Conjugation—Deconjugation Reactions in Drug Metabolism and Toxicity

1. Front Matter

   Pages I-XXIV

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2. Transferases and Hydrolases Involved in Phase II Conjugation—Deconjugation Reactions, Genetic Polymorphism and Regulation of Expression

   1. Front Matter

      Pages 1-1

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   2. The Uridine Diphosphate Glucuronosyltransferase Multigene Family: Function and Regulation

      • D. J. Clarke, B. Burchell

      Pages 3-43

   3. Sulfotransferase Enzymes

      • R. Weinshilboum, D. Otterness

      Pages 45-78

   4. Regulation of Expression of Rat Liver Glutathione S-Transferases: Xenobiotic and Antioxidant Induction of the Ya Subunit Gene

      • T. H. Rushmore, C. B. Pickett, A. Y. H. Lu

      Pages 79-107

   5. Human N-Acetyltransferases

      • K. P. Vatsis, W. W. Weber

      Pages 109-130

   6. Genetic Regulation of the Subcellular Localization and Expression of Glucuronidase

      • R. T. Swank, E. K. Novak, L. Zhen

      Pages 131-160

   7. Microsomal Amidases and Carboxylesterases

      • C. Y. Wang

      Pages 161-187

   8. O-, N- and S-Methyltransferases

      • C. R. Creveling, D. R. Thakker

      Pages 189-216

3. Regulation of Phase II Conjugation: Deconjugation Reactions in Intact Cells and Tissues

   1. Front Matter

      Pages 217-217

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   2. Cofactor Supply as a Rate-Limiting Determinant of Hepatic Conjugation Reactions

      • L. A. Reinke, F. C. Kauffmann, R. G. Thurman

      Pages 219-244

   3. Regulation of Drug Conjugate Production by Futile Cycling in Intact Cells

      • F. C. Kauffman

      Pages 245-255

   4. Pharmacokinetic Modeling of Drug Conjugates

      • K. S. Pang, M. Chiba

      Pages 257-309

   5. Regulation of Drug Conjugate Processing by Hepatocellular Transport Systems

      • M. Vore

      Pages 311-338

4. Pharmacology and Toxicology of Drug Conjugates

   1. Front Matter

      Pages 339-339

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   2. Biologically Active Conjugates of Drugs and Toxic Chemicals

      • F. C. Kauffman, J. Zaleski, R. G. Thurman, G. Y. Kwei

      Pages 341-366

   3. Acyl Glucuronides as Chemically Reactive Intermediates

      • C. Fenselau

      Pages 367-389

   4. Roles of Uridine Diphosphate Glucuronosyltransferases in Chemical Carcinogenesis

      • K. W. Bock, W. Lilienblum

      Pages 391-428

   5. Sulfonation in Chemical Carcinogenesis

      • J. A. Miller, Y.-J. Surh

      Pages 429-457

   6. Glutathione Conjugate-Mediated Toxicities

      • T. J. Monks, S. S. Lau

      Pages 459-509

Advances in molecular biology describing important enzyme systems involved in drug conjugation and deconjugation reactions and recent work indicating the importance of drug and xenobiotic conjugates as transport forms of biologically active compounds are reviewed comprehensively. Part One describes molecular events associated with the expression and regulation of transferases and hydrolases involved in Phase II drug conjugation and deconjugation. Part Two deals with the regulation of Phase II conjugation, and Part Three reviews critically the importance of drug conjugates in pharmacology and toxicology. This volume is an up-to-date source of information on this topic and will be of broad interest to pharmacologists and toxicologists.

• Drug conjugates
• Konjugation
• Stoffwechsel
• Transferasen
• acyl-linked conjugates
• conjugate
• enzymes
• hydrolases
• metabolism
• regulation
• transferases
• transport

• Laboratory for Cellular and Biochemical Toxicology College of Pharmacy, Rutgers University, Piscataway, USA

  Frederick C. Kauffman

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