LEADER 05902nam 2200769 450 001 9910138987203321 005 20230803220459.0 010 $a1-118-73990-6 010 $a1-118-73989-2 035 $a(CKB)2550000001166769 035 $a(EBL)1569027 035 $a(OCoLC)864747482 035 $a(SSID)ssj0001060918 035 $a(PQKBManifestationID)11587567 035 $a(PQKBTitleCode)TC0001060918 035 $a(PQKBWorkID)11097024 035 $a(PQKB)10243974 035 $a(PQKBManifestationID)16122021 035 $a(PQKB)23598912 035 $a(OCoLC)874967988 035 $a(MiAaPQ)EBC1569027 035 $a(DLC) 2013016032 035 $a(Au-PeEL)EBL1569027 035 $a(CaPaEBR)ebr10812057 035 $a(CaONFJC)MIL548147 035 $a(EXLCZ)992550000001166769 100 $a20131210d2014 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aEnzyme technologies $epluripotent players in discovering therapeutic agents /$fedited by Hsiu-Chiung Yang, Wu-Kuang Yeh, James R. McCarthy 210 1$aHoboken, New Jersey :$cWiley,$d2014. 210 4$dİ2014 215 $a1 online resource (366 p.) 225 1 $aChemical Biology of Enzymes for Biotechnology and Pharmaceutical Applications ;$vVolume II 300 $aDescription based upon print version of record. 311 $a0-470-28626-1 311 $a1-306-16896-1 320 $aIncludes bibliographical references and index. 327 $aEnzyme 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) 327 $aIII. 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) 327 $aX. 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 327 $aI. 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 327 $a7 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 327 $aII. THE STRUCTURE AND CATALYTIC MECHANISMS OF HUMAN ALPHA-GALACTOSIDASE A 330 $a"This book highlights how, what, and where enzymes have become critical in pharmaceutical and biotechnology research. It provides in-depth reviews of recent developments in select topics on biosynthesis, biocatalysis, and chemical biology of enzymes. Broad coverage of enzymatic assays includes emerging assay technologies for key enzyme classes in pharmaceutical research. In addition to new developments in proteomics, this book includes two emerging technologies in Life Sciences: metabolomics (including glycomics and lipidomics) and preclinomics. This volume reviews important progress on the chemical biology of enzymes in the post-genomic era"--$cProvided by publisher. 410 0$aChemical biology of enzymes for biotechnology and pharmaceutical applications ;$vv. 2. 606 $aEnzyme inhibitors 606 $aEnzymes$xPharmacokinetics 606 $aDrugs$xDesign 615 0$aEnzyme inhibitors. 615 0$aEnzymes$xPharmacokinetics. 615 0$aDrugs$xDesign. 676 $a615.3 686 $aSCI010000$2bisacsh 701 $aYang$b Hsiu-Chiung$0911816 701 $aYeh$b Wu-Kuang$f1942-$0911817 701 $aMcCarthy$b J. R$0911818 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910138987203321 996 $aEnzyme technologies$92041943 997 $aUNINA