Design and Mechanism of Tetrahydrothiophene-Based γ-Aminobutyric Acid Aminotransferase Inactivators
نویسندگان
چکیده
منابع مشابه
Mechanism of Inactivation of γ-Aminobutyric Acid Aminotransferase by (1S,3S)-3-Amino-4-difluoromethylene-1-cyclopentanoic Acid (CPP-115)
γ-Aminobutyric acid aminotransferase (GABA-AT) is a pyridoxal 5'-phosphate (PLP)-dependent enzyme that degrades GABA, the principal inhibitory neurotransmitter in mammalian cells. When the concentration of GABA falls below a threshold level, convulsions can occur. Inhibition of GABA-AT raises GABA levels in the brain, which can terminate seizures as well as have potential therapeutic applicatio...
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Since the cloning of the first γ-aminobutyric acid (GABA) transporter (GAT1; SLC6A1) from rat brain in 1990, more than 50 published studies have provided structure-function information on investigator-designed rat and mouse GAT1 mutants. To date, more than 200 of 599 GAT1 residues have been subjected to mutagenesis experiments by substitution with different amino acids, and the resulting transp...
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State Key Laboratory of Microbial Resources and Dept. of Industrial 4 Microbiology and Biotechnology, Institute of Microbiology, Chinese Academy of 5 Sciences, Beijing 100101, PR China; Key Laboratory of Agricultural and 6 Environmental Microbiology, Wuhan Institute of Virology, Chinese Academy of 7 Sciences, Wuhan 430071, People's Republic of China 8 9 Running title 10 GABA uptake system in C....
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ژورنال
عنوان ژورنال: Journal of the American Chemical Society
سال: 2015
ISSN: 0002-7863,1520-5126
DOI: 10.1021/jacs.5b01155