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2bk5
From Proteopedia
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Revision as of 14:35, 30 October 2007
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HUMAN MONOAMINE OXIDASE B: I199F MUTANT IN COMPLEX WITH ISATIN
Overview
Several reversible inhibitors selective for human monoamine oxidase B (MAO, B) that do not inhibit MAO A have been described in the literature. The, following compounds: 8-(3-chlorostyryl)caffeine, 1,4-diphenyl-2-butene, and trans,trans-farnesol are shown to inhibit competitively human, horse, rat, and mouse MAO B with K(i) values in the low micromolar range but are, without effect on either bovine or sheep MAO B or human MAO A. In, contrast, the reversible competitive inhibitor isatin binds to all known, MAO B and MAO A with similar affinities. Sequence alignments and the, crystal structures of human MAO B in complex with 1,4-diphenyl-2-butene or, with trans,trans-farnesol provide molecular insights into these, specificities. These inhibitors span the substrate and entrance cavities, ... [(full description)]
About this Structure
2BK5 is a [Single protein] structure of sequence from [Homo sapiens] with FAD and ISN as [ligands]. Active as [Amine oxidase (flavin-containing)], with EC number [1.4.3.4]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
Reference
Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors., Hubalek F, Binda C, Khalil A, Li M, Mattevi A, Castagnoli N, Edmondson DE, J Biol Chem. 2005 Apr 22;280(16):15761-6. Epub 2005 Feb 14. PMID:15710600
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