✦ LIBER ✦

Replacements for lysine in l-seryl-l-lysyl dipeptide amide inhibitors of candida albicans myristoyl-CoA:protein N-myristoyltransferase

✍ Scribed by David L. Brown; Balekudru Devadas; Hwang-Fun Lu; Srinivasan Nagarajan; Mark E. Zupec; Sandra K. Freeman; Charles A. McWherter; Daniel P. Getman; James A. Sikorski

Publisher: Elsevier Science
Year: 1997
Tongue: English
Weight: 225 KB
Volume: 7
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(97)00030-9

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✦ Synopsis

A survey of potential cyclic and acyclic lysine replacements in known L-seryl-L-lysyl dipeptide inhibitors of C. albicans NMT identified the thioether 16 and glycinamide 18 as submicromolar inhibitors of C. albicans NMT, which retained good selectivity over the human enzyme. All of the heterocyclic tysine mimetics that were examined exhibited dramatically weaker affinity with the fungal enzyme.