Document Report Card

ID: ALA1121710

Journal: J Med Chem

Title: alpha-Ethynyl and alpha-vinyl analogues of ornithine as enzyme-activated inhibitors of mammalian ornithine decarboxylase.

Authors: Danzin C, Casara P, Claverie N, Metcalf BW.

Abstract: alpha-Ethynyl- and alpha-vinylornithine were designed and synthesized as potential enzyme-activated inhibitors of mammalian ornithine decarboxylase. These two new inhibitors produce both immediate and time-dependent inhibition of rat liver ornithine decarboxylase in vitro. The inhibitions exhibition saturation kinetics. The apparent dissociation constants (KI) are 10 and 810 microM, and the times of half-inactivation at infinite concentration of inhibitor (t1/2) are 8.5 and 27 min, respectively, for alpha-ethynyl- and alpha-vinylornithine. In rats, alpha-ethynylornithine causes a rapid dose-dependent decrease of ornithine decarboxylase activity in prostate and, to a lesser extent, in thymus and testis.

CiteXplore: 7205870

DOI: 10.1021/jm00133a005