Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
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ABSTRACT:
SUBMITTER: Oslund RC
PROVIDER: S-EPMC2965735 | biostudies-literature | 2008 Aug
REPOSITORIES: biostudies-literature
Publications
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Oslund Rob C RC Cermak Nathan N Gelb Michael H MH
Journal of medicinal chemistry 20080708 15
We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human group X sPLA2 crystal structure, we prepared a highly potent and selective indole-based inhibitor of this enzyme. Also, we report human and mouse group IIA and IIE specific inhibitors and a substituted 6,7-benzoindole that inhibits nearly all human and mouse sPLA2s in the low nanom ...[more]
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