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Chemical Genetic Studies Cite ChemBridge Corporation’s DIVERSet Compound Collection


10/19/2005 5:13:03 PM

San Diego, CA, March 15, 2005 /PRNewswire -- ChemBridge is pleased to announce a recent stream of publications reporting active small molecules using DIVERSet as their primary screening library. DIVERSet is a small molecule collection of 50,000 structures, designed as a universal screening library, covering the broadest part of pharmacophore diversity space with the minimum number of compounds. DIVERSet is particularly useful for primary screening against a wide range of biological targets, including those where no structural information is available.The following is a brief synopsis of the published findings:

Harvard University has published work on an inhibitor of elF2á dephosphorylation that protects cells from ER (endoplasmic reticulum) Stress (Boyce, M.; Bryant, K. F.; Jousse, C.; Long, K.; Harding, H. P.; Scheuner, D.; Kaufman, R. J.; Ma, D.; Coen, D. M.; Ron, D.; Yuan, J; A Selective Inhibitor of eIF2á Dephosphorylation Protects Cells from ER Stress. Science 2005, 307, 935-939). One particular compound, named Salubrinal by the Harvard team, shows particular promise for this application. ER Stress is responded to by a process termed the Unfolded Protein Response (UPR) and dysfunction of this response has been implicated in several disease states including diabetes, Alzheimer’s disease, and broad viral infection.

The action of Salubrinal is very specific for the phosphatase complex consisting of the serine/threonine phosphatase PP1 with its non-enzymatic co-factor GADD34.

In an unrelated mechanistic study, a second Harvard group reported the identification of 2 structurally similar compounds, named Eeyarestatin I & II, that inhibit a step in a protein degradation pathway, allowing further study into the dislocation pathway for type I membrane proteins (Fiebiger, E.; Hirsch, C.; Vyas, J. M.; Gordon, E.; Ploegh, H. L.; Tortorella, D.; Dissection of the Dislocation Pathway for Type I Membrane Proteins with a New Small Molecule Inhibitor, Eeyarestatin. Molecular Biology of the Cell 2004, 15, 1635-1646).

A Colorado based biotech company, Myogen, Inc., released new results (Harrison, B. C.; Roberts, C. R.; Hood, D. B.; Sweeney, M.; Gould, J. M.; Bush, E. W.; McKinsey, T. A.; The CRM1 Nuclear Export Receptor Controls Pathological Cardiac Gene Expression. Molecular and Cellular Biology 2004, 24 (24), 10636-10649) based on an earlier DIVERSet screen by yet another Harvard group (Kau, T. R.; Schroeder, F.; Ramaswamy, S.; Wojciechowski, C.L.; Zhao, J. J.; Roberts, T. M.; Clardy, J.; Sellers, W. R.; Silver, P. A.; A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells. Cancer Cell 2003, 4, 463 476) identified a group of CRM1 inhibitors as part of a mechanistic study into the control of Cardiac Gene Expression and cardiac hypertrophy.

A collaborative effort by groups including Boston University Medical School (USA), Guy’s Hospital (UK), and the Max Delbruck Centre (Germany) have disclosed results for a small molecule identified from DIVERSet that suppresses Huntington’s disease (HD)-mediated neurodegeneration in vivo (Zhang, X.; Smith, D. L.; Meriin, A. B.; Engemann, S.; Russel, D. E.; Roark, M.; Washington, S. L.; Maxwell, M. M.; Marsh, J. L.; Thompson, L. M.; Wanker, E. E.; Young, A. B.; Housman, D. E.; Bates, G. P.; Sherman, M. Y.; Kazantsev, A. G.; A potent small molecule inhibits polyglutamine aggregation in Huntington’s disease neurons and suppresses neurodegeneration in vivo. PNAS 2004, 102 (3), 892-897). The molecule inhibits the polyglutamine (polyQ) aggregation familiar to Huntington’s Disease pathology. Further studies have identified highly effective molecules that suppress the polyQ aggregation and may lead to effective HD therapies.

A group at Stanford University have identified inhibitors of auxin transcriptional activation from DIVERSet (Armstrong, J. I.; Yuan, S.; Dale, J. M.; Tanner, V. N.; Theologis, A.; Identification of inhibitors of auxin transcriptional activation by means of chemical genetics in Arabidopsis. PNAS 2004, 101 (41), 14978-14983). This mechanistic chemical genetics study identified several small molecules interfering with Auxin modulated plant development pathways. This research has the potential to isolate Auxin-dependant signalling network components and will significantly aid the study of Auxin participation in plant development.

About ChemBridge ChemBridge Corporation, www.chembridge.com, is a leading global discovery chemistry CRO with an impeccable track record of quality and deliverability. The privately-held, self-funded ChemBridge was founded in Chicago in 1993 and has grown to a global company with 350 employees. ChemBridge has its corporate headquarters in San Diego, European offices in the UK, and a marketing agency in Japan. It also operates a large, state-of-the-art offshore discovery chemistry research site in Moscow, Russia. Over 400 pharmaceutical and biotech companies and universities worldwide have taken advantage of ChemBridge’s portfolio of advanced discovery chemistry services and products, including its library of 600,000 diverse drug-like small molecule compounds. Contact: ChemBridge Corporation Jennifer Le Page Sr. Sales & Marketing Manager Phone: 1-858-451-7400, ext. 210



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