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Enzyme technologies : pluripotent players in discovering therapeutic agents / / edited by Hsiu-Chiung Yang, Wu-Kuang Yeh, James R. McCarthy
| Enzyme technologies : pluripotent players in discovering therapeutic agents / / edited by Hsiu-Chiung Yang, Wu-Kuang Yeh, James R. McCarthy |
| Pubbl/distr/stampa | Hoboken, New Jersey : , : Wiley, , 2014 |
| Descrizione fisica | 1 online resource (366 p.) |
| Disciplina | 615.3 |
| Altri autori (Persone) |
YangHsiu-Chiung
YehWu-Kuang <1942-> McCarthyJ. R |
| Collana | Chemical Biology of Enzymes for Biotechnology and Pharmaceutical Applications |
| Soggetto topico |
Enzyme inhibitors
Enzymes - Pharmacokinetics Drugs - Design |
| ISBN |
1-118-73990-6
1-118-73989-2 |
| Classificazione | SCI010000 |
| Formato | Materiale a stampa  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
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 |
| Record Nr. | UNINA-9910138987203321 |
| Hoboken, New Jersey : , : Wiley, , 2014 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Enzyme technologies : pluripotent players in discovering therapeutic agents / / edited by Hsiu-Chiung Yang, Wu-Kuang Yeh, James R. McCarthy
| Enzyme technologies : pluripotent players in discovering therapeutic agents / / edited by Hsiu-Chiung Yang, Wu-Kuang Yeh, James R. McCarthy |
| Pubbl/distr/stampa | Hoboken, New Jersey : , : Wiley, , 2014 |
| Descrizione fisica | 1 online resource (366 p.) |
| Disciplina | 615.3 |
| Altri autori (Persone) |
YangHsiu-Chiung
YehWu-Kuang <1942-> McCarthyJ. R |
| Collana | Chemical Biology of Enzymes for Biotechnology and Pharmaceutical Applications |
| Soggetto topico |
Enzyme inhibitors
Enzymes - Pharmacokinetics Drugs - Design |
| ISBN |
1-118-73990-6
1-118-73989-2 |
| Classificazione | SCI010000 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
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 |
| Record Nr. | UNINA-9910814431703321 |
| Hoboken, New Jersey : , : Wiley, , 2014 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||