1ohy

From Proteopedia

Revision as of 13:50, 30 October 2007

4-AMINOBUTYRATE-AMINOTRANSFERASE INACTIVATED BY GAMMA-ETHYNYL GABA

Overview

Gamma-aminobutyric acid aminotransferase (GABA-AT) is a pyridoxal, 5'-phosphate-dependent enzyme responsible for the degradation of the, inhibitory neurotransmitter GABA. GABA-AT is a validated target for, antiepilepsy drugs because its selective inhibition raises GABA, concentrations in brain. The antiepilepsy drug, gamma-vinyl-GABA, (vigabatrin) has been investigated in the past by various biochemical, methods and resulted in several proposals for its mechanisms of, inactivation. In this study we solved and compared the crystal structures, of pig liver GABA-AT in its native form (to 2.3-A resolution) and in, complex with vigabatrin as well as with the close analogue, gamma-ethynyl-GABA (to 2.3 and 2.8 A, respectively). Both inactivators, form a covalent ternary adduct with the active ... [(full description)]

About this Structure

1OHY is a [Single protein] structure of sequence from [Sus scrofa] with FE, PLP and S as [ligands]. Active as [4-aminobutyrate transaminase], with EC number [2.6.1.19]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

Reference

Structures of gamma-aminobutyric acid (GABA) aminotransferase, a pyridoxal 5'-phosphate, and [2Fe-2S] cluster-containing enzyme, complexed with gamma-ethynyl-GABA and with the antiepilepsy drug vigabatrin., Storici P, De Biase D, Bossa F, Bruno S, Mozzarelli A, Peneff C, Silverman RB, Schirmer T, J Biol Chem. 2004 Jan 2;279(1):363-73. Epub 2003 Oct 8. PMID:14534310

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