Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Bergnest, G; Kaddurah-Daouk, R

Published Date

  • April 22, 1997

Published In

Volume / Issue

  • 7 / 8

Start / End Page

  • 1021 - 1026

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/S0960-894X(97)00161-3

Citation Source

  • Scopus