Literature summary for 2.6.1.19 extracted from

Lee, H.; Doud, E.H.; Wu, R.; Sanishvili, R.; Juncosa, J.I.; Liu, D.; Kelleher, N.L.; Silverman, R.B.
Mechanism of inactivation of gamma-aminobutyric acid aminotransferase by (1S,3S)-3-amino-4-difluoromethylene-1-cyclopentanoic acid (CPP-115) (2015), J. Am. Chem. Soc., 137, 2628-2640.

Crystallization (Commentary)

Crystallization (Comment)	Organism
crystal structures of enzyme inactivated by inhibitors (1S,2S,3E)-2-amino-3-(fluoromethylidene)cyclopentanecarboxylic acid and (1S,2S,3Z)-2-amino-3-(fluoromethylidene)cyclopentanecarboxylic acid. The Arg445-Glu270 salt bridge in the active site is disrupted during inactivation, and Glu270 rotates away from its original position to accommodate a weak electrostatic or hydrogen-bonding interaction between the formyl group of a metabolite and Arg445	Sus scrofa

Crystallization (Comment)

Organism

crystal structures of enzyme inactivated by inhibitors (1S,2S,3E)-2-amino-3-(fluoromethylidene)cyclopentanecarboxylic acid and (1S,2S,3Z)-2-amino-3-(fluoromethylidene)cyclopentanecarboxylic acid. The Arg445-Glu270 salt bridge in the active site is disrupted during inactivation, and Glu270 rotates away from its original position to accommodate a weak electrostatic or hydrogen-bonding interaction between the formyl group of a metabolite and Arg445

Sus scrofa

Inhibitors

Inhibitors	Comment	Organism	Structure
(1S,2S,3E)-2-amino-3-(fluoromethylidene)cyclopentanecarboxylic acid	monofluorinated analog of inhibitor CPP-115. Compound produces a metabolite that induces disruption of the Glu270-Arg445 salt bridge of GABA transaminase to accommodate interaction between the metabolite formyl group and Arg445. The inactivation mechanism is initiated by Schiff base formation with the active site pyridoxal 5'-phosphate, followed by gamma-proton removal	Sus scrofa
(1S,2S,3Z)-2-amino-3-(fluoromethylidene)cyclopentanecarboxylic acid	monofluorinated analog of inhibitor CPP-115. Compound produces a metabolite that induces disruption of the Glu270-Arg445 salt bridge of GABA transaminase to accommodate interaction between the metabolite formyl group and Arg445. The inactivation mechanism is initiated by Schiff base formation with the active site pyridoxal 5'-phosphate, followed by gamma-proton removal	Sus scrofa

Organism

Organism	UniProt	Comment	Textmining
Sus scrofa	P80147	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
brain	-	Sus scrofa	-