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Enzyme technologies : pluripotent players in doscovering therapeutic agents / ed. by Hsiu-Chiung Yang ...
Mitwirkende(r): Resource type: Ressourcentyp: Buch (Online)Buch (Online)Sprache: Englisch Reihen: Chemical biology of enzymes for biotechnology and pharmaceutical applications ; v.2 | Chemical Biology of Enzymes for Biotechnology and Pharmaceutical Applications SerVerlag: Hoboken : Wiley-Interscience, 2013Auflage: Online-AusgBeschreibung: Online-Ressource (1 online resource.)ISBN:- 9781306168960
- 0470286261
- 615.3
- QP601.5
- QP601.5 .Y33 2013
Inhalte:
Zusammenfassung: HSIU-CHIUNG YANG, PhD, is Research Advisor at Eli Lilly and Company. She is the author or coauthor of over forty publications and holder of two patents. WU-KUANG YEH, PhD, is Adjunct Professor at Indiana University Purdue University Indianapolis (IUPUI), and was Director of Research and Principal Investigator at PreClinOmics, Inc. The holder of six U.S. patents, Dr. Yeh is the author or coauthor of over 115 publications. JAMES R. McCARTHY, PhD, is Research Professor in the department of chemistry and chemical biology at Indiana University Purdue University Indianapolis (IUPUI), and was a Distinguished Research Fellow at Eli Lilly and Company. He is the author or coauthor of over 130 publications and holder of over sixty patents.Zusammenfassung: Intro -- 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 CYPs -- XI. 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. INTRODUCTION.PPN: PPN: 1657673421Package identifier: Produktsigel: ZDB-26-MYL | ZDB-30-PAD | ZDB-30-PQE
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
II. THE STRUCTURE AND CATALYTIC MECHANISMS OF HUMAN ALPHA-GALACTOSIDASE A
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