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Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.

Abstract：

:We disclose the first selective, nonpeptidic, small-molecule somatostatin receptor subtype 5 (SST5R) antagonists that were identified by a chemogenomics approach based on the analysis of the homology of amino acids defining the putative consensus drug binding site of SST5R. With this strategy, opioid, histamine, dopamine, and serotonine receptors were identified as the closest neighbors of SST5R. The H1 antagonist astemizole was chosen as a seed structure and subsequently transformed into a SST5 receptor antagonist with nanomolar binding affinity devoid of the original target activity.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Martin RE,Green LG,Guba W,Kratochwil N,Christ A

doi

10.1021/jm701143p

subject

Has Abstract

pub_date

2007-12-13 00:00:00

pages

6291-4

issue

25

eissn

0022-2623

issn

1520-4804

journal_volume

50

pub_type

杂志文章

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