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. 1999 Aug 5;9(11):1511–1516. doi: 10.1016/S0960-894X(99)00219-X

Design of the first highly potent and selective aminopeptidase N (EC 3.4.11.2) inhibitor

Huixiong Chen 1, Bernard P Roques 1,∗, Marie-Claude Fournié-Zaluski 1
PMCID: PMC7172755  PMID: 10386926

Abstract

A series of phosphinic compounds mimicking the transition state of substrates hydrolysed by aminopeptidase N (EC 3.4.11.2) were synthesized. These new compounds have potent inhibitory activities with Ki values in the nanomolar range. These derivatives behave as the most potent APN inhibitors designed to date.

Keywords: Enzyme inhibitors / Phosphinic acids and derivatives / Resolution

A series of phosphinic derivatives designed to inhibit aminopeptidase N (EC 3.4.11.2) were synthesized, to act as “transition state analogs”. They have potent inhibitory activities on APN with Ki values in the nanomolar range, and are highly selective versus other metallopeptidases.

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