Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine
The first hydrolytically stable phosphocreatine (CrP) analogs with a CH2-P isostere in place of the NH-P linkage have been synthesized and found to inhibit creatine kinase (CK) with potencies in the low mM range. The closest structural analog of CrP, 2, was found to have a K(i) (1.4 mM) near the K(m) of CrP (2.5 mM), making it the most potent known reversible inhibitor of CK.
Bergnest, G; Kaddurah-Daouk, R
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