Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UNIPROT:P80404 (
GABA transaminase
)
786
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
omega-Monofluoromethyl and omega-difluoromethyl analogues of the known substrates of
GABA-T
, beta-alanine, gamma-aminobutyric acid, and
5-aminopentanoic acid
, are time-dependent inhibitors of purified 4-aminobutyrate: 2-oxoglutarate aminotransferase (
GABA-T
). The inhibitory activity decreases with increasing chain length. In vitro, inhibitory activity decreases with increasing fluorine substitution of the methyl group. In vivo, beta-difluoromethyl-beta-alanine and 2,4-difluoro-3-aminobutyric acid are the most potent
GABA-T
inhibitors ever reported. Trifluoromethyl derivatives are devoid of
GABA-T
inhibitory activity in vitro or in vivo.
...
PMID:omega-Fluoromethyl analogues of omega-amino acids as irreversible inhibitors of 4-aminobutyrate:2-oxoglutarate aminotransferase. 679 12
