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Biotech / Medical : Smithkline Beecham (SBH)

SBH 9.940

+0.2%

3:59 PM EDT

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To: Mike Battin who wrote (34)	6/5/1998 4:42:00 PM
From: Henry Niman	of 61

Here's the abstract: Discovery Of A Small Molecule G-Csf Mimic Jonathan I. Rosen, Ph.D., Senior Director, Transcription Research and New Leads Discovery, Ligand Pharmaceuticals, Inc. The JAK/STAT signal transduction pathway utilized by many cytokines can be exploited to develop high throughput screens for small molecule cytokine modulators. We applied this approach to the discovery of G-CSF mimics and have identified a non-peptidyl small molecule capable of activating granulocyte-colony stimulating factor (G-CSF) signal transduction pathways. This compound induces both the biochemical and cellular phenotypic responses characteristic of G-CSF. Remarkably, this compound is active in vivo with an efficacy similar to recombinant G-CSF. The identification of this compound provides proof of principle for drug discovery using JAK/STAT-based assays, and shows for the first time that a small non-peptidyl molecule can trigger the selective activation of a protein hormone receptor.

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