Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 25, Pages 6291-6294Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm701143p
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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 HI 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.
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