The first potent inhibitor of mammalian group X secreted phospholipase A2: elucidation of sites for enhanced binding.
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ABSTRACT:
SUBMITTER: Smart BP
PROVIDER: S-EPMC2963729 | biostudies-literature | 2006 May
REPOSITORIES: biostudies-literature
Publications
The first potent inhibitor of mammalian group X secreted phospholipase A2: elucidation of sites for enhanced binding.
Smart Brian P BP Oslund Rob C RC Walsh Laura A LA Gelb Michael H MH
Journal of medicinal chemistry 20060501 10
Using the X-ray structure of human group X secreted phospholipase A(2) (hGX), we carried out structure-based design of indole-based inhibitors and prepared the compounds using a new synthetic route. The most potent compound inhibited hGX and the mouse orthologue with an IC(50) of 75 nM. This compound is the most potent hGX inhibitor reported to date and was also found to inhibit a subset of the other mouse and human sPLA(2)s. ...[more]
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