Enzyme technologies : pluripotent players in discovering therapeutic agents /

"This book highlights how, what, and where enzymes have become critical in pharmaceutical and biotechnology research. It provides in-depth reviews of recent developments in select topics on biosynthesis, biocatalysis, and chemical biology of enzymes. Broad coverage of enzymatic assays includes...

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Detalles Bibliográficos
Clasificación:Libro Electrónico
Autor principal: McCarthy, J. R.
Otros Autores: Yang, Hsiu-Chiung, Yeh, Wu-Kuang, 1942-
Formato: Electrónico eBook
Idioma:Inglés
Publicado: Hoboken, New Jersey : Wiley-Interscience, [2014]
Colección:Chemical biology of enzymes for biotechnology and pharmaceutical applications ; v. 2.
Temas:
Enzyme inhibitors.
Enzymes > Pharmacokinetics.
Drugs > Design.
Enzyme Inhibitors
Enzymes > pharmacokinetics
Drug Design
Antienzymes.
Enzymes > Pharmacocinétique.
Médicaments > Conception.
SCIENCE > Biotechnology.
Drugs > Design
Enzyme inhibitors
Acceso en línea:Texto completo
Tabla de Contenidos:
  • Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agents; Copyright; Contents; Contributors; Preface; PART A ENZYMES
  • ESSENTIAL WORKHORSES IN PHARMACEUTICAL RESEARCH; 1 ASSAY TECHNOLOGIES FOR PROTEASES; I. INTRODUCTION; II. PROTEASE ACTIVITY ASSAYS; III. ASSAYS FOR SOME CLINICALLY SIGNIFICANT PROTEASES; IV. COMPUTATIONAL APPROACHES FOR PROTEASE IDENTIFICATION AND CHARACTERIZATION; 2 DISCOVERY AND DEVELOPMENT OF ISOZYME-SELECTIVE INHIBITORS INVOLVED IN LIPID METABOLISM; I. INTRODUCTION; II. DIACYLGLYCEROL ACYLTRANSFERASE (DGAT)
  • III. ACYL-COA: CHOLESTEROL ACYLTRANSFERASE (ACAT)IV. CONCLUSIONS AND FUTURE PERSPECTIVES; References; 3 COVALENT ENZYME INHIBITION IN DRUG DISCOVERY AND DEVELOPMENT; I. INTRODUCTION; II. MECHANISM OF INHIBITION: MECHANISTIC TYPES BY PRINCIPLE OF INHIBITION; III. KINETICS: CONCEPTUAL AND EXPERIMENTAL CONSIDERATIONS; IV. SPECIFIC EXAMPLES OF COVALENT INHIBITORS; V. COVALENT ADDUCT WITH COFACTOR ALONE; VI. FULLY IRREVERSIBLE NONCOVALENT INHIBITION; VII. REVERSIBILITY AND DRUG RESISTANCE; VIII. PSEUDO-IRREVERSIBLE INHIBITION; IX. IRREVERSIBLE INHIBITORS AS TOOLS: ACTIVITY-BASED PROTEOMICS (ABP)
  • X. MBI OF CYPsXI. THE PROBLEM OF HAPTENATION; XII. CONCLUSION; References; 4 PRECLINOMICS: ENZYME ASSAYS AND RODENT MODELS FOR METABOLIC DISEASES; I. INTRODUCTION; II. EVOLVING ENZYME ASSAYS; III. DEVELOPING NEW RAT MODEL FOR METABOLIC DISEASES; IV. ZDSD RAT: EVALUATING CURRENT DRUGS; V. EXISTING RODENT MODELS: ESTABLISHING POSITIVE CONTROLS; VI. EXISTING RODENT MODELS AND ONE CANCER PATIENT: TESTING NUTRITIONAL SUPPLEMENT (ALKA VITA); VII. CONCLUDING REMARKS; References; PART B ENZYMES
  • INDISPENSABLE TOOLS FOR IMPROVING DRUGGABILITY; 5 ENZYMES AND TARGETED ACTIVATION OF PRODRUGS
  • I. INTRODUCTIONII. ENDOGENOUS ENZYMES; III. NONENDOGENOUS ENZYMES; IV. CONCLUDING REMARKS; References; 6 EVOLUTION OF AN ORALLY ACTIVE PRODRUG OF GEMCITABINE; I. INTRODUCTION; II. PREPARATION OF GEMCITABINE PRODRUGS; III. ADVANTAGE OF CYCLOPROPYL ESTER PRODRUGS; IV. ISSUES WITH CYCLOPROPYL ESTERS OF GEMCITABINE; V. ALTERNATIVE PRODRUGS OF GEMCITABINE; VI. CO-CRYSTALS OF VALPROATE AMIDE OF GEMCITABINE; VII. STABILITY OF VALPROATE AMIDE PRODRUG; VIII. BIOAVAILABILITY OF AMIDE PRODRUG; IX. ANTITUMOR ACTIVITY OF PRODRUG; X. SUMMARY; References
  • 7 ENZYMATICALLY ACTIVATED PHOSPHATE AND PHOSPHONATE PRODRUGSI. INTRODUCTION; II. PHOSPHATE GROUP USED FOR SOLUBILITY ENHANCEMENT; III. PHOSPHATE AND PHOSPHONATE PRODRUGS; IV. CONCLUSIONS; References; PART C ENZYMES
  • POWERFUL WEAPONS FOR CORRECTING NATURE ' S ERRORS; 8 TREATMENT OPTIONS FOR MUCOPOLYSACCHARIDOSIS TYPE II (HUNTER'S SYNDROME); I. INTRODUCTION; II. HISTORY; III. BIOCHEMISTRY; IV. GENETICS; V. CLINICAL MANIFESTATION; VI. MANAGEMENT AND TREATMENT; VII. FUTURE PERSPECTIVES; References; 9 ENZYME REPLACEMENT THERAPY FOR FABRY DISEASE; I. INTRODUCTION

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