2c67

From Proteopedia

Revision as of 09:24, 30 October 2007

MAO INHIBITION BY RASAGILINE ANALOGUES

Overview

Monoamine oxidases A and B (MAO A and B) catalyze the degradation of, neurotransmitters and represent drug targets for the treatment of, neurodegenerative disorders. Rasagiline is an irreversible, MAO, B-selective inhibitor that has been approved as a novel anti-Parkinson's, drug. In this study, we investigate the inhibition of recombinant human, MAO A and MAO B by several rasagiline analogues. Different substituents, added onto the rasagiline scaffold alter the binding affinity depending on, the position on the aminoindan ring and on the size of the substituent., Compounds with a hydroxyl group on either the C4 or the C6 atom inhibit, both isozymes, whereas a bulkier substituent such as a carbamate is, tolerated only at the C4 position. The 1.7 A crystal structure of MAO B in, complex ... [(full description)]

About this Structure

2C67 is a [Single protein] structure of sequence from [Homo sapiens] with FAD and RM1 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

Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis., Binda C, Hubalek F, Li M, Herzig Y, Sterling J, Edmondson DE, Mattevi A, J Med Chem. 2005 Dec 29;48(26):8148-54. PMID:16366596

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