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Biotech / Medical : TELK -- Telik, Inc. -- Ignore unavailable to you. Want to Upgrade?

To: scaram(o)uche who wrote (52)	12/15/2000 3:04:41 PM
From: keokalani'nui	Read Replies (1) \| Respond to of 887

Since this is temporary chemokine thread... Re: Banyu 1: J Biol Chem 2000 Aug 25;275(34):25985-92 Related Articles, Books, LinkOut A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry. Sabroe I, Peck MJ, Van Keulen BJ, Jorritsma A, Simmons G, Clapham PR, Williams TJ, Pease JE Leukocyte Biology Section, Biomedical Sciences Division, Sir Alexander Fleming Building, Imperial College School of Medicine, South Kensington, London SW7 2AZ, United Kingdom. We describe a small molecule chemokine receptor antagonist, UCB35625 (the trans-isomer J113863 published by Banyu Pharmaceutical Co., patent WO98/04554), which is a potent, selective inhibitor of CCR1 and CCR3. Nanomolar concentrations of UCB35625 were sufficient to inhibit eosinophil shape change responses to MIP-1alpha, MCP-4, and eotaxin, while greater concentrations could inhibit the chemokine-induced internalization of both CCR1 and CCR3. UCB35625 also inhibited the CCR3-mediated entry of the human immunodeficiency virus-1 primary isolate 89.6 into the glial cell line, NP-2 (IC(50) = 57 nm). Chemotaxis of transfected cells expressing either CCR1 or CCR3 was inhibited by nanomolar concentrations of the compound (IC(50) values of CCR1-MIP-1alpha = 9.6 nm, CCR3-eotaxin = 93.7 nm). However, competitive ligand binding assays on the same transfectants revealed that considerably larger concentrations of UCB35625 were needed for effective ligand displacement than were needed for the inhibition of receptor function. Thus, it appears that the compound may interact with a region present in both receptors that inhibits the conformational change necessary to initiate intracellular signaling. By virtue of its potency at the two major eosinophil chemokine receptors, UCB35625 is a prototypic therapy for the treatment of eosinophil-mediated inflammatory disorders, such as asthma and as an inhibitor of CCR3-mediated human immunodeficiency virus-1 entry. PMID: 10854442, UI: 20408936 More to the business end: profiles.wisi.com And, re ChemoCentryx, the only way to get there is via tech's 49% ownership (which looks like it cost them only $5m and still got them diagnostic rights!). So far, nothing cheap about any of them.