Aspartic Acid Proteases as Therapeutic Targets

Description

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.Content: Chapter 1 Introduction to the Aspartic Proteinase Family (pages 1–21): Ben M. DunnChapter 2 Aspartic Proteases: Structure, Function, and Inhibition (pages 23–41): Jordan TangChapter 3 Human Aspartic Proteinases (pages 43–70): John Kay and Daniel BurChapter 4 Structure?Based Drug Design Strategies for Inhibition of Aspartic Proteinases (pages 71–105): Jon B. CooperChapter 5 HIV?1 Protease: Role in Viral Replication, Protein–Ligand X?Ray Crystal Structures and Inhibitor Design (pages 107–137): Irene T. Weber and Yuan?Fang WangChapter 6 First?Generation HIV?1 Protease Inhibitors for the Treatment of HIV/AIDS (pages 139–168): Scott C. VirgilChapter 7 Second?Generation Approved HIV Protease Inhibitors for the Treatment of HIV/AIDS (pages 169–204): Prof. Dr. Arun K. Ghosh and Bruno D. ChapsalChapter 8 Darunavir, a New PI with Dual Mechanism: From a Novel Drug Design Concept to New Hope against Drug?Resistant HIV (pages 205–243): Prof. Dr. Arun K. Ghosh, Bruno D. Chapsal and Hiroaki MitsuyaChapter 9 Development of HIV?1 Protease Inhibitors, Antiretroviral Resistance, and Current Challenges of HIV/AIDS Management (pages 245–262): Hiroaki Mitsuya and Prof. Dr. Arun K. GhoshChapter 10 Discovery and Development of Aliskiren, the First?in?Class Direct Renin Inhibitor for the Treatment of Hypertension (pages 263–296): Jeanette M. Wood and Jurgen MaibaumChapter 11 Evolution of Diverse Classes of Renin Inhibitors through the Years (pages 297–324): Colin M. Tice and Suresh B. SinghChapter 12 ??Secretase: An Unusual Enzyme with Many Possible Disease Targets, Including Alzheimer's Disease (pages 325–351): Johan Lundkvist and Urban LendahlChapter 13 ??Secretase Inhibition: An Overview of Development of Inhibitors for the Treatment of Alzheimer's Disease (pages 353–390): Christopher L. Hamblett, Sanjiv Shah, Richard Heidebrecht and Benito MunozChapter 14 BACE: A (Almost) Perfect Target for Staving off Alzheimer's Disease (pages 391–412): Sukanto SinhaChapter 15 The Discovery of ??Secretase and Development toward a Clinical Inhibitor for AD: An Exciting Academic Collaboration (pages 413–440): Jordan Tang, Lin Hong and Prof. Dr. Arun K. GhoshChapter 16 Peptidomimetic BACE1 Inhibitors for Treatment of Alzheimer's Disease: Design and Evolution (pages 441–479): Ulrich Iserloh and Jared N. CummingChapter 17 Nonpeptide BACE1 Inhibitors: Design and Synthesis (pages 481–509): Derek C. Cole and Matthew G. BursavichChapter 18 The Plasmepsin Family as Antimalarial Drug Targets (pages 511–547): Adam J. Ruben, Yoshiaki Kiso and Ernesto FreireChapter 19 Plasmepsins Inhibitors as Potential Drugs against Malaria: Starving the Parasite (pages 549–571): Sandra GemmaChapter 20 Fungal Aspartic Proteases as Possible Therapeutic Targets (pages 573–606): Michel Monod, Peter Staib, Utz Reichard and Olivier Jousson