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In this ground-breaking practical reference, the family of aspartic acid proteases is described from a drug developer's perspective. The first part provides a general introduction to the family of aspartic acid proteases, their physiological functions, molecular structure and inhibition. Parts two to five present various case studies of successful protease inhibitor drug design and development, as well as current and potential uses of such inhibitors in pharmaceutical medicine, covering the major therapeutic targets HIV-1 protease, renin, beta-secretase, gamma-secretase,plasmepsins and fungal proteases.A ready reference aimed primarily at professionals in the pharmaceutical industry, as well as for anyone studying proteases and their function.
List of contents
OVERVIEW OF ASPARTIC ACID PROTEASESIntroduction to the Aspartic Proteases FamilyAspartic Acid Proteases, Structure, Function and InhibitionHuman Aspartic ProteinasesStructure-based Drug Design Strategies for the Inhibition of Aspartic Acid ProteasesHIV-1 PROTEASE FOR THE TREATMENT OF HIV/AIDSHIV-1 Protease: Role in Viral Replication, Protein-Ligand X-ray Crystal Structures and Inhibitor DesignFirst generation FDA Approved HIV protease inhibitorsSecond-Generation Approved HIV Protease Inhibitors for Treatment of HIV/AIDSDesign, Conception and Clinical Development of Darunavir, a HIV-1 Protease Inhibitor to Combat Drug ResistanceDevelopment of Protease Inhibitors and Challenges to Drug-Resistance of HIV-1RENIN FOR TREATMENT OF HYPERTENSIONDiscovery and Development of Aliskiren, the First-in-Class Direct Renin Inhibitor for the Treatment of HypertensionEvolution of Diverse Classes of Renin Inhibitors Through the YearsGAMMA-SECRETASE FOR TREATMENT OF ALZHEIMER'S DISEASEChemistry and Biology of gamma-Secretase as a Possible Target for Alzheimer's DiseaseGamma-Secretase Inhibition: An overview of Development of Inhibitors for Alzheimer's DiseaseBETA-SECRETASE FOR TREATMENT OF ALZHEIMER'S DISEASEBACE - An (Almost) Perfect Target for Staving Off Alzheimer's DiseaseDiscovery of Memapsin 2 (BACE1), Design of Inhibitors and Drug-design ToolsPeptidomimetic BACE1 Inhibitors for Treatment of Alzheimer's Disease: Design and EvolutionNon-Peptide BACE1 Inhibitors: Design and SynthesisPLASMEPSINS AND OTHER ASPARTIC PROTEASES AS DRUG TARGETSThe Plasmepsin Family as Antimalarial Drug TargetsDesign and Synthesis of Plasmepsin Inhibitors for Treatment of MalariaFungal aspartic proteases as possible therapeutic targets
About the author
Hugo Kubinyi gehört seit 1985 der BASF AG an, wo Kombinatorische Chemie, Molecular Modelling und Wirkstoffdesign zu seinen Tätigkeitsfeldern zählten. Sein Spezialgebiet sind Struktur-Wirkungs-Beziehungen und QSAR-Methoden.
Summary
In this ground-breaking practical reference, the family of aspartic acid proteases is described from a drug developer's perspective. The first part provides a general introduction to the family of aspartic acid proteases, their physiological functions, molecular structure and inhibition. Parts two to five present various case studies of successful protease inhibitor drug design and development, as well as current and potential uses of such inhibitors in pharmaceutical medicine, covering the major therapeutic targets HIV-1 protease, renin, beta-secretase, gamma-secretase,plasmepsins and fungal proteases.
A ready reference aimed primarily at professionals in the pharmaceutical industry, as well as for anyone studying proteases and their function.
Report
"Overall, this book comprises an excellent themes and publications based on aspartic protease research, and I strongly recommend this book for novices, as well as experienced researchers in this area." (ChemMedChem, 2011)
