Aspartic Acid Proteases as Therapeutic Targets

✍ Scribed by R. Mannhold, H. Kubinyi, G. Folkers(eds.)

• Year: 2010
• Tongue: English
• Leaves: 622
• Series: Methods and Principles in Medicinal Chemistry
• Category: Library

✦ Synopsis

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. Dunn
Chapter 2 Aspartic Proteases: Structure, Function, and Inhibition (pages 23–41): Jordan Tang
Chapter 3 Human Aspartic Proteinases (pages 43–70): John Kay and Daniel Bur
Chapter 4 Structure?Based Drug Design Strategies for Inhibition of Aspartic Proteinases (pages 71–105): Jon B. Cooper
Chapter 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 Wang
Chapter 6 First?Generation HIV?1 Protease Inhibitors for the Treatment of HIV/AIDS (pages 139–168): Scott C. Virgil
Chapter 7 Second?Generation Approved HIV Protease Inhibitors for the Treatment of HIV/AIDS (pages 169–204): Prof. Dr. Arun K. Ghosh and Bruno D. Chapsal
Chapter 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 Mitsuya
Chapter 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. Ghosh
Chapter 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 Maibaum
Chapter 11 Evolution of Diverse Classes of Renin Inhibitors through the Years (pages 297–324): Colin M. Tice and Suresh B. Singh
Chapter 12 ??Secretase: An Unusual Enzyme with Many Possible Disease Targets, Including Alzheimer's Disease (pages 325–351): Johan Lundkvist and Urban Lendahl
Chapter 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 Munoz
Chapter 14 BACE: A (Almost) Perfect Target for Staving off Alzheimer's Disease (pages 391–412): Sukanto Sinha
Chapter 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. Ghosh
Chapter 16 Peptidomimetic BACE1 Inhibitors for Treatment of Alzheimer's Disease: Design and Evolution (pages 441–479): Ulrich Iserloh and Jared N. Cumming
Chapter 17 Nonpeptide BACE1 Inhibitors: Design and Synthesis (pages 481–509): Derek C. Cole and Matthew G. Bursavich
Chapter 18 The Plasmepsin Family as Antimalarial Drug Targets (pages 511–547): Adam J. Ruben, Yoshiaki Kiso and Ernesto Freire
Chapter 19 Plasmepsins Inhibitors as Potential Drugs against Malaria: Starving the Parasite (pages 549–571): Sandra Gemma
Chapter 20 Fungal Aspartic Proteases as Possible Therapeutic Targets (pages 573–606): Michel Monod, Peter Staib, Utz Reichard and Olivier Jousson