Article
Mechanistic and structural requirements for active site labeling of phosphoglycerate mutase by spiroepoxides.
Molecular bioSystems - 1 Jul 2007
Evans Michael J, Morris Garrett M, Wu Jane, Olson Arthur J, Sorensen Erik J, Cravatt Benjamin F
Abstract excerpt
We recently reported the pharmacological screening of a natural products-inspired library of spiroepoxide probes, resulting in the discovery of an agent MJE3 that displayed anti-proliferative effects in human breast cancer cells. MJE3 was found to covalently inactivate phosphoglycerate mutase-1 (PGAM1), a glycolytic enzyme with postulated roles in cancer cell metabolism and proliferation. Considering that MJE3 is...
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