Discovery and optimization of (R)-prolinol-derived agonists of the Growth Hormone Secretagogue receptor (GHSR).

Weixu Zhai,Neil Flynn,Daniel A Longhi,Joseph A Tino,Brian J Murphy,Dorothy Slusarchyk,David A Gordon,Anna Pendri,Shuhao Shi,Robert Stoffel,Baoqing Ma,Michael J Sofia,Samuel W Gerritz

Bioorganic & Medicinal Chemistry Letters（2008）

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摘要

The discovery of single-digit nanomolar full agonists (e.g., 10b) of the Growth Hormone Secretagogue receptor (GHSR) is reported, starting with a micromolar screening hit identified from a GPCR-targeted solid-phase library. The ‘library pedigree’ of this series greatly facilitated its rapid optimization.

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关键词

Solid-phase library,Hit to lead,Combinatorial chemistry,Non-additive SAR,Non-linear SAR,Growth hormone secretagogue receptor,GHSR,G-protein coupled receptor,GPCR,Solid-phase synthesis,Parallel synthesis,GPCR agonist,Matrix library

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