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Development of Enzyme Inhibitors as Drugs

Tham khảo tài liệu 'development of enzyme inhibitors as drugs', tài liệu phổ thông, sinh học phục vụ nhu cầu học tập, nghiên cứu và làm việc hiệu quả | 5 Development of Enzyme Inhibitors as Drugs H. John Smith and Claire Simons CONTENTS 5.1 Introduction 5.1.1 Basic Concepts 5.1.1.1 Substrate Agonist Accumulation or Preservation 5.1.1.2 Decrease in Metabolite Production 5.2 Rational Selection of Suitable Target Enzyme and Inhibitor 5.2.1 Target Enzyme 5.2.2 Types of Inhibitor for Selected Target Enzyme 5.2.2.1 Reversible Inhibitors 5.2.2.2 Irreversible Inhibitors 5.3 Selectivity and Toxicity 5.4 Rational Approach to the Design of Enzyme Inhibitors 5.4.1 Lead Inhibitor Discovery 5.4.1.1 Modification of the Lead 5.4.2 Design from a Knowledge of the Catalytic Mechanism 5.4.2.1 Examples 5.4.3 Molecular Modeling 5.4.3.1 Crystal Structure of Enzyme or Enzyme-Inhibitor Complex Available 5.4.3.2 Prediction of 3-D Structure of Enzyme by Other Means 5.5 Development of a Drug Candidate from the Bench to the Marketplace 5.5.1 Oral Absorption 5.5.2 Metabolism 5.5.2.1 Examples 5.5.3 Toxicity 5.5.3.1 Examples 5.5.4 Stereochemistry 5.5.4.1 Optical Stereoisomerism 5.5.5 Drug Resistance Further Reading 5.6 Enzyme Inhibitor Examples for the Treatment of Breast Cancer L.W. Lawrence Woo 5.6.1 Introduction 5.6.2 Endocrine Therapy 2005 by CRC Press 5.6.3 Aromatase 5.6.4 Inhibition of Aromatase as Endocrine Therapy 5.6.4.1 Nonsteroidal Aromatase Inhibitors NSAIs 5.6.4.2 Steroidal Aromatase Inhibitors 5.6.4.3 Computer-Aided Drug Design of Aromatase Inhibitors 5.6.5 Steroid Sulfatase 5.6.5.1 The Enzyme and Breast Cancer 5.6.6 Inhibition of Steroid Sulfatase as Endocrine Therapy 5.6.6.1 Steroidal STS Inhibitors 5.6.6.2 Nonsteroidal STS Inhibitors 5.6.6.3 Mechanism of Action for STS and STS Inhibitors 5.6.7 Future Directions Acknowledgment Further Reading 5.7 Enzyme Inhibitor Examples for the Treatment of Prostate Tumor Samer Haidar and Rolf W. Hartmann 5.7.1 5a-Reductase and Androgen-Dependent Diseases 5.7.2 Inhibitors of 5a-Reductase 5.7.3 Prostate Cancer and CYP 17 5.7.4 Inhibitors of CYP 17 Further Reading 5.8 Thrombin Inhibitor Examples