Evaluation of phosphorus-containing inhibitors of γ-glutamyl hydrolase

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 12, 1998, Pages 1521-1524

  Rodriguez, Chester E ^a   Holmes, H Michael ^a   Mlodnosky, Karyn L ^a   Lam, Vinh Q ^a   Berkman, Clifford E ^a  

^a SAN FRANCISCO STATE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

GAMMA GLUTAMYL HYDROLASE; HYDROLASE INHIBITOR; METHOTREXATE; PHOSPHONAMIDATE ESTER DERIVATIVE; PHOSPHONAMIDOIC ACID DERIVATIVE; PHOSPHORAMIDATE ESTER DERIVATIVE; PHOSPHORUS DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG MECHANISM; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; STRUCTURE ACTIVITY RELATION;

DRUG EVALUATION; ENZYME INHIBITORS; GAMMA-GLUTAMYL HYDROLASE; KINETICS; PHOSPHORUS; PHOSPHORYLATION;

EID: 0032537528     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00253-4     Document Type: Article

References (16)

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12. i values of 1a and 1b were 0.06 and 0.04, respectively.
13. 2+) of 0.015 units γ-GH (Carboxypeptidase G; Sigma Chemical Co., St. Louis MO) was added 100 μL inhibitor solution(1a or 2b dissolved in water) or 100 μL water as control. The enzyme reaction was initiated by the addition of 100 μL substrate (MTX) and monitored at 320 nm for absorbance decreases due to substrate consumption. For Lineweaver-Burk studies, substrate concentrations were varied from 5 to 50 μM and inhibitor concentrations were varied from 0 to 8 mM. For Dixon analyses, inhibitor concentrations were varied from 0 to 8 mM. All data was collected in at least triplicate, averaged, and presented with standard errors.
14. 2+) and monitored at 320 nm for absorbance decreases due to substrate consumption. All data was collected in triplicate, averaged, and presented with standard errors.
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