Archive for the ‘Targeted Libraries’ Category
Molecular Target for Screening: G-Protein-Coupled Receptors
Last Updated on Friday, 20 August 2010 06:48 Written by Editor Thursday, 19 August 2010 03:10
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
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.
Zelinsky Institute Inc. announced collaboration with ART-CHEM
Last Updated on Saturday, 10 October 2009 06:10 Written by admin Saturday, 10 October 2009 06:10
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.â€
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. Â 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:Â Â Â Â Â +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:
TimTec Expands Partnership With Collaborative Drug Discovery Through Publishing Three Additional Libraries on CDD’s Free Public Access Database
Last Updated on Wednesday, 13 May 2009 03:56 Written by admin Wednesday, 13 May 2009 03:56
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 collaborateâ€Â® 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
Posted under Compound Libraries, Diversity Libraries, North America, Press Releases, Targeted Libraries | No Comments
KINAXO’s Cellular Target Profiling® reveals mTOR as a new target of Celebrex
Last Updated on Sunday, 10 May 2009 08:46 Written by admin Sunday, 10 May 2009 08:46
Martinsried, Germany, April 29, 2009 / b3c newswire / - Kinaxo Biotechnologies GmbH has successfully applied its Cellular Target Profiling® technology to identify the protein kinase mTOR as a new cellular target of celecoxib (Celebrex®, Pfizer). Celecoxib is a non-steroidal, anti-inflammatory Cox-2 inhibitor approved for the treatment of osteoarthritis, rheumatoid arthritis and acute pain. In addition, celecoxib’s anti-proliferative effect has earned it a place in numerous clinical trials against several malignancies.
The discovery that celecoxib targets mTOR contributes to a better understanding of the drug’s mode of action and efficacy in cancer patients. mTOR (mammalian target of rapamycin) acts as a central regulator of cell proliferation, cell survival, angiogenesis and cell metabolism. Moreover, mTOR is a key intracellular convergence point for a number of signaling pathways that are abnormally activated in many types of cancer.
As traditional drug development approaches become more and more expensive, drug repositioning has been widely recognized as an opportunity to expand a drug’s therapeutical applications. Here, Cellular Target Profiling® provides a powerful approach to revealing new targets that indicate additional or alternative medical uses for clinically validated or approved drugs. Further information on celecoxib reprofiling (AN3) and similar studies with other small molecules (e.g. profiling of the natural product geldanamycin, AN2) can be downloaded from our website at www.kinaxo.com.
Link to the news release
http://www.b3cnewswire.com/popup.php?id=149
About KINAXO
Kinaxo Biotechnologies GmbH is a privately-held biotechnology company based in Munich/Martinsried, Germany. We offer advanced chemical proteomics and phosphoproteomics services to support lead compound selection, target deconvolution, drug reprofiling, and off-target toxicity assessment. Kinaxo has several ongoing collaborations, including with Boehringer Ingelheim, Johnson & Johnson and Takeda.
Posted under Cancer Research, Drug Development, Europe, Medicinal Chemistry, Press Releases, Proteomics, Targeted Libraries | No Comments
Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs
Last Updated on Friday, 27 March 2009 10:00 Written by admin Friday, 27 March 2009 10:00
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.â€
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.
Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs
Last Updated on Friday, 20 March 2009 04:54 Written by Editor Friday, 20 March 2009 04:54
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.â€
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.
Ligand Pharmaceuticals Inc. (LGND) Enters into Screening Agreement with Trevena
Last Updated on Thursday, 12 February 2009 04:00 Written by Editor Thursday, 12 February 2009 04:00
SAN DIEGO–(BUSINESS WIRE)–Ligand Pharmaceuticals Incorporated (NASDAQ:LGND – News) and Trevena Inc. today announced the initiation of a joint research and license alliance to screen targets using Trevena’s novel biological platform against Ligand’s combinatorial library of compounds, to identify active compounds with potential for development as novel G-protein coupled receptor (GPCR) therapeutics.
Under the terms of the agreement, Trevena has been granted exclusive worldwide rights to sublicense active compounds resulting from the collaboration. Ligand expects to screen 24 targets over two years and receive payments triggered by a tiered screening paradigm for each target.
“We are delighted to enter into this collaboration that allows us to generate cash flow from the combinatorial chemistry technology we gained through our acquisition of Pharmacopeia,” said John L. Higgins, President and Chief Executive Officer of Ligand. “Working closely with the Trevena team, we hope to rapidly identify and advance novel drug candidates using their unique insight into GPCR signaling pathways.”
Maxine Gowen, President and CEO of Trevena said, “We are excited to work with these exceptional scientists and get access to this proven chemistry platform. We believe that this collaboration will accelerate our drug discovery efforts and the validation of our biological platform.”
About Trevena, Inc.
Trevena, Inc. is a Philadelphia-based drug discovery company focused on developing pharmaceutical products targeting GPCRs. Pharmaceutical products that target GPCRs represent up to 40% of marketed drugs today. Trevena’s drug discovery platform, licensed from Duke University Medical Center, is based on extensive research from the laboratories of scientists Robert J. Lefkowitz, M.D. and Howard A. Rockman, M.D. The company’s drug discovery portfolio is currently focused on programs for cardiovascular and CNS indications. Trevena, Inc. is privately held. (www.trevenainc.com)
About Ligand Pharmaceuticals
Ligand discovers and develops new drugs that address critical unmet medical needs of patients with muscle wasting, frailty, hormone-related diseases, osteoporosis, inflammatory diseases and anemia. Ligand’s proprietary drug discovery and development programs are based on its leadership position in gene transcription technology. In December 2008, we acquired Pharmacopeia in a transaction that provides Ligand rights to numerous collaborations with pharmaceutical companies, pipeline programs and the world’s largest combinatorial chemistry library.
Posted under Collaborations, Compound Libraries, North America, Press Releases, Targeted Libraries | No Comments
Galapagos enters strategic alliance in diabetes and obesity with Merck & Co., Inc.
Last Updated on Monday, 12 January 2009 03:47 Written by Editor Monday, 12 January 2009 03:47
Galapagos NV (Euronext: GLPG) announced today that it has entered into a multi-year global strategic alliance with Merck & Co., Inc. to develop potential new therapies in obesity and diabetes.
Galapagos will be responsible for the discovery and pre-clinical development of new small molecule candidate drugs based on novel Galapagos targets. Merck will have the exclusive option to license each candidate for clinical development and commercialization on a worldwide basis. The alliance will make use of Galapagos’ proprietary SilenceSelect(R: 36.098, -1.882, -4.96%) target discovery platform for identification of novel targets in obesity and diabetes. After validation, targets will be selected by a joint steering committee and entered into screening and chemistry by Galapagos. Merck has the option to acquire an exclusive license to each candidate drug and upon exercise of such an option, Merck will be responsible for the development and commercialization of the candidate drug. Galapagos may execute phase I clinical studies and will have the right to further develop and commercialize certain compounds for which Merck does not exercise its exclusive option.
Under the terms of the agreement, Galapagos will receive an upfront fee of EUR 1.5 million from Merck. In addition Galapagos is eligible to receive discovery, development and regulatory milestone payments that could potentially exceed EUR 170 million total for multiple products, as well as specific sales milestones and royalties upon commercialization of any products covered under the agreement.
“The alliance with Merck in obesity and diabetes further demonstrates Galapagos’ ability to expand into new therapeutic areas,” said Onno van de Stolpe, CEO. “Galapagos has a proven track record of delivering on its alliance programs, making us attractive to potential pharma partners seeking to fill their pipelines with medicines based on novel modes of action. Galapagos has been successful through careful management of its R&D programs; this early stage alliance with Merck fits nicely into our alliance infrastructure as other programs advance into later stages.”
“By combining Galapagos’ novel target identification strategy with Merck’s drug development expertise this collaboration provides a unique opportunity to discover and develop potential new therapies for diabetes and obesity,” said Catherine Strader, Vice President, External Basic Research, Merck Research Laboratories.
Conference call and webcast presentation
Galapagos will conduct a conference call open to the public today at 11.30 Central European Time (CET: 14.7001, -0.06, -0.41%), which will also be webcast. To participate in the conference call, please call +31 20 794 8504, ten minutes prior to commencement. A question and answer session will follow the presentation. Click here to access the live audio webcast. The archived webcast also will be available for replay shortly after the close of the call.
About diabetes and obesity
Diabetes mellitus is a disorder in which blood sugar (glucose) levels are abnormally high because the body does not produce enough insulin to meet its needs. Patients with diabetes type 1 (10% of diabetes patients) have lost the ability to produce insulin themselves. In type 2 diabetes, patients develop resistance to the effects of insulin; obesity is the chief risk factor in developing this type, as 80-90% of patients with type 2 diabetes are obese. Diabetes symptoms include increased urination, thirst, and weight loss. Diabetes also can lead to nerve damage, blood vessel damage, and increased risk of heart attack, stroke, and kidney failure. About 15% of people over the age of 70 develop Type 2 diabetes. Treatment of diabetes involves diet, exercise, education, and, for most people, drugs. Global sales of diabetes drugs totaled $15 billion in 2005[1].
Obesity is the excess accumulation of body fat and is defined as having a Body Mass Index[2] > 30. Being obese increases the risk of many disorders, such as diabetes, heart disease, and certain cancers, and can result in high blood pressure and early death. Increasing activity and reducing caloric intake are essential to treating obesity, but some people also need to take drugs. Around 10% of the world population is obese[3], and sales of obesity drugs in the world’s largest markets are expected to grow from $500 million in 2006 to more than $2 billion by 2016[4].
About Galapagos
Galapagos (Euronext Brussels: GLPG; Euronext Amsterdam: GLPGA; OTC: GLPYY) is a drug discovery company with pre-clinical programs in bone and joint diseases and bone metastasis. Its BioFocus DPI division offers a full suite of target-to-drug discovery products and services to pharmaceutical and biotech companies, encompassing target discovery and validation, screening and drug discovery through to delivery of pre-clinical candidates. BioFocus DPI also provides adenoviral reagents for rapid identification and validation of novel drug targets, compound libraries for drug screening as well as chemogenomics and ADMET database products to select targets and compounds. Galapagos currently employs about 460 people and operates facilities in six countries, with global headquarters in Mechelen, Belgium. More information about Galapagos can be found at www.glpg.com.
Posted under Collaborations, Europe, North America, Press Releases, Targeted Libraries | No Comments
Trends in Drug Research 27th Noordwijkerhout-Camerino-Cyprus Conference Noordwijkerhout, The Netherlands, May 3 – 8, 2009
Last Updated on Thursday, 27 November 2008 10:24 Written by admin Thursday, 27 November 2008 10:24
The Symposium is sponsored by the European Federation of Medicinal Chemistry (EFMC).
The Organising and Scientific Committees cordially invite you to attend the 27 edition of this meeting on Trends in Drug Research. The interplay between molecular structure and biological activity is central to contemporary biomedical and translational research, relevant not only to structural biologists but also to diverse scientists involved in the study of bioactive compounds and signalling mediators and those working in drug discovery and development.
The scientific programme will include plenary lectures, oral communications and poster sessions. Registration will open on Sunday May 3, followed by an inaugural evening lecture and a welcome gathering.
The scientific programme ends on Thursday May 7 and the meeting will be concluded by the symposium dinner on Thursday evening. On Friday after the conference, a complimentary workshop “Virtual Screening and De Novo Design” is offered by BioSolveIT.
REGISTRATION Information and the complete SCIENTIFIC PROGRAMME is available on the SYMPOSIUM’S WEBSITE: WWW.NOORDWIJKERHOUTMEDCHEM.ORG
PROGRAMME
Opening keynote lecture
Chairman Prof. Henk TIMMERMAN (VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands)
Chemistry’s Role In Target Identification And Validation Dr. Scott A. BILLER (NOVARTIS, Cambridge, United States)
KINASE INHIBITORS: TARGETING THE NON-ATP SITE
Chairman: Dr. Edmond DIFFERDING (UCB, Braine-l’Alleud, Belgium)
Discovery And Development of Selective, Orally Bioavailable Tyrosine Kinase Inhibitors For Targeted Treatment Of Human Cancers Prof. Stephen K. BURLEY (SGX PHARMACEUTICALS, SAN DIEGO, United States)
Non-Competitive Inhibitors of MEK1: from Discovery to the Clinic Dr. Jeffrey OHREN (PFIZER, GROTON, United States)
Allosteric Inhibition of Kinase Function Philip E. SANDERSON (MERCK, Rahway, United States)
CHEMICAL AND ENZYMATIC MODIFICATION OF THERAPEUTIC PEPTIDES AND PROTEINS TO IMPROVE THEIR MODE OF ACTION
Chairman: Dr. Stan VAN BOECKEL (ORGANON, Oss, The Netherlands)
Title to be announced
Dr. Jesper LAU (NOVO NORDISK, Maaloev, Denmark)
Sugars and Proteins
Prof. Ben DAVIS (OXFORD UNIVERSITY, Oxford, United Kingdom)
CarboCarrier(TM): a Novel Technology to Extend the Half-life of Small Proteins and Peptides Martin DE KORT (ORGANON, Oss, The Netherlands)
PROMISES IN GPCR DRUG DISCOVERY
Chairman: Prof. ROB LEURS (LEIDEN/AMSTERDAM CENTER FOR DRUG RESEARCH, Amsterdam, The Netherlands)
Structural Genomics of GPCRs; New Opportunities for Drug Discovery Chris TATE (MRC LABORATORY OF MOLECULAR BIOLOGY, Cambridge , Belgium)
GPCR Hetero-Dimerisation: Contribution to Receptor Pharmacology and Function Prof. Graeme MILLIGAN (UNIVERSITY OF GLASGOW, Glasgow, United Kingdom)
Dicovery & Development of Allosteric Modulators: Hopes and Promises Dr Emmanuel LE POUL (ADDEX PHARMA, Plan les Ouates, Switzerland)
TRANSPORTERS
Chairman: Prof. Gerhard ECKER (UNIVERSITY OF VIENNA, Vienna, Austria)
Predicting Substrate Properties for ABC-Transporter – Safety Sciences on the Molecular Level Prof. Gerhard ECKER (UNIVERSITY OF VIENNA, Vienna, Austria)
Drug Transport and Metabolism: Value of Knockout and Transgenic Mouse Models Dr. Alfred SCHINKEL (HET NEDERLANDS KANKER INSTITUUT , Amsterdam, The Netherlands)
Title to be announced
Prof. Robert FORD (THE UNIVERSITY OF MANCHESTER, Manchester, United Kingdom)
OFF-TARGET EFFECTS
Chairman: Prof. Hugo KUBINYI (Weisenheim am Sand, Germany)
GPCR Antitargets – Prediction and Prevention of Side Effects Dr. Thomas KLABUNDE (SANOFI-AVENTIS DEUTSCHLAND GMBH, Frankfurt am Main, Germany)
Understanding Ion Channels Using Computational Approaches Dr. Marcel J. DE GROOT (PFIZER, Sandwich, United Kingdom)
The QSARome of the Receptorome: Development of Robust QSAR Models Capable of Predicting Compound Binding Profiles against Multiple Targets Prof. Alexander TROPSHA (UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, Chapel Hill, United States)
FRAGMENT BASED DRUG DISCOVERY
Chairman: Dr. Iwan DE ESCH (VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands)
Experiences in Fragment-based Lead Discovery Prof. Roderick E. HUBBARD (UNIVERSITY OF YORK, York, United Kingdom)
SPR Biosensor-Based Fragment Screening and Lead Characterization Prof. U. Helena DANIELSON (UPPSALA UNIVERSITY, Uppsala, Sweden)
Novel-Generation Kinase Inhibitors: Deep Pocket Binders by Fragment- Based Design Dr. Gerhard MÃœLLER (CSO PROTEROS FRAGMENTS GMBH, Munich/Martinsried, Germany)
ANTI-INFLAMMATORY DRUG DISCOVERY
Chairman: Robin THURMOND (JOHNSON & JOHNSON, San Diego, United States)
Histamine H4 Antagonists as Future Anti-Inflammatory Drugs Robin THURMOND (JOHNSON & JOHNSON, San Diego, United States)
JAK3 Kinase: a Molecular Target for Treatment of Inflammatory Diseases and Renal Transplant Rejection Dr. Paul S. CHANGELIAN (CHANGELIAN BIOSCIENCE, LLC, , United States)
Molecular Mechanim of Action for Chemokine and Other Anti-inflammatory Agents on 7TM Receptors Dr. Thue W. SCHWARTZ (UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark)
Complimentary Workshop on Friday: “Virtual Screening and De Novo Design” offered by BioSolveIT Late Departure – the transportation will be provided by the organisers.
http://www.LDOrganisation.com
Posted under ADMET Studies, Drug Development, Europe, Europe, Press Releases, Targeted Libraries | No Comments
Fragment Based Screening Service at CRELUX and ZoBio
Last Updated on Thursday, 27 November 2008 10:04 Written by admin Thursday, 27 November 2008 10:04
Munich (D) and Leiden (NL), November 24, 2008 / b3c newswire / – CRELUX and ZoBio announced today that they have successfully executed their first fragment based screening projects from a jointly established platform.
One of the first targets, which also will be made accessible to customers, was Pim1, a kinase that has been implicated in the progression of several haematological malignancies. In addition to the “off the shelf†data on Pim1, tailor made fragment based screening projects are available for customers upon request.
The joint technology platform combines ZoBio’s proprietary Target Immobilized NMR Screening (TINS) technology with CRELUX’s high performance kinase crystallography platform. In the first campaign Pim1 was screened by TINS using ZoBio’s fragment library, hits were assessed in an in vitro kinase assay and the top 50 hits have been soaked into protein crystals. 37 out of these 50 fragments showed defined binding modes. Together with this high hit rate the structural diversity within this group generated multiple points for optimization and clearly proved the power of this technology combination.
“We are delighted to have found a perfect partner for entering into high performance fragment based screening. The collaboration with ZoBio adds another crucial drug discovery technology to our service portfolioâ€, commented Dr. Michael Schäffer, CEO of CRELUX.
“This project demonstrates the power of the combination of TINS with top notch crystallography. I am absolutely convinced that together we can provide our customers with critical starting point to jump start their challenging or failed targets.†noted Dr. Gregg Siegal, CSO of ZoBio.
CRELUX has used its state-of-the-art structural biology platform to solve more than 270 crystal and co-crystal structures for pharma and biotech companies. This platform encompasses all steps – from target cloning and expression all the way to high-throughput protein crystallization and in-house x-ray crystallography.
ZoBio provides fragment discovery and characterization services to the pharmaceutical and biotech industries using its proprietary Target Immobilized NMR Screening (TINS) platform. TINS, with its unparalleled sensitivity and reliability, has been used to discovery highly diverse, efficient ligands for a variety of targets including kinases, protein-protein interactions, viral targets and membrane proteins.
Posted under Collaborations, Diversity Libraries, Europe, HT Screening, New Products, Press Releases, Targeted Libraries | No Comments
Virtual Screening Gives Drug Design a Boost
Last Updated on Wednesday, 19 November 2008 05:07 Written by Editor Wednesday, 19 November 2008 05:07
San Diego, CA (OBBeC) – Researchers at the University of California, San Diego, developed a unique computational approach to identify key compounds that could lead to new drugs to combat African sleeping sickness — a disease spread by the biting tsetse fly and caused by the parasite Trypanosoma brucei.
The approach developed by McCammon’s group uses a combination of several computational tools. It starts with a detailed model of the biological target –REL1 in this case — derived from X-ray crystallography. It then uses biophysical principles to find all the ways in which the protein can twist, turn, and wiggle.
McCammon’s computational method has already proven its utility for designing other important drugs. His group used it to develop a model for a new class of drugs to treat AIDS that led to raltegravir, which the Food and Drug Administration approved in 2007. McCammon’s team also used the method to identify promising drug candidates for treating H5N1 avian flu.
TOCRIS SIGNS EXCLUSIVE DEAL TO SUPPLY GEFITINIB
Last Updated on Thursday, 4 September 2008 03:20 Written by admin Thursday, 4 September 2008 03:20
September 4th, 2008 – Tocris Bioscience announced today the signing of an exclusive deal with AstraZeneca to supply Gefitinib (also known as Iressa and ZD1839) to preclinical researchers working on the mechanisms underlying cancer development. For the first time, scientists will be able to buy authentic, fully licensed, non-formulated Gefitinib as an off-the shelf product for use in biological research.
In recent years pharmaceutical companies have developed a number of small molecule drugs that are clinically effective against certain types of cancer. Tyrosine kinase inhibitors (TKIs) such as Gefitinib are at the forefront of this new generation of targeted anticancer agents.
Gefitinib is an EGFR-TKI (epidermal growth factor tyrosine kinase inhibitor), which targets and blocks the activity of the EGFR-TK, an enzyme that regulates intracellular signalling pathways implicated in cancer cell proliferation and survival. Growth factor signalling has been identified as a key driver of tumour growth and spread in a wide range of cancers. For clinical use, Gefitinib has been approved for the treatment of advanced Non Small Cell Lung Cancer (NSCLC) in 36 countries.
This molecule has been licensed to Tocris for use as a preclinical research compound only. Strict conditions have been imposed by AstraZeneca to ensure that it is not used in human studies.
Duncan Crawford, Tocris’ Chief Scientific Officer, said, “We know that there is a great deal of interest in Gefitinib from the global research community. By making fully licensed Gefitinib available through our catalogue, we hope to promote new and exciting research in the fundamental processes that drive cancer development. For Tocris this important new product perfectly compliments our comprehensive and expanding range of high purity compounds, which are in use worldwide to further biomedical research. We are delighted that our excellent relationship with AstraZeneca has allowed us to make this compound available to scientists working on the fundamental mechanisms of cancer cell biology”
About Tocris Bioscience
Tocris Bioscience is a leading supplier of high performance chemicals, peptides and antibodies, with customers in virtually all of the world’s major pharmaceutical companies, universities and research institutes. The Company is committed to making new life science discoveries possible by providing the highest performing and most innovative range of research reagents.
Tocris Bioscience products are used by scientists carrying out non-clinical research in fields such as cancer, stroke, Alzheimer’s disease and obesity. The Company’s product range of over 2,000 reagents represents a unique collection of novel, exclusive and licensed research tools. A major source of key signal transduction reagents and arguably the world leader in the supply of neuroscience reagents, the Company won the Queen’s Award for Enterprise (International Business) in 2002.
Tocris Bioscience is the trading name for the companies in the Tocris Cookson Group. Formed from the 1994 merger of Tocris Neuramin and Cookson Chemicals, Tocris Cookson Ltd is privately held and headquartered in Bristol, UK. Its US subsidiary, Tocris Cookson Inc, is located in St. Louis, Missouri, USA. There are approximately 50 employees in the Group worldwide, operating out of two sites in the UK and one in the US.
About AstraZeneca
AstraZeneca is a major international healthcare business engaged in the research, development, manufacturing and marketing of meaningful prescription medicines and supplier for healthcare services. AstraZeneca is one of the world’s leading pharmaceutical companies with healthcare sales of $29.55 billion and is a leader in gastrointestinal, cardiovascular, neuroscience, respiratory, oncology and infectious disease medicines. For more information about AstraZeneca, please visit: www.astrazeneca.com
Ion Channel Targets 2008 9 – 10 September 2008, South San Francisco, CA, USA
Last Updated on Saturday, 19 July 2008 03:51 Written by admin Saturday, 19 July 2008 03:51
Select Biosciences is proud to announce their 4th annual Ion Channel Targets conference and exhibition. This year’s event will take place at the South San Francisco Conference Center. Alongside an exhibition of selected scientific posters and service providers, Select Biosciences is organizing a two day event gathering some of the most influential players in the field from America and across the globe. The agenda will include world leading research from renowned speakers including:
- Gary Desir
Professor, Yale School of Medicine - Min Li
Professor, Department of Neuroscience & High Throughput Biology Center, John Hopkins School of Medicine - Merritt Maduke
Assistant Professor, Stanford University - George Miljanich
Chief Executive Officer, Airmid - Birgit Priest
Senior Research Fellow, Department of Ion Channels, Merck Research Laboratories - Frederick Sachs
Distinguished Professor, New York State University at Buffalo - David Triggle
Professor, New York State University at Buffalo - And many more…
The full two day agenda includes the following sessions:
- Calcium Channels
- Potassium Channels
- Sodium Channels
- Target Opportunities
- Therapeutics
To guarantee a high attendance at this exciting event Select Biosciences will maintain their traditional low registration fees and group booking discounts.
Full conference passes include admission to all sessions and the exhibition as well as conference documentation. Lunch, coffee breaks and the drinks reception provide ample time for networking and to continue discussions from the question and answer sessions.
To further increase the value of their trip, delegates can opt to attend the additional business tutorials and training courses which will be co-located with the conference. Details of the tutorials and courses are available on IonChannelTargets.com
The conferences division of Select Biosciences Ltd. is focused on organizing specialist biomedical meetings each year. Experts from both academia and commerce are invited to present timely information from current research through to commercial implementation of new technologies. These events also provide a unique networking facility and the opportunity to reach a highly targeted scientific audience.
www.selectbiosciences.com
Posted under North America, Press Releases, Targeted Libraries, USA and Canada | No Comments
CRELUX and ProQinase establish joint crystal-grade kinase protein and structures platform
Last Updated on Wednesday, 7 May 2008 05:30 Written by admin Wednesday, 7 May 2008 05:30
Munich and Freiburg, Germany, May 7, 2008 / b3c newswire / – CRELUX and ProQinase announced today that they have entered into a joint agreement to supply customers with crystal-grade protein kinases and readily available kinase complex structures.
Under the agreement, CRELUX and ProQinase will establish and continuously expand an off-the-shelf crystal-grade protein kinase portfolio, optimized and quality-controlled for successful crystallization. In addition, the two companies will work closely together to provide new crystal-grade protein or crystal structures, tailored to meet customers’ needs.
Recombinant protein kinases, optimized for crystallization, will be produced and exclusively marketed by ProQinase, while CRELUX will continue to provide customers with crystallization and x-ray crystallography services. CRELUX will support ProQinase by performing crystallization quality control for each crystal grade protein batch. At the same time, ProQinase will grant CRELUX privileged direct access to kinase crystal-grade protein.
“This new joint crystal-grade kinase platform offers tremendous advantages: It enables us to continue to focus on our core expertise – complex structure solution – while leveraging the expertise of ProQinase to significantly strengthen our capacities in protein expression,†commented Dr. Michael Schäffer, CEO of CRELUX.
“The combination of CRELUX’s expertise in protein crystallography and ProQinase’s know-how in kinase cloning and expression makes the two companies the partners of choice for all customers interested in kinase crystallography,†noted Dr. Christoph Schächtele, CEO of ProQinase.
CRELUX has used its state-of-the-art structural biology platform to solve more than 250 crystal and co-crystal structures for pharma and biotech companies. This platform encompasses all steps – from target cloning and expression all the way to high-throughput protein crystallization and in-house x-ray crystallography.
ProQinase, as part of its integrated protein kinase technology platform, offers more than 150 recombinant human protein kinases – all produced in-house – and provides all types of in vitro testing services, with more than 220 protein kinases.
Notes to editors
CRELUX GmbH ( www.crelux.com) provides fast and affordable access to co-crystal structures for biotech and pharma companies worldwide. Three dimensional structures of target-compound complexes are unique sources of information during the rational drug discovery process. Straightforward availability of structural data at an early stage of the drug development process significantly enhances productivity and success rates during hit selection, lead generation, and lead optimization. CRELUX has streamlined the processes of structure generation and solved hundreds of co-crystal structures using an integrated technology platform. In addition to customer designed projects crystallization conditions of numerous relevant therapeutic targets are available within the Off-The-Shelf Program of CRELUX. Off-The-Shelf target structures are delivered at a fixed price and short turn around times, facilitating affordable access to structural information.
ProQinase GmbH ( www.proqinase.com) provides an Integrated Protein Kinase Technology (iProKiTe®) Platform for preclinical drug development of protein kinase inhibitors. More than 150 highly active recombinant kinases are offered for sale and more than 220 kinases are available for in vitro testing services (HTS and selectivity profiling etc.). Cellular and in vivo test systems including orthotopic tumor models allow further testing of lead compounds. A Clinical biomarker analysis service supports the evaluation of clinical trials.
Posted under BioInformatics, Collaborations, Europe, Press Releases, Targeted Libraries | No Comments
Graffinity Announces Multitarget Drug Discovery Research Collaboration With Pfizer
Last Updated on Friday, 30 November 2007 08:28 Written by admin Friday, 30 November 2007 08:28
Heidelberg, Germany, November 29, 2007 /b3c newswire/ — Graffinity Pharmaceuticals GmbH announced today that it has entered into its second drug discovery collaboration with Pfizer, Inc. Through the collaboration, Graffinity will provide Pfizer with access to its proprietary, fragment-based screening technology for use in screening Pfizer drug targets. The agreement is Graffinity’s sixth discovery collaboration since it was established as an independent company in 2006.
Under the terms of the agreement, Graffinity will receive technology access fees and payments for follow-up chemistry for the generation of novel small molecule hits against a number of drug targets. Financial details of the transaction were not disclosed.
Mathias Woker, Chief Business Officer of Graffinity, remarked, â€We are pleased that Pfizer will be using our high-throughput approach to fragment screening. Our technology allows our partners to identify truly novel chemical entities against demanding drug targets. If desired, we even can give our customers reliable access to allosteric binders during our screens. The combination of these capabilities with a very deep and broad fragment library is what creates the value that our partners seek when working with usâ€.
Kristina Schmidt, CEO of Graffinity, stated, â€Graffinity was established almost two years ago as an independent company to commercialize its proprietary fragment-based discovery technology. To have entered into six collaborations in such a short period of time highlights the outstanding progress we have made, underscores the potential both of our technology and business model, and positions us as a leader in this growing area of drug discovery.â€
About Graffinity Pharmaceuticals GmbH – www.graffinity.com
Heidelberg, Germany based Graffinity Pharmaceuticals is a leader in the field of small molecule fragment based drug discovery. The company pursues high-profile drug discovery collaborations with leading pharmaceutical and biotechnology companies worldwide. Graffinity employs a flexible business model which allows it to tailor programs to the specific needs of each partner and offers numerous benefits to its customers on a straightforward fee-for-service basis. Graffinity’s fragment screening platform combines chemical microarrays with a proprietary method for the standardized, label-free detection of compound-protein interactions via SPR imaging. The company’s rapid and scalable drug discovery technology explores a rich chemical universe to identify drug fragments which address challenging drug targets. With its 110,000-compound library that contains 23,000 true fragments, Graffinity possesses one of the most diverse fragment libraries. Graffinity has established collaborations with pharmaceutical and biotechnology partners including Amgen, Boehringer-Ingelheim, Genentech, Pfizer and Merck-Serono.
Graffinity’s unique fragment based discovery platform has been invented in 1998, and has been in routine industrial use since 2002 in screening more than 60 drug targets.
Posted under Collaborations, Drug-Like Compounds, Europe, North America, Press Releases, Targeted Libraries | No Comments
7th Annual Protein Kinases Congress 10-12 March 2008 in Crowne Plaza Berlin City Centre, Berlin, Germany
Last Updated on Sunday, 4 November 2007 09:41 Written by admin Sunday, 4 November 2007 09:41
Innovating kinase inhibitor development is the key to successful clinical development. At Informa Life Sciences 7th Annual Protein Kinases Congress hear the latest thinking and strategies towards creating a selective inhibitor. Learn about new targets, industry trends in structure-based drug design, clinical case-studies and discuss the issue of cardiotoxicity.
For more information visit: http://www.iir-events.com/IIR-Conf/page.aspx?id=9547
Posted under Clinical Trials, Europe, Press Releases, Proteomics, Targeted Libraries | No Comments
NEW KINASE ProHit COMPOUND SETS
Last Updated on Tuesday, 30 October 2007 02:32 Written by admin Tuesday, 30 October 2007 02:32
OTAVA, the company that specializes in combinatorial chemistry, fluorescent probes and drug discovery technologies, offers unique ProHit compounds displaying inhibitory activity against distinct protein kinases.
ProHit Compound Sets are distributed on an exclusive basis and can be used in the development of drugs targeting protein kinase enzymes.
Every Kinase ProHit Compound Set is organized as a cluster of similar compounds having the following features:
- obtained by organic synthesis
- showed high inhibitory activity towards the targe (IC50 less than 1 uM for the most active compounds)
- have good drug-likeness
- showed chemical stability
- showed chemical feasibility
- free of Intellectual property
- checked in specialized databases to define patentability
Protein Kinase CK2 ProHit Set (CK2ProHit) is now available.
For more information, please contact us
http://www.otavachemicals.com
More Kinase ProHit Sets are on the way!
Posted under Europe, Targeted Libraries | No Comments
Bucks County’s Institute for Hepatitis and Virus Research and BioLeap Collaborate on New Discoveries
Last Updated on Thursday, 18 October 2007 01:31 Written by admin Thursday, 18 October 2007 01:30
New Hope, PA — (SBWIRE) — 10/10/2007 — Bucks County’s Institute for Hepatitis and Virus Research (IHVR) and BioLeap have entered into a collaboration to develop new therapeutic compounds for the treatment of Hepatitis C. Up to 50% of patients treated with current standard therapies do not respond adequately and often suffer serious side effects from the drugs. Thus there is a critical need for new tools to treat this disease. By combining BioLeap’s leading edge computational fragment-based design capabilities with the IHVR’s extensive experience and in-depth knowledge of viral diseases, the collaboration will result in new classes of lead drug molecules with novel modes-of-action.
Of particular interest to the IHVR is BioLeap’s proprietary technology that rapidly calculates the free energies, or affinities of interactions between small molecular fragments of potential drugs and biomolecular structures of the proteins they will target, displaying the distribution and orientation of these fragments. This information provides a unique insight into how small molecules bind into key protein binding sites that cannot be achieved from the static crystal structure alone, or from methods that can only measure the enthalpic properties of binding. In addition to lead discovery, the quantitative free-energy based analysis of protein-drug-fragment interactions adds significant value to the lead optimization process. In combination, this proprietary approach provides chemists and biologists the information they need to assemble, fragment by fragment, a completely new molecule that not only optimally binds to the targeted protein site but also has properties desirable in a drug, including solubility and bioavailability.
Commenting on the collaboration, BioLeap’s Gerry Evans, Executive Vice President of BioLeap, noted: “Dr. Tim Block and his team at the IHVR are renowned for their work in this field. We are very excited by the opportunity to focus our combined expertise on this important target.â€
Dr. Tim Block, president of the IHVR, is enthusiastic about the prospects for this collaboration. “One approach in discovering new treatments is the time and labor intensive process of screening tens or hundreds of thousands of molecules from compound libraries. BioLeap’s technology provides a potential shortcut by eliminating the need to screen compound libraries, while significantly broadening the field of chemical diversity. The molecules designed by BioLeap are not limited by what is present in any compound library. This greatly increases our odds of finding a potential drug that precisely targets the hepatitis C virus and that will not easily succumb to viral resistance. Once BioLeap has identified several candidate molecules, our scientists will test their effectiveness on the hepatitis C virus. Based on these results, we will repeat this iterative process until we have found the ideal drug.â€
About the Institute for Hepatitis and Virus Research:
Established as the research arm of the Hepatitis B Foundation, the mission of the Institute for Hepatitis and Virus Research is to use discovery science to find new therapies for viral hepatitis and liver cancer; to advance its research discoveries through traditional scholarship and educational opportunities; to nurture biotechnology through technology transfer and new company formation; and to promote public health outreach programs to improve the quality of life for those with viral hepatitis.
About BioLeap:
Bioleap is a leader in computational fragment-based drug design. The company’s proprietary design technology and process successfully addresses one of the biggest problems in preclinical drug discovery: limited chemical diversity of compound libraries. Development collaborations span a broad spectrum of target proteins including: kinases, nuclear hormone receptors, metalloenzymes, and metalloproteases.
Dr. Stephen Burley, SGX Pharmaceuticals–Keynote speaker at 3rd Modern Drug Discovery & Development
Last Updated on Thursday, 18 October 2007 01:26 Written by admin Thursday, 18 October 2007 01:26
(PRLog.Org) – Oct 17, 2007 – MONROVIA, CA – Dr. Stephen K. Burley, Chief Scientific Officer and Senior Vice-President Research at SGX Pharmaceuticals, Inc. located in San Diego, CA will give the Keynote presentation at GTCbio’s Drug Design & Lead Discovery conference – one of six tracks at the 3rd Modern Drug Discovery & Development Summit on November 28-30, 2007 at the Hyatt Regency San Francisco Airport.
Dr. Burley’s presentation will cover fragment-based discovery of selective, orally bioavailable tyrosine kinase inhibitors for targeted treatment of human cancers with examples from SGX’s FAST™ (Fragments of Active Structures) platform.
The fragment-based drug discovery platform utilizes high-throughput X-ray crystallography for lead identification/optimization. The process exploits crystallographic screening to detect, visualize and identify small ligands (MW 150-200) that are bound to the target protein. Each member of the FAST™ fragment/scaffold library was selected to be amenable to rapid chemical elaboration at two or three points of chemical diversity using parallel organic synthesis. Initial lead optimization involves using SGX’s knowledge of the co-crystal structure of the target-fragment complex and advanced computational chemistry tools to guide synthesis of small focused linear (one-dimensional) libraries. These linearly elaborated fragments/scaffolds are then evaluated with in vitro biochemical and cellular assays and co-crystal structure determinations. Thereafter, optimal variations at each point of chemical diversity are combined to synthesize focused combinatorial (two- or three-dimensional) libraries that are again examined with assays and crystallography. (The potential chemical diversity of the fully elaborated FAST™ fragment/scaffold library far exceeds 160 million compounds.) Active compound series are prioritized for further medicinal chemistry and compound development efforts using the results of in vitro and in vivo ADME and in vitro toxicology studies. Successful applications of the FAST™ fragment-based lead discovery/optimization process will be presented for a portfolio of well validated oncology targets.
The 3rd Modern Drug Discovery & Development Summit features over 150 speakers participating in 6 concurrent conferences, 6 study sessions and 3 pre-conference workshops. Tracks include Biological Therapeutics, Drug Delivery Technology, Translational Medicine, Drug Design and Lead Optimization, Emerging Targets, and Pharmaco – Kinetics, Dynamics, Genomics and Genetics. For more information, visit www.gtcbio.com.
Caliper Life Sciences Introduces EZ Reader Series for In-house Kinase Profiling
Last Updated on Wednesday, 8 August 2007 11:58 Written by Fred Wednesday, 8 August 2007 11:58
HOPKINTON, Mass., Aug. 7 /PRNewswire-FirstCall/ — Caliper Life Sciences, Inc. today launched the Caliper LabChip(R) EZ Reader(TM) Series, delivering a complete range of products for in-house kinase profiling. The series, which complements the existing LabChip 3000 system, Caliper’s most sophisticated system for drug discovery, includes the new EZ Reader II system, a bench-top reader to use for real-time kinetic analysis with push-button operation, and the EZ Reader system, formerly the DeskTop Profiler(TM) system. Each product in the EZ Reader Series utilizes Caliper’s LabChip microfluidic-based screening technology to yield high-quality, reproducible data to help pharmaceutical researchers more confidently qualify potential lead candidates.
The EZ Reader Series features innovative systems that rapidly profile compounds against a diverse kinase panel in a timely and cost-effective manner. The Series complements Caliper’s existing offerings for kinase profiling. The EZ Reader system features a four-sipper Caliper LabChip microfluidic device, while the EZ Reader II system provides a choice of either a 4-sipper or a 12-sipper LabChip device to run assays with up to three times higher throughput. The EZ Reader II system also enables real time kinetic analysis, allowing researchers to study enzyme behavior over time in mechanism-of-action (MOA) studies. Its compact, bench-top size and push-button operation delivers a high level of functionality without a large footprint or the need for highly skilled operators. Caliper’s ProfilerPro(TM) kinase reagent profiling kit, which allows broad range, rapid kinase profiling in-house, accompanies each system.
“The EZ Reader II system extends the benefits of Caliper’s LabChip technology to academic laboratories, small biotech companies and distributed therapeutic groups,” said Rick Bunch, Business Unit Manager, LabChip Systems, Caliper Life Sciences. “Its inclusion in the EZ Reader series demonstrates Caliper’s commitment to delivering technology and services that fulfill a broad range of customer needs.”
The EZ Reader II system is currently on display at the Drug Discovery & Development of Innovative Therapeutics (DDT) conference in Boston. For additional information, please visit Caliper Life Sciences at booth 628.
About Caliper Life Sciences
Caliper Life Sciences is a leading provider of cutting-edge technologies enabling researchers in the life sciences to create life-saving and enhancing medicines and diagnostic tests more quickly and efficiently. Caliper is aggressively innovating new technology to bridge the gap between in vitro assays and in vivo results and then translate those results into cures for human disease. Caliper’s portfolio of offerings includes state-of-the-art microfluidics, lab automation & liquid handling, optical imaging technologies, and discovery & development outsourcing solutions. For more information please visit http://www.caliperLS.com.
Caliper, LabChip, DeskTop Profiler, ProfilerPro and EZ Reader are trademarks of Caliper Life Sciences, Inc.
Posted under North America, Press Releases, Targeted Libraries | No Comments
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