Table of contents

Part One: Overview of Aspartic Acid Proteases

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

Part Two: HIV-1 Protease as Target for the Treatment of HIV/AIDS

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

Part Three: Renin as Target for the Treatment of Hypertension

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 Jürgen Maibaum

Chapter 11
Evolution of Diverse Classes of Renin Inhibitors through the Years (pages 297–324)
Colin M. Tice and Suresh B. Singh

Part Four: γ-Secretase as Target for the Treatment of Alzheimer's Disease

Chapter 12
γ-Secretase: An Unusual Enzyme with Many Possible Disease Targets, Including Alzheimer's Disease (pages 325–351)
Johan Lundkvist and Urban Lendahl

Chapter 13
γ-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

Part Five: β-Secretase as Target for the Treatment of Alzheimer's Disease

Chapter 14
BACE: A (Almost) Perfect Target for Staving off Alzheimer's Disease (pages 391–412)
Sukanto Sinha

Chapter 15
The Discovery of β-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

Part Six: Plasmepsins and Other Aspartic Proteases as Drug Targets

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