2-Iminobiotin is an inhibitor of nitric oxide synthases

Biochemical and Biophysical Research Communications
S J SupS K Grant

Abstract

Nitric oxide synthase (NOS, EC 1.14.23) catalyzes the oxidation of the guanidino-nitrogen of L-arginine to form nitric oxide and L-citrulline. 2-Iminobiotin was found to be a reversible inhibitor of murine iNOS and rat n-cNOS with Ki values of 21.8 and 37.5 microM, respectively. The urea and thiourea analogs, biotin and thiobiotin, were not inhibitors of NOS, indicating that the guanidino group of 2-iminobiotin is essential for binding. 2-iminobiotin carboxy derivatives were also inhibitors of iNOS which indicates that the free carboxyl group is not required for binding. 2-Iminobiotin is a novel, potent inhibitor of NO biosynthesis and may be a useful reagent in the understanding of binding-site interactions for this important class of enzymes.

Citations

Jan 29, 2005·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Evelyn R W van den TweelFloris Groenendaal
Feb 23, 1996·Biochemical Pharmacology·G J Southan, C Szabó
Jun 1, 2006·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Cora H A NijboerCobi J Heijnen
May 30, 2015·Chemical Communications : Chem Comm·Wen Xiu RenJong Seung Kim
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Sep 7, 2002·Stroke; a Journal of Cerebral Circulation·Cacha Peeters-ScholteFloris Groenendaal

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