메뉴 건너뛰기




Volumn 2, Issue 12, 2007, Pages 1730-1740

Stereochemical and steric control of the UDP-glucuronosyltransferase- catalyzed conjugation reaction: A rational approach for the design of inhibitors for the human UGT2B7

Author keywords

3D QSAR; Eudismic analysis; Inhibition; Metabolism; UGT

Indexed keywords

ENZYME INHIBITOR; GLUCURONOSYLTRANSFERASE; UGT2B7 PROTEIN, HUMAN; UNCLASSIFIED DRUG;

EID: 48849084735     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.200700122     Document Type: Article
Times cited : (6)

References (39)
  • 5
    • 0037396292 scopus 로고    scopus 로고
    • The term catalytic promiscuity has been originally used to describe the ability of an enzyme to catalyze an adventitious secondary activity at the active site responsible for the primary activity see S. D. Copley, Curr. Opin. Chem. Biol. 2003, 7, 265-272, However, in the case of metabolic enzymes like UGTs the term has been used to depict their overlapping substrate selectivities
    • The term catalytic promiscuity has been originally used to describe the ability of an enzyme to catalyze an adventitious secondary activity at the active site responsible for the primary activity (see S. D. Copley, Curr. Opin. Chem. Biol. 2003, 7, 265-272). However, in the case of metabolic enzymes like UGTs the term has been used to depict their overlapping substrate selectivities.
  • 22
    • 78650381453 scopus 로고    scopus 로고
    • c) I. Bichlmaier, Drug Metab. Rev. 2006, 38 (Suppl. 2), 185-186.
    • (2006) Drug Metab. Rev , vol.38 , Issue.SUPPL. 2 , pp. 185-186
    • Bichlmaier, I.1
  • 30
    • 54549108319 scopus 로고    scopus 로고
    • MOE Molecular Modeling Software, version 2006.8; Chemical Computing Group, Montreal, Canada
    • MOE Molecular Modeling Software, version 2006.8; Chemical Computing Group, Montreal, Canada.
  • 31
    • 54549103908 scopus 로고    scopus 로고
    • SYBYL Molecular Modeling Software, version 7.2; Tripos Inc, St. Louis, USA
    • SYBYL Molecular Modeling Software, version 7.2; Tripos Inc., St. Louis, USA.
  • 33
    • 54549117467 scopus 로고    scopus 로고
    • Eudismic analysis investigates the interaction between chiral compounds and their biological targets. This analytical method is used in drug design and development to increase the selectivity and potency of a chiral lead compound toward the pharmacological target. The term eudismic analysis was derived from the expressions eutomer and distomer. The more biologically active stereoisomer is termed eutomer, the less active one is called distomer. See: a R. Crossley, Chirality and the biological activity of drugs, CRC, Boca Raton, 1995, p. 196;
    • Eudismic analysis investigates the interaction between chiral compounds and their biological targets. This analytical method is used in drug design and development to increase the selectivity and potency of a chiral lead compound toward the pharmacological target. The term eudismic analysis was derived from the expressions eutomer and distomer. The more biologically active stereoisomer is termed eutomer, the less active one is called distomer. See: a) R. Crossley, Chirality and the biological activity of drugs, CRC, Boca Raton, 1995, p. 196;
  • 35
    • 54549126292 scopus 로고    scopus 로고
    • The eudismic ratio was calculated by dividing the amount of formed eutomer glucuronide by the amount of formed distomer glucuronide. The eudismic ratio therefore expressed the preferential formation of the glucuronide of one compound over that of its respective stereoisomer
    • The eudismic ratio was calculated by dividing the amount of formed eutomer glucuronide by the amount of formed distomer glucuronide. The eudismic ratio therefore expressed the preferential formation of the glucuronide of one compound over that of its respective stereoisomer.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.