Bivalent inhibitors of glutathione S-transferase: The effect of spacer length on isozyme selectivity

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 14, 2006, Pages 3780-3783

  Maeda, Dean Y ^a   Mahajan, Sumit S ^b   Atkins, William M ^b   Zebala, John A ^a  

^a SYNTRIX BIOSYSTEMS INC   (United States)

^b UNIVERSITY OF WASHINGTON   (United States)

Author keywords

Bivalent inhibitor; Glutathione S transferase inhibitor; Selective bivalency

Indexed keywords

ENZYME INHIBITOR; ETACRYNIC ACID; GLUTATHIONE TRANSFERASE; ISOENZYME;

ARTICLE; CATALYSIS; CONJUGATION; CYTOSOL; DIMERIZATION; DRUG BINDING SITE; DRUG DESIGN; DRUG SELECTIVITY; ENZYME SUBSTRATE COMPLEX; IC 50; PROTEIN DOMAIN; PROTEIN FAMILY;

ANTINEOPLASTIC AGENTS; BINDING SITES; CELL LINE, TUMOR; DIMERIZATION; ENZYME INHIBITORS; ETHACRYNIC ACID; GLUTATHIONE TRANSFERASE; HUMANS; INHIBITORY CONCENTRATION 50; ISOENZYMES; LIGANDS; SUBSTRATE SPECIFICITY;

EID: 33746495603     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.04.041     Document Type: Article

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15. M values (A1-1: 350 and 720 μM; P1-1: 150 and 820 μM). Rates of product formation were obtained by measuring absorption at 340 nM for 1 min on Beckmann DU 7400 spectrophotometer. Inhibitor concentrations spanned four orders of magnitude and experiments were carried out in triplicate. The resulting data were then fitted to sigmoidal dose-response curves using GraphPad Prism (GraphPad Software Inc., San Diego, CA) to determine the 50% inhibitory concentration.