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Aspartic Acid Proteases as Therapeutic Targets, Volume 45. Methods and
Principles in Medicinal Chemistry
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 sechs 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 academics and pharmaceutical industry, as well as for
anyone studying proteases and their function.
Contents:
OVERVIEW OF ASPARTIC ACID PROTEASES
Introduction to the Aspartic Proteases Family
Aspartic Acid Proteases, Structure, Function and Inhibition
Human Aspartic Proteinases
Structure–based Drug Design Strategies for the Inhibition of Aspartic Acid Proteases
HIV–1 PROTEASE FOR THE TREATMENT OF HIV/AIDS
HIV–1 Protease: Role in Viral Replication, Protein–Ligand X–ray Crystal Structures and Inhibitor Design
First generation FDA Approved HIV protease inhibitors
Second–Generation Approved HIV Protease Inhibitors for Treatment of HIV/AIDS
Design, Conception and Clinical Development of Darunavir, a HIV–1 Protease Inhibitor to Combat Drug
Resistance
Development of Protease Inhibitors and Challenges to Drug–Resistance of HIV–1
RENIN FOR TREATMENT OF HYPERTENSION
Discovery and Development of Aliskiren, the First–in–Class Direct Renin Inhibitor for the Treatment of
Hypertension
Evolution of Diverse Classes of Renin Inhibitors Through the Years
GAMMA–SECRETASE FOR TREATMENT OF ALZHEIMER'S DISEASE
Chemistry and Biology of gamma–Secretase as a Possible Target for Alzheimer's Disease
Gamma–Secretase Inhibition: An overview of Development of Inhibitors for Alzheimer's Disease
BETA–SECRETASE FOR TREATMENT OF ALZHEIMER'S DISEASE
BACE –
An (Almost) Perfect Target for Staving Off Alzheimer's Disease
Discovery of Memapsin 2 (BACE1), Design of Inhibitors and Drug–design Tools
Peptidomimetic BACE1 Inhibitors for Treatment of Alzheimer's Disease: Design and Evolution
Non–Peptide BACE1 Inhibitors: Design and Synthesis
PLASMEPSINS AND OTHER ASPARTIC PROTEASES AS DRUG TARGETS
The Plasmepsin Family as Antimalarial Drug Targets
Design and Synthesis of Plasmepsin Inhibitors for Treatment of Malaria
Fungal aspartic proteases as possible therapeutic targets
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Aspartic Acid Proteases as Therapeutic Targets, Volume 45. Methods and Principles
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