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Literature summary for 2.5.1.59 extracted from

  • Mansha, M.; Kumari, U.U.; Cournia, Z.; Ullah, N.
    Pyrazole-based potent inhibitors of GGT1 Synthesis, biological evaluation, and molecular docking studies (2016), Eur. J. Med. Chem., 124, 666-676 .
    View publication on PubMed
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Crystallization (Commentary)

Crystallization (Comment) Organism
molecular docking of inhibitor (S)-N-(1-amino-3-(4-fluorophenyl)-1-oxopropan-2-yl)-4-((1-(3,4-dichlorophenyl)-4-(2-(methylthio)ethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanamide shows several hydrogen bonding interactions and pi-pi contacts to the binding pocket of GGT1 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-N-(1-amino-3-(4-fluorophenyl)-1-oxopropan-2-yl)-4-((1-(3,4-dichlorophenyl)-4-(2-(methylthio)ethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanamide potent GGT1 inhibitor, anti-proliferative efficacy against MDA-MB-231 cells has an IC50 value of 0.0076 mM Homo sapiens
(S)-N-(1-amino-3-(4-methoxyphenyl)-1-oxopropan-2-yl)-4-((1-(3,4-dichlorophenyl)-4-(2-(methylthio)ethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanamide potent GGT1 inhibitor Homo sapiens
GGTI-DU40
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 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P49354 and P49356 P49354 i.e. subunit alpha, P49356 i.e. subunit beta, cf. EC 2.5.1.58
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Source Tissue

Source Tissue Comment Organism Textmining
MDA-MB-231 cell
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 Homo sapiens
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IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0024
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 pH 7.4, 30°C Homo sapiens (S)-N-(1-amino-3-(4-fluorophenyl)-1-oxopropan-2-yl)-4-((1-(3,4-dichlorophenyl)-4-(2-(methylthio)ethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanamide
0.0031
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 pH 7.4, 30°C Homo sapiens (S)-N-(1-amino-3-(4-methoxyphenyl)-1-oxopropan-2-yl)-4-((1-(3,4-dichlorophenyl)-4-(2-(methylthio)ethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanamide