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Full Description
In contrast to previous texts focusing on either computational, structural or synthetic methods, this one-of-a-kind guide integrates all three skill sets for a complete picture of contemporary structure-based design. As a result, this practical book demonstrates how to develop a high-affinity ligand with drug-like properties for any given drug target for which a high-resolution structure exists. The authors, both of whom have successfully designed drug-like molecules that were later developed into marketed drugs, use numerous examples of recently developed drugs to present best practice in structure-based drug design with the novice in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design.
Contents
From Traditional Medicine to Modern Drugs: Historical Perspective of Structure-Based Drug Design CONCEPTS, TOOLS, LIGANDS AND SCAFFOLDS FOR STRUCTURE-BASED DESIGN OF INHIBITORS Design of Inhibitors of Aspartic Acid Proteases Design of Serine Protease Inhibitors Design of Proteosome Inhibitors Design of Cysteine Protease Inhibitors Design of Metalloprotease Inhibitors Structure-Based Design of Protein Kinase Inhibitors Protein X-Ray Crystallography in Structure-Based Drug Design Structure-Based Design Strategies for Targeting G-Protein Coupled Receptors (GPCRs) STRUCTURE-BASED DESIGN OF FDA-APPROVED INHIBITOR DRUG AND DRUGS UNDERGOING CLINICAL DEVELOPMENT Angiotensin-Converting Enzyme Inhibitors for the Treatment of Hypertension: Design and Discovery of Captopril HIV-1 Protease Inhibitors for the Treatment of HIV Infection and AIDS: Design of Saquinavir, and Darunavir Protein Kinase Inhibitor Drugs for Targeted Cancer Therapy: Design and Discovery of Imatinib, Nilotinib and Dasatinib NS3/4A Serine Protease Inhibitors for the Treatment of HCV: Design and Discovery of Boceprevir and Telaprevir Proteasome Inhibitors for the Treatment of Relapsed Multiple Myeloma: Design and Discovery of Bortezomib and Carfilzomib Direct Thrombin Inhibitors as Anticoagulant Drugs Development of Direct Thrombin Inhibitor, Dabigatran Etexilate, as an Anticoagulant Drug Non-Nucleoside HIV Reverse Transcriptase Inhibitors for the Treatment of HIV/AIDS: Design and Development of Etravirine and Rilpivirine Renin Inhibitor for the Treatment of Hypertension: Design and Discovery of Aliskiren Neuraminidase Inhibitors for the Treatment of Influenza: Design and Discovery of Zanamivir and Oseltamivir Carbonic Anhydrase Inhibitors for the Treatment of Glaucoma: Design and Discovery of Dorzolamide Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease: Preclinical and Clinical Inhibitors Index
