Download Conjugation—Deconjugation Reactions in Drug Metabolism and by D. J. Clarke, B. Burchell (auth.), Professor Frederick C. PDF

By D. J. Clarke, B. Burchell (auth.), Professor Frederick C. Kauffman Ph.D. (eds.)

Advances in molecular biology describing vital enzyme platforms enthusiastic about drug conjugation and deconjugation reactions and up to date paintings indicating the significance of drug and xenobiotic conjugates as shipping sorts of biologically energetic compounds are reviewed comprehensively. half One describes molecular occasions linked to the expression and law of transferases and hydrolases considering part II drug conjugation and deconjugation. half offers with the legislation of section II conjugation, and half 3 stories seriously the significance of drug conjugates in pharmacology and toxicology. This quantity is an updated resource of data in this subject and may be of vast curiosity to pharmacologists and toxicologists.

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1989). Only patients with type 2 disease respond to phenobarbital administration, their serum bilirubin levels being reduced by approximately 20%-30% as a result (RoY CHOWDHURY et al. 1989; SINAASAPPEL and JANSEN 1991). Recently, analysis of bile aspirates has proved to be a more definitive method of diagnosing the disease type (SINAASAPPEL and JANSEN et al. 1992; CLARKE and BURCHELL, in preparation). The molecular basis of these syndromes has recently been characterised by catalytic, immunochemical and molecular genetic analysis.

FEBS Lett 243:119-122 Fournel-Gigleux S, Sutherland L, Sabolovic N, Burchell B, Siest G (1990) Stable expression of two human UDP-glucuronosyltransferase cDNAs in V79 cell cultures. Mol Pharmacol 39: 177 -183 Frances B, Gout R, Campistron G, Panconi E, Cros J (1990) Morphine-6-glucuronide is more mu-selective and potent in analgesis tests than morphine. Prog Clin BioI Res 328:477-480 Franson KL, Burchell B, Mathis GA (1990) 17p-Hydroxysteroid UDP-glucuronosyltransferase is expressed in bile ductular epithelial cells under physiological conditions.

1993). bEBNER and BURCHELL (1993). cEBNER et aI. (1993). d BURCHELL et al. (unpublished). e The major drug substrate which is glucuronidated at a ten fold greater rate than the other compounds in each column. 1. CLARKE and B. BURCHELL 450 monooxygenase gene family, which has over 30 members (GONZALEZ 1992). IV. Structure and Mapping of Uridine Diphosphate Glucuronosyltransferase Gene Loci The four human UDPGT isoforms that belong to the UGTI family share identical C-terminal ends (Table 2 and Sect.

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