clinical and Translational Science Awards (CTSA) program which is led by the National Center for Research Resources (NCRR), part of the National Institutes of Health.

“A critical goal of biomedical research is to transform discoveries into preventions, treatments, and cures,” said NIH Director Francis S. Collins, M.D., Ph.D. By working together, CTSAs are removing barriers to research, training new generations of clinical and laboratory research teams, and providing them with the equipment and resources they need.

Now in its fourth year, the CTSA consortium has generated resources that transform the research and training environment to enhance the efficiency and quality of clinical and translational research. Examples include a Web-based national recruitment registry that connects researchers with volunteers interested in participating in clinical studies, establishing public-private partnerships, and a portal that connects researchers with potential investigational drugs that may be useful in new ways.

The 2010 CTSAs expand consortium representation in new areas including New Mexico, Virginia and the District of Columbia, growing the consortium to 55 member institutions. The nine new institutions are:

Children’s National Medical Center, Washington, D.C.
Georgetown University with Howard University, Washington, D.C.
Medical College of Wisconsin, Milwaukee
University of California, Irvine
University of California, San Diego
University of Massachusetts, Worcester
University of New Mexico Health Sciences Center, Albuquerque
University of Southern California, Los Angeles
Virginia Commonwealth University, Richmond

View descriptions of these CTSA awardees at www.ncrr.nih.gov/ctsa2010.

“The nine institutions that have received CTSAs this year extend the geographic reach of the consortium and bring additional talent and expertise in such areas as children’s health, outreach to underrepresented communities, and systems to share research information,” said NCRR Director Barbara Alving, M.D.

The CTSA consortium now includes awardees in 28 states and the District of Columbia. When the program is fully implemented in 2011, it will support approximately 60 CTSAs across the nation.

A sixth and final funding opportunity announcement for CTSAs is available, calling for the next round of applications to be submitted by Oct. 14, 2010, with the awards expected in July 2011. For more information about this funding announcement, see www.ncrr.nih.gov/crfunding.

For more information about the CTSA program, visit www.ncrr.nih.gov/ctsa. The CTSA consortium website, which provides information on the consortium, current members and new grantees, can be accessed at www.CTSAweb.org.

The National Center for Research Resources (NCRR), a part of NIH, provides laboratory scientists and clinical researchers with the resources and training they need to understand, detect, treat and prevent a wide range of diseases. NCRR supports all aspects of translational and clinical research, connecting researchers, patients and communities across the nation. For more information, visit www.ncrr.nih.gov.

The National Institutes of Health (NIH)  The Nation’s Medical Research Agency  includes 27 Institutes and Centers and is a component of the U.S. Department of Health and Human Services. It is the primary federal agency for conducting and supporting basic, clinical and translational medical research, and it investigates the causes, treatments, and cures for both common and rare diseases. For more information about NIH and its programs, visit www.nih.gov.

TimTec Launches Division of Organic Synthesis and Medicinal Chemistry Contract Research Services

Newark, DE, July 8, 2010 Press Release – TimTec, LLC is pleased to announce the launching of the new Division that manages Organic Synthesis and Medicinal Chemistry Contract Research Services. The emergence of the division is an evolutionarily progression for TimTecs business development. The company has been known for its expertise in organic chemistry design and supply for drug discovery for 15 years. TimTec scientists have a proven track record of providing high quality services and showing outstanding integrity to their clients.

The Head of Contract Research Services, J. C. Pelletier, PhD., has over 20 years of research experience in the US pharmaceutical industry as a hands-on medicinal chemist and project Team Leader at large companies and smaller, start-up operations. The TimTec contract research team consists of experienced, bench level scientists who have access to state of the art synthesis, analytical and quality control facilities. TimTec specialists are keenly aware of all the intricate details and chemistry challenges that go into bench-top research before a qualified lead molecule emerges.

TimTec remains flexible in delivering practical chemistry solutions molded to custom research requirements and budgets. Contract research services include, but are not limited to, flexible contracts, program management, structure-activity relationship evaluation,  lead optimization,  property optimization for ADME and PK, metabolite synthesis,  enabling technologies (parallel synthesis, multistep synthesis, analytical chemistry),  mg to kg synthesis capacity,  compound distribution, and patent application preparation assistance. The Contract Research Division puts great emphasis on speed, real-time feedback, ongoing communication, superior compound quality, and the protection of clients knowledge resources and interests. Dedication to service is matched by exceptionally competitive prices.

Contact Information:

TimTec LLC
Harmony Business Park A-301
Newark DE 19711
Tel 302 292 8500

Fax 302 292 8520

info@timtec.net

http://www.timtec.net/contract-research-services.html

About TimTec

TimTec LLC is a privately held company located in Newark Delaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds and collections, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.

Optimer Pharmaceuticals Receives Milestone Payment From Cempra for Next-Generation Macrolide Antibiotic

SAN DIEGO, July 8 /PRNewswire-FirstCall/ – Optimer Pharmaceuticals, Inc. today announced it has received a $500,000 milestone payment from Cempra Pharmaceuticals, Inc. pursuant to the terms of a licensing agreement between the companies.  The milestone payment was made as a result of Cempra’s continuing development of a next-generation macrolide (CEM-101) for the treatment of respiratory infections. Cempra licensed CEM-101 from Optimer and has successfully completed a Phase 1 study.

“The successful completion of the CEM-101 Phase 1 study further validates our OPopSâ„¢ drug discovery platform. We are pleased to see this compound progress into the next phase of development by Cempra,” said Pedro Lichtinger, Optimer’s President and CEO.

CEM-101 is a next-generation oral macrolide entering Phase 2 clinical development for the treatment of community-acquired bacterial pneumonia (CABP). Cempra has exclusive worldwide rights, except in Association of Southeast Asian Nations, or ASEAN, countries, from Optimer to discover, develop and commercialize macrolides from a library of more than 500 compounds, including CEM-101, originated from Optimer’s OPopS drug discovery platform.

In vitro and in vivo studies of CEM-101 have shown potent activity against S. pneumoniae as well as an extended spectrum of activity against community-associated methicillin-resistant Staphylococcus aureaus (CA-MRSA), M. avium and in animal models of malaria. These studies have also indicated that CEM-101 is active against atypical bacteria, such as Legionella, Mycoplasma and Ureaplasma and against gonococci and other organisms that cause genitourinary tract infections.

About OPopSâ„¢

Optimer’s OPopS drug discovery platform allows the development of potential drug candidates through carbohydrate mediated medicinal chemistry and enables the rapid synthesis of a wide variety of proprietary molecules. It includes GlycoOptimization, which enables the modification of a carbohydrate group on an existing drug to improve its properties, and De Novo Glycosylation, which introduces new carbohydrate groups on existing drugs to create new patentable compounds with improvement of pharmacokinetics.

About Optimer Pharmaceuticals

Optimer Pharmaceuticals, Inc. is a biopharmaceutical company focused on discovering, developing and commercializing innovative anti-infectives to treat serious infections and address unmet medical needs. Optimer has two late-stage anti-infective product candidates under development. Fidaxomicin is a narrow spectrum antibiotic being developed for the treatment of Clostridium difficile infection (CDI).  In two Phase 3 trials completed by Optimer to study the safety and efficacy of fidaxomicin for the treatment of CDI, fidaxomicin was statistically superior to vancomycin in global cure rate (defined as cure with no recurrence within four weeks of completing therapy) as well as statistically superior in reducing recurrences of CDI by up to 50% when compared with vancomycin, the only FDA approved product for CDI. Pruvel™ is a prodrug in the fluoroquinolone class of antibiotics being developed as a treatment for infectious diarrhea.  Optimer has also successfully completed two Phase 3 trials with Pruvel.  Additional information can be found at http://www.optimerpharma.com.

Sanford-Burnham robots speed up path to discovery

The work force at Lake Nona’s Sanford- Burnham Institute includes 90 scientific staffers, 60 administrators and support personnel — and a team of three robots. The robots are part of a $15 million investment from the National Institutes of Health and occupy a large, glass-enclosed room on the bottom floor of Burnham’s Lake Nona campus.

Although they resemble the robotic arms used in automobile assembly lines, these robots have a far different task: filling test tubes faster than a human being. And that, scientists say, will speed up the process of scientific discovery.

“The robots are from the automobile industry,” said Greg Roth, director of medicinal chemistry at Burnham’s Conrad Prebys Center for Chemical Genomics. “We use them because of the accuracy and precision of their movements.”

The robotic arms can fill miniature test-tube “wells” so tiny that 1,536 of them fit on a plate the size of an index card. Using such small test tubes allows researchers to save money on chemicals and compounds.

After filling the wells, the robotic arms take a plate of the tubes and subject them to numerous tests such as varying temperatures and pressures. The robots are connected to a main computer that compiles the data from the millions of tests.

Pharmaceutical companies developed the ultra-high throughput screening technology in the mid-1990s, but universities and nonprofit research institutions such as Burnham did not have access to the robots until recently.

Funded by NIH, the Burnham center and eight others around the country form the institute’s Molecular Libraries Production Centers Network. This resource library and network assists scientists in research and allows results to be shared across the public and private sectors.

The reason for the federal government’s interest? As the results of the Human Genome Project began pouring in, scientists found themselves with so many avenues to explore that they needed faster research procedures.

“My scientists like to say they can do more than a robot, but they can only do it for a day,” said Michelle Palmer, director of screening for the Broad Institute at Harvard and Massachusetts Institute of Technology.

“The humans can do it faster and better, but they can’t sustain it. We need to sustain this over months of effort and get it done exactly the same way every time,” Palmer said.


Molecular Templates and ImClone Systems Form Oncology Drug Discovery and Translation Research Collaboration

GEORGETOWN, Texas, Jul 06, 2010 (BUSINESS WIRE) — Molecular Templates announced today that it has entered into a collaborative oncology drug discovery and translation research agreement with ImClone Systems, a wholly-owned subsidiary of Eli Lilly and Company.

Under the terms of the agreement, Molecular Templates will identify Engineered Toxin Bodies (ETBs) against an undisclosed oncology target of interest selected by ImClone. ImClone will conduct preclinical studies utilizing the ETBs to evaluate their therapeutic potential in oncology. Upon completion of the evaluation of the ETBs, Molecular Templates and ImClone have the option to continue exclusive development of selected ETBs by ImClone for potential commercialization by Lilly. Molecular Templates will receive upfront, milestone and royalty payments if any of the ETBs are selected for further development and commercialization. Financial terms of the agreement were not disclosed.

“We are excited to partner with a premier biologics innovator like ImClone,” said Eric Poma, president and chief executive officer of Molecular Templates. “We look forward to collaborating with ImClone to identify novel oncology therapies by leveraging our ETB technology. Given ImClone’s depth in the oncology and biologics arena, we view this partnership as validation of our novel platform and its potential to be used to discover and develop the next generation of targeted biologic medicines.”

ETBs represent a new class of small biologic therapeutics derived from modified bacterial toxins that retain the potent direct cell-kill properties, internalization capabilities, and predictable pharmacokinetics of the parent toxins, but have significantly reduced immunogenicity. These features confer a host of advantages over traditional biologic and small molecule approaches and allow for discovery of therapeutic targets that may be uniquely accessible by ETBs. Molecular Templates has created a vast library (>10(15)) of ETBs, each with distinct binding affinities that can be directly screened for cell-kill ability to rapidly identify promising therapeutic candidates based on both specificity and efficacy to a given target.

About ImClone Systems

ImClone Systems, a wholly-owned subsidiary of Eli Lilly and Company, is committed to advancing oncology care by developing a portfolio of targeted biologic treatments designed to address the medical needs of patients with a variety of cancers. Additional information about ImClone is available at www.imclone.com.

About Molecular Templates

Molecular Templates is a private biopharmaceutical company focused on the discovery and development of Engineered Toxin Bodies (ETBs), a next generation targeted biologics platform. Using the Direct Select Platform (DSP), Molecular Templates has created ETBs libraries that can be screened in a high throughput manner to identify novel therapeutic targets and molecules for various disease states. Molecular Templates plans to identify and develop therapeutics through partnerships with select biopharmaceutical companies as well as on its own. The company completed a series A financing in 2009 led by Sante Ventures. For more information, visit www.moleculartemplates.com.

SOURCE: Molecular Templates

TimTec’s Contract Research Services

High Quality Organic Synthesis and Medicinal Chemistry Contract Research Services at an Outstanding Value

TimTec brings 15 years of expertise in organic chemistry design and supply for drug discovery closer to your supplemental bench-top requirements by launching The Organic Synthesis and Medicinal Chemistry Contract Research Services Division. TimTec scientists have a proven track record of providing high quality services and showing outstanding integrity to their clients.

TimTec remains flexible in delivering practical chemistry solutions molded to custom research requirements and budgets. All Contract Research Services are delivered with an emphasis on speed, real-time feedback, ongoing communication, superior compound quality, and the protection of our clients’ knowledge resources and interests. We are dedicated to providing these services at exceptionally competitive prices.

The Head of Contract Research Services has over 20 years of research experience in the US pharmaceutical industry as a hands-on medicinal chemist  and project Team Leader at large companies and smaller, start-up operations. We are keenly aware of all the intricate details and chemistry challenges that go into bench-top research before a qualified lead molecule emerges. Your TimTec contract research team consists of experienced, bench level scientists who have access to state of the art synthesis, analytical and quality control facilities.

TimTec Contract Research Services Start with:

  • Flexible Contracts

  • Program Management

  • State of the Art Facilities

  • Structure-Activity Relationship Evaluation

  • Lead Optimization

  • Property Optimization for ADME and PK

  • Metabolite Synthesis

  • Enabling Technologies – Parallel synthesis, multistep synthesis, analytical chemistry

  • Mg to Kg Capacity

  • Compound Distribution – Solid or solution, vials or plates

  • Patent Application Preparation Assistance

Supplemental Services and Products:

Custom Synthesis
Compound Acquisition
Weighting and Plating
HTS compounds and compound collections – ActiMol Line of products


Neuronetrix’ COGNISIONâ„¢ System

Alzheimer’s disease is a chronic neurodegenerative disease of the brain which afflicts roughly 5 million individuals in the United States.  Approximately 10% of those over 65 and 50% of those over 85 will die as a result of Alzheimer’s disease.

Even with several therapies available to treat Alzheimer’s disease, there still is a significant gap between the onset of the disease and point at which treatment actually begins.  This treatment gap is directly tied to the challenges in diagnosing the disease early, before the significant loss of memory, cognition, and activities of daily living.  Patients, doctors, caregivers, and the pharmaceutical industry, are looking for and demanding a solution to this problem.

Neuronetrix’ COGNISIONâ„¢ System will, for the first time, directly detect the abnormal cognitive effects of Alzheimer’s disease!  This will facilitate an earlier and more accurate diagnosis than is currently available.  Physicians will use the COGNISIONâ„¢ test to determine which patients would benefit from the available drug treatments.  The system can also be used to monitor the efficacy of the prescribed therapy.

With the aging of America and the proliferation of new Alzheimer’s therapies, the market for Alzheimer’s screening could approach several billion dollars per year in the United States alone.

Following the validation of the COGNISION™ System for Alzheimer’s disease, Neuronetrix will expand into other neurodiagnostic markets such as ADHD, dyslexia, and depression.

http://www.neuronetrix.com/

Weighing & Pipetting Skills and Solutions

FREE Weighing & Pipetting Skills and Solutions Seminar on Thursday, December 3, 2009 at the Doubletree Hotel & Executive Meeting Center in Somerset, NJ.

In these challenging times where training budgets are stretched and laboratories are searching for new efficiencies to improve productivity, METTLER TOLEDO can help. This half-day Insight! Education seminar will focus on the METTLER TOLEDO Good Weighing Practiceâ„¢ (GWP®) program and Pipetting 360° from RAININ, and will include an introduction to associated solutions for the laboratory. The seminar is valued at $495.00 per person, but is completely free of charge with your advance registration – however, space is limited, so register today!

Learn from Acknowledged Industry Authorities:

Proper weighing and pipetting skills and operations are fundamental laboratory functions critical to achieving accurate results in your analytical processes. Yet, there is often confusion on many aspects with regards to balance and pipette use and operation.

Instructor – Henry Oppermann, former Division Chief for Weights and Measures, National Instituted of Standards [NIST].

Learn the Good Weighing Practice (GWP®) approach to selection, use, calibration, and ongoing management of balances for your laboratory, department, or even entire organization from an acknowledged industry authority. During his career, Henry Oppermann has been instrumental in developing many of the guidelines and practices designed to improve weighing processes. Join him and experts from METTLER TOLEDO for this insightful session.

Together with knowledgeable experts on the RAININ 360° approach to pipette use and management, you’ll learn valuable risk-based approaches to working with two of the most common – yet critical instruments in the lab, that will enhance your skills, career and results in any industry setting!

Also, we’re pleased to introduce Quantos – a revolutionary innovation for routine and precise dosing of powder compounds in the lab. Quantos is the winner of the 2009 Lab Automation Association and R&D 100 Awards! Learn more about how Quantos can improve speed, safety, and savings in your lab. See Quantos and a variety of other METTLER TOLEDO solutions live following the seminar during our product exposition.

If you think a colleague would be interested in attending this informative seminar, then forward to a colleague.

Date:    Thursday, December 3, 2009
Time:    8:30 am – 12:15 pm (Continental Breakfast at 8:00am / Lunch following seminar.)
Cost:    FREE with Advance Registration. Hurry – Space is limited! Free parking.
Location:    Doubletree Hotel & Executive Meeting Center 200 Atrium Drive, Somerset, New Jersey 08873

Schedule

Time:
8:00am – 8:30am Arrival & Check-in with Complimentary Continental Breakfast
8:30am – 12:15pm Seminar and speakers
12:15pm – 1:30pm Complimentary lunch concurrent with product exposition
Free parking.

Cost:
FREE with Registration (A $495 Insight! Education value)

Agenda:

8:00 am – 8:30 am: Check-in and Complimentary Continental Breakfast

8:30 am to 10:15 am – Good Weighing Practice™ GWP® Presented by Henry Oppermann, Former Division Chief for Weights and Measures at the National Institutes of Standards and Technology (NIST).

Minimize weighing risks with a minimum of effort. Good Weighing Practice allows you to improve control of your whole measuring process from balance Evaluation, Selection, Installation, Calibration and Routine Operation. With Good Weighing Practice you weigh without risks, comply with regulations easily, and achieve consistent good quality of your product and analytical processes appropriate for your industry or application.  Click here to learn more about Good Weighing Practice.

10:15 am to 10:30 am – Break

10:30 am to 10:55 am – Minimizing Weighing Measurement Uncertainty
METTLER TOLEDO knows it is essential for you to produce accurate results, achieve compliance, and improve traceability in the lab. See how to address all requirements regarding measurement uncertainty as outlined in ISO 17025 and ISO 9000/9001. Ensure strict compliance with your Quality Management SOP’s. Verify all calibrations and automatically perform routine weight checks on schedule while efficiently capturing your weighing data transparently while meeting all regulatory requirements.

10:55 am to 11:20 am – A New Solution in Automated Powder Dosing
New QUANTOSâ„¢ from METTLER TOLEDO solves many of the challenges of repetitive weighing of powder materials, such as reference standards for use with chromatography and other analytical lab applications, capsule filling or inhaler work, bottling, and more. Precise dosing of small amounts of powder in the Bio/Pharmaceutical or the chemical laboratory is a difficult, time consuming, and potentially hazardous task. Often the scientist is in contact with highly potent compounds or has a limited amount of precious material, and dosing may be hindered by electrostatic or hygroscopic effects. QUANTOS solves these challenges and more. Click here to learn more about QUANTOSâ„¢.

11:20 am to 12:15 pm – Good Practices in Pipette Use and Management – Pipetting 360°
Pipette liquid handling involves a variety of principles and practical considerations. This informative presentation from RAININ will cover handling principles with practical considerations, address how to best maximize accuracy & performance technique in your pipette work, tip selection and application, calibration approaches and solutions, and steps you can take to improve your results and productivity. Click here to learn more about RAININ Pipettes.

12:15 pm – 1:30 pm – Complimentary Lunch and Product Exposition
A Free Product Exposition will run concurrent with and following a noon luncheon where you can see a variety of these and other METTLER TOLEDO and RAININ Solutions displayed and demonstrated, while having your questions answered.

Exposition Products and Technologies will include:

* Analytical, Precision, and MicroBalances from METTLER TOLEDO
* QUANTOS® Perfect Dosing Solution
* RAININ Pipette Solutions including the New Rainin Liquidator 96 Benchtop Pipetting System
* Pipette Calibration Workstations
* Potentiometric and Karl Fischer Titrators from METTLER TOLEDO
* Density & Refractometry Systems
* pH measurement solutions
* Thermal Analysis including DSC, TGA, TMA, and DMA technologies and melting point solutions
* Moisture Balances
* LabX Software for Balance and Instrument control and data capture.
* And more…

1:30 pm – Conclude

Doubletree Hotel & Executive Meeting Center
200 Atrium Drive
Somerset, New Jersey 08873

http://mt.com/us/en/home/events/fairs/somerset_semin.html

Zelinsky Institute Inc. announced collaboration with ART-CHEM

Zelinsky Institute Inc. (Newark, DE, August 2009) – Zelinsky Institute Inc. expands its partnership and supplier network with the announcement of collaboration with one of the premier fine chemistry companies – ART-CHEM, which originated from Moscow, Russia, and has started its operations in Berlin, Germany, in 2005. ART-CHEM specializes in synthesis of highly diverse and rich in unique scaffolds HTS compounds and building blocks. The entire line of ART-CHEM product offerings is going to be available via Zelinsky Institute Inc., which is headquartered in and currently operates from Delaware, USA, offices.

ART-CHEM founder, Dr. B. Ugrak, comments, “We are pleased to become a part of Zelinsky Institute, a recognized supplier of specialty chemicals. Together we can provide greater value serving our, now, joined customer base.” Zelinsky Institute CEO, Dr. M. Niazoff, agrees adding, “We are happy to have ART-CHEM high quality fine chemistry products and service capabilities accessible via Zelinsky Institute. Together, we are looking forward to growing our market fueled by ever-evolving research demands.”

Collaboration aims at making ART-CHEM products and services known and easily accessible for existing and prospective Zelinsky Institute Inc. customers worldwide. September 2009 product databases distributed by Zelinsky Institute Inc. are going to include ART-CHEM’s drug-like and chemically diverse compounds for screening, building blocks, and intermediates. Zelinsky Institute Inc. is going to coordinate procurement, orders, and consolidated delivery of HTS products. Zelinsky Institute Inc. and ART-CHEM collaboration is open to custom projects going beyond the supply of just existing fine organic chemistry. For recently launched databases, products and services, inquiries, orders, and customized solutions please contact \n info@zelinsky.com This e-mail address is being protected from spambots. You need JavaScript enabled to view it .

Zelinsky Institute Inc., located in Delaware, USA, is the official representative of Zelinsky Institute of Organic Chemistry of the Russian Academy of Sciences (ZIOC) in Moscow, Russia. ZIOC is one of the world’s largest scientific centers in the fields of organic chemistry, organic catalysis, and chemistry of biologically active compounds. The Institute was founded on February 23, 1934, following the Decision of the Presidium of the Academy of Sciences of the USSR.

Zelinsky Institute Inc. began its operations in the USA in 1993 to establish the first commercialization bridge in compound supply industry linking Former USSR research centers unique chemistries and R&D service capabilities with Western life-science industries demands. Among Zelinsky Institute Inc. first customers were DuPont, Merck, Johnson&Johnson, and Ely Lilly.  Zelinsky Institute Inc. has expanded its markets and partnerships and welcomes new global customers and scientific challenges.

Contacts:

ART-CHEM GmbH

Campus Berlin-Buch, Haus B55

Robert-Roessle-Strasse 10

13125 Berlin, Germany

Phone: +49 (0)30 9489-2180

Fax:      +49 (0)30 9489-2181

Zelinsky Institute Inc.
POB 8941, Newark, DE, 19714 USA

For products and services, inquiries, orders, and customized solutions please visit:

http://www.zelinsky.com

Sirona Biochem Optimizes Key Test for Diabetes and Obesity Drug Development

VANCOUVER, BC — (Marketwire) — 07/16/09 — Sirona Biochem Corp. (TSX-V: SBM) announced today it is now ready to begin testing its novel new compounds to fight diabetes and obesity.

The completion of the company’s key SGLT biological assessment test and testing will be done under contract with Richmond, BC based SignalChem.

Sirona Biochem owns the worldwide rights to a library of potential new sodium glucose transporter (SGLT) inhibitors developed to treat diabetes and obesity. SGLT Inhibitors are a novel new drug class currently under development that block the reuptake of excess sugars from urine in the kidney which can then reduce high blood sugar to normal levels. Excess sugar in the blood is a primary medical challenge associated with treating diabetes and obesity.

Sirona has a research and development agreement with TFChem (Rouen, France), where a significant number of SGLT drug analogs are being prepared for first stage evaluation. Preliminary primary stage testing conducted earlier this year provided positive indications to support Sirona Biochem’s project and provided key insights to optimize the new test that is now ready for use to evaluate the next library set of molecules.

Mark Senner, President, explained, “SGLT inhibitors are a new and exciting class of compounds that have great promise to treat both diabetes and obesity which are now at epidemic levels worldwide. This new drug class is one considered to have extraordinary market potential in the fight against diabetes and obesity.

“Development of this new drug class however is challenging due to the fragile nature of these ‘sugar’ based molecules that render them unstable and difficult to develop for clinical use. Given this challenge, it is believed that the use of the patented GlycoMim® technology, licensed from TFChem to develop SGLT Inhibitors, will increase drug stability and, therefore, improve their overall clinical effectiveness. Potential licensing and development partners have expressed interest in our concept of improving molecules in this new drug class. We intend to develop ‘best in class’ SGLT Inhibitors through use of this technology.

“The key and critical first test has been developed and optimized for use by SignalChem under contract from Sirona Biochem. Through use of this proprietary test, the company will be able to determine which molecules have the desired potency and selectivity compared to a reference standard. Screening of the current library of compounds will generate key data for ongoing drug development and provide first stage proof of concept necessary to secure future partnering opportunities. Sirona’s scientific team aims to identify lead compounds by the end of 2009,” continued Senner.

“The results from our new optimized test will be critical to direct our ongoing development of novel new SGLT inhibitors. The development and optimization of this sophisticated test, completed by SignalChem, is a significant and key milestone achievement for us. We are very pleased with the progress that we are making on our SGLT drug development program,” commented Senner.

Upon selection of compounds with the desired potency and selectivity for the SGLT 2 carrier protein, further preclinical screening for cytotoxicity, ADME properties, pharmacokinetics and in vivo efficacy will need to be carried out to select compounds for future clinical development. The primary objective of this critical first stage development plan with SignalChem was to develop, qualify and optimize the key test required for the initial development of SGLT inhibitors.

Investors are invited to visit the Sirona Biochem website at: http://www.sironabiochem.com where we feature the most recent information about the company and its activities. Alternatively, investors are able to e-mail all questions and correspondence to info@sironabiochem.com where they can also request to be added to the investor e-mail list to receive all future press releases and updates or call John Dougherty, Corporate Development at 604-641-4466.

About the Company:

Sirona Biochem Corp. (TSX-V: SBM) is a emerging biotech company dedicated to the discovery and development of novel drug compounds. The current focus is on treatments for Type II Diabetes and Obesity. Sirona has entered into a license agreement with TFChem S.A.R.L., a Drug Discovery company based in Rouen, France. TFChem licenses its technology of fluorinated carbohydrate mimics: GlycoMim®, and products in development to biotech companies. The license agreement with TFChem provides for research and development of new compounds known as S.G.L.T. inhibitors. S.G.L.T. inhibitors are a new and exciting class of compounds that have great promise and potential to treat both diabetes and obesity.

About SignalChem:

SignalChem, based in Richmond, B.C., Canada is a biotechnology company focused on the research, development and production of innovative cell signaling products to advance basic research and drug discovery efforts, with specific emphasis on the production of highly purified biologically active human recombinant proteins. SignalChem is emerging as a leader and a key contender in the life science recombinant protein market place. SignalChem offers a comprehensive discovery service which includes: gene cloning & expression of therapeutic ‘targets,’ custom assay & antibody development and compound profiling for drug ‘potency’ & ‘selectivity.’

Mark Senner
President and Director

Neither the TSX Venture Exchange nor its Regulation Services Provider (as that term is defined in the policies of the TSX Venture Exchange) accepts responsibility for the adequacy or accuracy of this release.

Sirona Biochem
950-789 West Pender Street
Vancouver, B.C., V6C 1H2
Direct: 604-641-4466
Fax: 604-608-5471
info@sironabiochem.com

Source: www.sys-con.com

Cognition Therapeutics Closes Series A Financing to Advance Drug Candidates for Alzheimer’s Disease

Start-up company continues momentum with selection of disease-modifying small molecule drug leads for behavioral testing
PITTSBURGH, July 16 /PRNewswire/ — Cognition Therapeutics Inc., a Pittsburgh-based drug discovery company developing small molecule disease-modifying treatments for Alzheimer’s, has closed on a $1.21M Series A financing. The round was led by Ogden CAP, LLC of New York City and includes M5Invest Partners of Villanova, PA, the Pittsburgh Life Sciences Greenhouse, Innovation Works (Pittsburgh), and several individual investors. The round included both new investments and the conversion of existing convertible notes.

“This investment facilitates the advancement of our existing lead molecules towards a major milestone,” said Cognition Therapeutics President and CEO Hank Safferstein, Ph.D., J.D. “Our combination of novel, small molecule drug candidates and biologically-relevant screening methods is unique in the pharmaceutical industry. We’re pleased to have Ogden CAP and M5Invest join our other investors in supporting our pioneering approach to treat or prevent Alzheimer’s disease by targeting the proteins that cause the earliest stages of this disease”.

“As early investors, we are impressed by Cognition Therapeutics’ combination of cutting-edge technology, influential and experienced leadership, and large clinical and commercial potential,” said Robert Gailus, senior advisor to Ogden CAP. “Alzheimer’s disease is a major health epidemic that places increasing strains on the world’s healthcare systems as the population ages. The drug candidates being developed by Cognition have the potential to significantly impact this devastating disease,” Gailus continued. Alzheimer’s disease affects an estimated four and a half million people in the United States today. That number is expected to exceed 12 million people by 2050.

Funds raised in this round will support advancement of Cognition Therapeutics’ pioneering lead molecules that block the activity of the toxic oligomeric form of Abeta protein that interferes with normal learning and memory. Studies from the world’s leading academic laboratories indicate that the memory deficits caused by the oligomeric protein are among the earliest changes seen in Alzheimer’s disease and Mild Cognitive Impairment, the precursor to Alzheimer’s. These studies indicate that blocking the effects of this protein may halt or reverse Alzheimer’s disease. Cognition will use these funds to test its most promising lead molecules in behavioral models of Alzheimer’s disease. “The advancement of the company’s lead compounds into behavioral testing represents a significant milestone for the company,” says Dr. Franz Hefti, Chairman of the Board. “Cognition’s scientific approach is unique among the approaches being taken by the pharmaceutical industry today. Cognition has a novel Alzheimer’s disease model for the critical molecular step that causes memory loss. In addition, the company’s proprietary chemistry is based on natural molecular scaffolds which brought us effective drugs like aspirin, lidocaine and taxol. We anticipate new disease-modifying drugs for Alzheimer’s disease will result from this unique combination,” Dr. Hefti continued.

About Cognition

Cognition Therapeutics, Inc. is a leader in the discovery and development of small molecule therapeutics targeting the toxic proteins that cause the cognitive decline associated with Alzheimer’s disease and other degenerative diseases of the human brain. Toxic proteins play a crucial role in a large class of diseases, and there are currently no therapeutics available to prevent or block the destructive effects of toxic oligomeric proteins. Cognition has leveraged its scientific expertise with these difficult targets to pioneer the use of proprietary assays that emphasize functional responses and proprietary medicinal chemistry that ensures novel, high quality small-molecule drug candidates for the treatment of these diseases.

Cognition has developed a number of screening strategies to identify small molecules capable of blocking the central toxicity of proteins in Alzheimer’s disease and other neurodegenerative diseases. These assays emphasize phenotypic or functional responses of mature primary neurons to the toxic proteins. Cognition’s proprietary chemistry platform converts natural products into low molecular weight chemically stable druglike molecules, and is thus a source of novel pharmacophores and valuable drug candidates. These two technology platforms harken back to the origins of the pharmaceutical industry, when phenotypic responses were the sole screening method and natural product derivatives formed the starting materials for successful drug discovery.

Cognition Therapeutics was founded on small molecule chemical libraries licensed from co-founder Dr. Gilbert Rishton at California State University Channel Islands and proprietary screening strategies established by co-founder and Chief Science Officer Dr. Susan Catalano. After initial investment and relocation to Pittsburgh, the company secured Dr. Hank Safferstein as President and CEO, bringing with him more than 15 years of leadership experience in drug development, commercialization and marketing for a number of public and private companies. www.cogrx.com.

About Ogden CAP, LLC

Ogden CAP, LLC is a New York company that has investments is a wide variety of asset classes, including venture capital. Over the past two years Ogden CAP, LLC has invested in 10 early stage companies. Besides its investment in Cognition, Ogden CAP, LLC has two other investments in the Pittsburgh area: FASTTAC, a document control and management company for the construction industry, and TSG, Inc. an energy company that converts coal to fuels.

About the Pittsburgh Life Sciences Greenhouse (PLSG)

The Pittsburgh Life Sciences Greenhouse (PLSG) provides capital investments and customized company formation and business growth services to western Pennsylvania’s life sciences enterprises. The PLSG supports biosciences companies with promising innovations in the following concentrations: Biotechnology Tools, Diagnostics, Healthcare IT, Medical Devices and Therapeutics. The PLSG is propelling the sustainable growth of the region’s life sciences economy by accelerating research and technology commercialization with seed and early-stage companies; connecting investors with their Investment Portfolio companies; expanding established life sciences ventures and relocating biomedical companies to Pennsylvania.

www.plsg.com

About Innovation Works (IW)

Innovation Works provides risk capital and business expertise to the most promising early-stage technology companies in Southwestern PA to help them grow and succeed. Innovation Works is one of the most active seed-stage investors in the country, having invested in more than 120 emerging technology companies since beginning their seed fund in 1999. Those companies have gone on to raise over $600 million in additional capital from a diverse set of VCs, private investors, strategic partners and other sources of capital.

SOURCE Cognition Therapeutics Inc.

The Further In You Go, The Bigger It Gets

I had a printout of the structure of maitotoxin on my desk the other day, mostly as a joke to alarm anyone who came into my office. “Yep, here’s the best hit from the latest screen. . .I hear that you’re on the list to run the chemistry end. . .what’s that you say?”
Maitotoxin.jpg
This is, needless to say, one of the largest and scariest marine natural product structures ever determined (and that determination has been no stroll past the dessert table, either).

But that’ hasn’t stopped people from messing around with it. And there’s much speculation that other people are strongly considering messing around with it, too – you synthetic chemists can guess the sorts of people that this might be, and their names, and what it might be like to sit through the seminars that result, and so on.

I fear that a total synthesis of maitotoxin would be largely a waste of time, but I’m willing to hear arguments against that position. Just looking at it, though, inspires thought. This eldrich beastie has 98 chiral centers. So let’s do some math. If you’re interested in the SAR of such molecules, you have your choice of (two to the 98th) possible isomers, which comes out to a bit over (3 times ten to the 29th) compounds. This is. . .a pretty large number. If you’re looking for 10mg of each isomer to add to your screening collection (no sense in going back and making them again), then you’re looking at a good bit over half the mass of the entire Earth. And that’s just in sheer compounds; we’re not counting the weight of vials, which will, I’d say, safely move you up toward the planetary weight of a low-end gas giant. We will ignore shelving considerations in the interest of time.

Recall that yesterday’s post gave a number of about 27 million compounds below 11 heavy atoms. You could toss 27 million compounds into a collection of ten to the 29th and never see them again, of course. But that brings up two points: one, that the small-compound estimate ignores stereochemistry, and we’ve been getting those insane maitotoxin numbers by considering nothing but. The thing is, with only 11 non-hydrogen atoms, there aren’t quite as many chances for things to get out of control. The GDB compound set goes up only to 110 million or so if you consider stereoisomers, which actually isn’t nearly as much as I’d thought.

But the second point is that this shows you why the Berne group stopped at 11 heavy atoms, because the problem becomes intractable really fast as you go higher. It’s worth remembering that the GDB people actually threw out over 98% of their scaffolds because they represented potential ring structures that are too strained to be very stable. And they only considered C, N, O and F as heavy atoms (even adding sulfur was considered too much to deal with, computationally). Then they tossed out another 98 or 99% of the structures that emerged from that enumeration as reactive and/or unstable. Relax your standards a bit, allow another atom or two, bump up the molecular weight, do any of those and you’re going to exceed anyone’s computational capacity. Update: the Berne group has just taken a crack at it, and managed a reasonable set up to 13 heavy atoms, with various simplifying assumptions to ease the burden. If you want to mess around with it, it’s here, free of charge).

Source: Corante

International Swine Flu Conference August 19-21 Washington DC

Top leaders and key decision-makers of major companies representing a broad range of industries will meet with distinguished scientists, public health officials, law enforcers, first responders, and other experts to discuss pandemic prevention, preparedness, response and recovery at the 1st International Swine Flu Summit.

At the summit, attendees will be able to draw on first-hand best practices to create the solid business continuity plans that their companies and organizations need in order to prepare for, respond to, and survive a pandemic.

The summit draws on the success of the seven previous Bird Flu summits which featured as speakers several distinguished personalities such as Dr. David Nabarro, the United Nations Coordinator for Avian and Human Influenza, Alex Thiermann of the World Organization for Animal Health (OIE) and Dr. Wenqing Zhang of the WHO Epidemic and Pandemic Alert and Response.

Well-known emergency responders, heads of hospitals from around the world, and hog/swine industry leaders will speak in this summit.

Topics Include:
Country Report & Situations Update
Surveillance and Data Management
Preparing Communities Strategies; Local Partnership and Participation
Delivery of Vaccine and Antiviral Medication
National Pandemic Influenza Medical Countermeasure
Socio Economic Impact on Hog/Swine Industry
Benefit-risk Assessment: Public Health, Industry and Regulatory Perspectives
Prevention Education Efforts and Risk Communication
Command, Control and Management
Emergency Response Management
Business-Based Planning
School-Based Planning
Community-Based Planning

http://new-fields.com/isfc/

TimTec Expands Partnership With Collaborative Drug Discovery Through Publishing Three Additional Libraries on CDD’s Free Public Access Database

Last October, TimTec and Collaborative Drug Discovery (CDD) established a collaboration in which CDD’s web-based data management system would host two TimTec Natural Products libraries on their free community Public Access site.  Through this partnership, researchers would be able to register for a free account with CDD allowing them to chemically mine the contents of these TimTec compound libraries using CDD’s powerful, intuitive web-based database software.

TimTec is now offering three more libraries on the CDD Public Access database:

The TimTec ActiTarg-K Kinase Modulators library contains over 6,000 compounds known to inhibit protein kinase activity:

http://www.timtec.net/actitarg-k-kinase-modulators.html

The TimTec OGT Inhibitors Analogs library contains more than 300 compounds analogous to three known O-GlcNAc Transferase inhibiting molecules:

http://www.timtec.net/o-glcnac-transferase-inhibitors.html

Finally, the TimTec resourceful Diversity Set is a general screening collection of drug-like compounds that present most diversified selection from TimTec stock. This screening library contains 10,000 of the most diverse compounds, all complying with the Lipinski Rule of Five:

http://www.timtec.net/diversity-set-10k.html

TimTec’s five databases join more than 25 other databases containing chemical and biological data hosted on CDD Public Access, including:

  • 47,000 Ki values for 20,000 compounds against 699 GPCR targets from the NIMH Psychoactive Drug Screening Program at the University of North Carolina
  • Over 15,000 compounds with Malaria assay data from 5 public data sources
  • 48,818 compounds from the Distributed Drug Discovery (D3) at Indiana University – Purdue University Indianapolis (IUPUI)
  • Almost 7,500 compounds with Tuberculosis antibacterial and cell viability information from 4 public data sets and growing thanks to their collaboration with the Bill & Melinda Gates Foundation

About TimTec, LLC.

TimTec LLC. – http://www.timtec.net – is a privately held company located in NewarkDelaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. The company has developed strong in-house expertise assembling general and targeted library collections for variety of research purposes. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.

For more information on TimTec library collections, please contact:

Kay Denisova
Business Development
TimTec LLC
Harmony Business Park Building 301-A
Newark, DE 19711
Tel 302 292 8500
Fax 302 292 8520
info(at)timtec.net
http://www.timtec.net

About Collaborative Drug Discovery, Inc.

Collaborative Drug Discovery, Inc. (CDD) – http://www.collaborativedrug.com – provides web-based software that organizes preclinical research data to help scientists advance new drug candidates more effectively. The CDD database enables scientists to “archive, mine, and collaborate”® around preclinical chemical and biological drug discovery data through a web-based interface. The software helps distributed research groups to safely store and intelligently analyze small molecule, enzyme, cell and animal bioactivity data accumulated from both low-throughput and high-throughput screens. Unique collaboration features and CDD’s community-oriented approach help unite globally dispersed humanitarian efforts against neglected infectious diseases. Similar collaborative strategies are also rapidly gaining prominence in the commercial arena. CDD offers its industrial-strength database software at a price affordable to academic laboratories, research foundations, and small companies.

For further information please contact:

Barry Bunin, PhD
President & CEO
Collaborative Drug Discovery (CDD)
1633 Bayshore Hwy, Suite 342
Burlingame, CA 94010
info(at)collaborativedrug.com

CLC bio’s enterprise platform wins award at Bio-IT World Expo in Boston

Boston, Massachusetts, USA — April 30, 2009 — CLC bio’s enterprise platform for Next Generation Sequencing data analysis, CLC Genomics Server, has just been awarded the “Best of Show” prize at the Bio-IT World Conference & Expo 2009 – an award judged by a team of Bio-IT World magazine editors and leading industry experts.

Bio-IT World Editor-in-Chief Kevin Davies, PhD., comments, “Each year we go through a process where our judging panel debates the technical merits and likely business impact of the different technologies presented at the Best of Show awards. CLC bio’s success this year clearly reflects the importance of the incredibly exciting Next Generation Sequencing space, with a solution that is obviously gaining traction with it’s capabilities to handle the immense data management and analytical challenges required in this area.”

“Judging on several criteria, such as the importance of the problem being addressed and the elegance of the solution provided, it was clear to the judging panel that CLC Genomics Server, and the flexible plug-in structure it provides, delivers an ideal platform for researchers working with Next Generation Sequencing data.” says M. Michael Barmada, PhD. – member of the “Best of Show” judging panel and Director of the Center for Computational Genetics at the Graduate School of Public Health, University of Pittsburgh. “It’s nice to see complex computational algorithms and routines presented with an elegant interface in a user-friendly way, which lowers the technical barriers for all researchers working with high-throughput sequence data analysis.”

CLC Genomics Server is CLC bio’s advanced and powerful bioinformatics solution which is built upon a powerful and modern three-tier server architecture, that yields flexible options of executing centralized services, easy integration with other applications and services, powerful database communication and data integration, and secure access control framework and central action logging. Customers already using this enterprise platform, includes J. Craig Venter Institute, Albert Einstein College of Medicine, Veridex, and University of California – Berkeley. Read more about this solution here:

http://www.clcbio.com/index.php?id=1376

Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs

BERKELEY, Calif.–(BUSINESS WIRE)–Plexxikon Inc. today announced the issuance of key composition-of-matter patents covering novel compounds discovered through the company’s Scaffold-Based Drug Discoveryâ„¢ platform. Plexxikon’s pipeline of preclinical and clinical stage product opportunities currently span potential treatments for cardio-renal disease, CNS disorders, inflammation, metabolic disease and oncology. Two of the three recently issued patents (U.S. patents no. 7,498,342 and no. 7,504,509) cover compounds derived from the company’s discovery efforts to target protein kinases for the treatment of multiple indications including oncology and inflammation. The third patent (U.S. patent no. 7,476,746) covers novel compounds from the company’s PPAR (peroxisome proliferator-activated receptor) program yielding novel therapeutic opportunities for metabolic disorders and other diseases.

“We are pleased to be adding these additional patents to our growing and broad intellectual property portfolio,” stated K. Peter Hirth, Ph.D., chief executive officer of Plexxikon. “Plexxikon’s novel approach to drug discovery has enabled the company to advance multiple first-in-class drug candidates which are covered by strong intellectual property, and as a result, to secure significant pharmaceutical industry interest in our programs.”

In contrast to fragment-based approaches, Plexxikon’s platform has generated multiple product opportunities by mining the relatively unexplored chemical space of scaffold-like cores and by utilizing co-crystallography early in the discovery process to guide chemical optimization of these scaffolds. Further, the company has developed methods to make highly selective kinase inhibitors as yet rarely seen. Plexxikon has demonstrated the ability to develop selectivity between two targets with as little as one amino acid difference in their catalytic domains. This capability has created the opportunity for the development of new targeted drugs not only for oncology, but also for chronic disease indications outside oncology where safety hurdles are even higher. To date, Plexxikon’s platform has led to the development of a targeted medicine for the treatment of melanoma, a drug candidate for polycystic kidney disease (PKD), an oral agent for rheumatoid arthritis and a broad spectrum oral diabetic therapeutic, all representing novel agents addressing significant unmet needs.

Dr. Prabha Ibrahim Promoted to Vice President of Chemistry

In other news, Prabha N. Ibrahim, Ph.D., was promoted to the position of vice president of chemistry, bringing over 15 years of experience to her position. As head of chemistry since 2002, she has played a key role in building the company’s synthetic and medicinal chemistry capabilities leading to the discovery of Plexxikon’s novel drug candidates now in the clinic and in preclinical development. Prior to Plexxikon, Dr. Ibrahim was a senior scientist at CV Therapeutics, where she was responsible for the identification and development of preclinical candidates for cardiovascular indications. She also previously worked at Amgen, where she played an integral role in small molecule drug discovery for inflammation therapeutics. Dr. Ibrahim earned her Ph.D. at the University of Victoria, Canada, and was a Welch Foundation Fellow at Rice University in Houston.

Plexxikon Profile

Plexxikon is a leader in the structure-guided discovery and development of novel small molecule pharmaceuticals to treat human disease. The company’s clinical stage programs include PLX4032 for the treatment of melanoma and colorectal cancer, PLX5568 for the treatment of PKD and PLX204 for the treatment of diabetes. Among the company’s preclinical development programs, candidates are being developed for the treatment of rheumatoid arthritis, multiple sclerosis and other autoimmune diseases.

Plexxikon’s proprietary Scaffold-Based Drug Discovery™ platform is being applied to build a pipeline of product opportunities in multiple therapeutic areas. This discovery process integrates multiple state-of-the-art technologies, including structural screening as one key component that provides a significant competitive advantage over other drug discovery approaches. To date, the company has discovered a portfolio of clinical and preclinical stage compounds in varied disease areas addressing significant unmet needs in each therapeutic category.

Plexxikon is seeking pharmaceutical and biotechnology partners for select collaboration opportunities. For more information, please visit www.plexxikon.com.

Molecular Fingerprints Point The Way To Earlier Cancer Diagnosis And More Targeted Treatment

ScienceDaily (Mar. 27, 2009) — Metabolites are molecular fingerprints of what your cells are up to and Dr. Arun Sreekumar wants to know the impression made by cancer.

You’ve likely heard about metabolites; your physician probably screens for some known ones such as triglycerides or cholesterol at your annual physical. Scientists suspect we have about 3,000 metabolites that come from our food or are synthesized from different compounds in our bodies.

Dr. Sreekumar, a cancer researcher at the Medical College of Georgia Cancer Center, wants those screens of the blood or urine to also detect early signs of cancers such as leukemia, bladder, kidney and breast when the chance for cure is best.

He’s already begun to identify metabolites that indicate not only the presence of prostate cancer, but its aggressiveness, a tool that could help tailor optimal treatment. The search began in men at risk: those with elevated prostate specific antigen, or PSA, levels. A PSA test along with a digital rectal exam is today’s standard for prostate screening so physicians typically do both in men age 50 and older. But PSA levels are actually better at helping determine if prostate cancer has returned, Dr. Sreekumar says.

Elevated levels of PSA, a protein, are not always predictive of cancer, which means a lot of men get unnecessary biopsies. PSA measurements also can’t distinguish between tumors that have a good outcome versus those with a poor one.

“The physician does not really have the tools in hand to really say that this tumor will spread to other organs or not.” says the Georgia Cancer Coalition Distinguished Cancer Scholar. “We want to find clinical markers that supplement PSA.”

Aggressiveness is a major factor in prostate cancer treatment. In fact some men with slow growing disease likely won’t even need treatment. So he wants to provide a complement of biomarkers that accurately diagnose and categorize the disease then help monitor success of treatment. These early studies indicate a urine test may one day be possible to do just that.

He and colleagues at the University of Michigan reported in the Feb. 12 issue of Nature what appears to be one of the first metabolites implicated in cancer invasion. They looked at 1,126 metabolites in 262 samples taken from men with high PSA levels. They consistently found elevated levels of the amino acid sarcosine in the prostate tissues of men with cancer; levels were highest in what appeared to be the most aggressive tumors.

Sarcosine, a modified form of the amino acid glycine, was a known entity but its function was unclear. Scientists thought it might be a dumping ground for excess methyl groups needed to enable chemical changes of genes, proteins and other body components that can affect what and how much they do.

This process called methylation can be a good thing – like when it’s helping an embryo develop – but when it goes badly, it can cause disease such as cancer. While sarcosine’s dumping role seemed to protect from cancer, the Michigan scientists found its action actually helps induce tumors. In fact, when they added it to prostate cancer cells, the cells became more aggressive. Exactly how that process works is still under study but the findings were pretty consistent.

“When we looked at patients with metastatic disease, sarcosine levels were sky high compared to patients with localized tumors,” says Dr. Sreekumar. “It’s enabling invasion.”

Because cancer and people are both very heterogenous, measures need to be taken in larger population samples, he says. Also, they found a small group of patients with negative biopsies and high sarcosine levels. “We don’t know how many of them have missed cancer,” says Dr. Sreekumar who joined the MCG faculty in February.

These are among the reasons he believes in strength in numbers. “In the real world of biomarkers, you want 100 percent sensitivity. If the patient has cancer, you want to pick it up. We need to have a kind of multiplex test where you can test for say10 different entities and have a greater confidence that what you are stating about the tumor is true. Our goal is to develop such a panel and research on sarcosine is a first step toward achieving this.”

In his new position at MCG, he’s looking to expand the number of metabolites known to be predictive of prostate and other cancers. In prostate cancer, he’s beginning with follow up on other metabolites identified in the Michigan study in which researchers identified a total of six metabolites, including sarcosine, linked to increased tumor progression. A total of 89 metabolites were different in metastatic prostate cancer compared to localized disease.

He’s excited about what metabolites will one day tell cancer physicians and patients but adds that they are just a piece of what our bodies can tell us about a potential cancer growing inside. Scientists also need to continue to look at genes expressed by tumors and the proteins expressed by those genes to get the bigger picture. “It’s basically a systems approach you need to take,” he says.

The young scientist has worked with all those pieces in his relatively short career. He started his postdoctoral fellowship at the University of Michigan in1999, when the ability to look at gene expression was new. With his mentor, Dr. Arul M. Chinnaiyan, director of Michigan Center for Translational Pathology, Pathology Research Informatics and Cancer Bioinformatics at Michigan, he helped develop the next step: the ability to look at expression of hundreds of proteins at a time, instead of a handful, an important advance in light of the fact that there are about 1 million proteins. Recently they were among the first to venture into the world of metabolites, which are made by proteins.

“Previous technology was looking at a cell from a narrow perspective and cells never act in isolation, proteins never act in isolation, they always form complexes, act in pathways,” Dr. Sreekumar says.

His inspiration to follow those pathways is a fellow Ph.D. student who died too young and quickly of an aggressive leukemia and the fact that cancer is a leading cause of death worldwide.

GTCbio Announces 4th Annual Assay Development and Screening Conference taking place June 8-9, 2009.

San Francisco, CA – GTCbio Announces its 4th Annual Assay Development and Screening Conference taking place June 8-9, 2009. As compounds derived from high throughput screening increasingly find their way into clinical trials, drug screening has become widely accepted as a critical step in the drug discovery process. After more than a decade of rapid growth, tremendous progress has been made in assay technology, laboratory automation, and informatics. These technological developments have not only facilitated a drastic increase in throughput and efficiency in drug screening, but have also provided novel solutions in other areas of drug discovery and development. As screening has also become prominent in biological research, screening facilities have become increasingly popular in academic institutions.

As the pharmaceutical industry continues to face the challenges of developing more new chemical entities and reducing the cost of R&D, the demand for novel technologies and creative approaches for improving the efficiency of screening has intensified. Cell-based assays used in compound screening and high-content screening technologies have gained popularity in the industry. Years of intensive research have finally resulted in label-free technologies in the drug screening market place. These technologies provide new ways of interrogating cellular and molecular binding events and enable orthogonal screening approaches to drug targets.

The goal of the 4th annual Assay and Screening Technologies Conference is to provide a forum for academics and professionals in the drug discovery industry to stay abreast of exciting new developments in assay technologies while exchanging ideas and developing more efficient approaches to the drug discovery and development process.

For more information, visit http://gtcbio.com/conferenceDetails.aspx?id=123

Salk Forms Stem Cell Partnership With Sanofi-Aventis

The Salk Institute says it has formed a new stem cell research partnership with Sanofi-Aventis, the international pharmaceutical giant based in Paris. Financial terms of the five-year alliance were not disclosed, and some details of the deal remain to be worked out, Salk spokesman Mauricio Minotta told me this afternoon.

The Sanofi-Aventis regenerative medicine program will sponsor grants in promising research areas, and is intended to provide long-term, multi-participant collaborations between scientists at San Diego-based Salk and Sanofi-Aventis. “It’s meant to be a true collaboration, it’s not just funding,” says Michael White, who oversees the institute’s office of technology management and development. Sanofi-Aventis has about 16,000 employees in the United States, mostly at its U.S. headquarters in Bridgewater, NJ, and about 100,000 employees worldwide.

The program also will provide unrestricted support for the Salk Institute’s stem cell facility, which was created as a separate laboratory supported by private funding during the years the Bush Administration had placed restrictions on federal stem cell funding.

In a statement, Salk president William Brody says there are no preconditions concerning the collaborative alliance. “Our scientists will continue to freely explore cutting-edge research and publish their work,” Brody says. (That’s important to academic freedom, because companies have been known to try to squelch research findings if they don’t support the company’s marketing message.) Under this deal, Salk will also gain access to “extensive resources” at Sanofi-Aventis, which includes a large-scale facility in Tucson, AZ, for screening compounds with potential to be new drugs.

“That’s something that’s very attractive to us, to be able to screen our targets with their drugs,”White says.

Such industry collaborations could be a sign of the times. In January, San Diego’s Burnham Institute for Medical Research announced a multi-year agreement with Johnson & Johnson’s Pharmaceutical Research and Development unit.

Source: xconomy.com