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Drug Discovery and Design - 1st Edition - ISBN: 9780120342563, 9780080493381

Drug Discovery and Design, Volume 56

1st Edition

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Serial Editors: Frederic Richards David Eisenberg Peter Kim
Serial Volume Editor: Edward Scolnick
eBook ISBN: 9780080493381
Imprint: Academic Press
Published Date: 9th April 2001
Page Count: 567
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Table of Contents

Preface. "Natural History" Clinical Trials: An Enduring Contribution to Modern Medical Practice, E.M. Scolnick, E.E. Slater, and G.W. Williams: Introduction. Role of the Pharmaceutical Industry in Clinical Trials. Use of "Natural History" RCTs to Validate the Cholesterol Hypothesis and Support Changes in the Management of Other Conditions. Development of a New Chemical Entity. "Natural History" RCTs: Some Considerations. Patient Safety. Clinical Trials and the Practice of Medicine in the Age of Genomics. Angiotensin-Converting Enzyme Inhibitors, J. Menard and A. Patchett: Introduction. Peptide Inhibitors. Captopril. Enalapril. Lisinopril. Fosinopril. Clinically Available ACE Inhibitors. Contribution of ACE Inhibitors to the Growth of Physiological and Pathophysiological Knowledge. Biological Advances in the Knowledge of ACE That Evolved in Parallel with the Drug Development Process. Clinical Development Process of ACE Inhibitors in Hypertension. Benefits of ACE Inhibition Beyond the Fall in Blood Pressure. ACE Inhibitors and Congestive Heart Failure. ACE Inhibitors and Myocardial Infarction. ACE Inhibitors, Coronary Heart Disease, and Atherosis. ACE Inhibitors and Prevention of Restenosis. ACE Inhibitors and Renal Insufficiency. The Fallacy of the Concepts of Normotension and Hypertension and the Cardiovascular Protective Effects of ACE Inhibitors. Surrogate End Points in Clinical Trials of ACE Inhibition: Are We Being Misled? Conclusion. HMG-CoA Reductase Inhibitors, R. Illingworth and J.A. Tolbert: Background and History. Effects of Lipoproteins. Mechanisms of the Cholesterol-Lowering Effects of Reductase Inhibitors. Combination Therapy. Safety and Tolerability. Outcome Studies. Mechanisms of the Reduction in Coronary Morbidity and Mortality. Safety of HMG-CoA Reductase Inhibitors in the Megatrials. Future Directions. Cyclooxygenase-2 Inhibitors, A.S. Nies: Introduction. Background. Assays for Cyclooxygenase-2 Selective Inhibitors. Selectivity of Cyclooxygenase Inhibitors. Enzymology/Medicinal Chemistry. Clinical Development of Cyclooxygenase-2 Inhibitors. Future Directions. Conclusions. 5α-Reductase Inhibitors, J.D. McConnell and E. Stoner: Introduction. Identification and Characterization of 5α-Reductase. Development of 5α-Reductase Inhibitors. Clinical Studies in Men with Androgenic Disorders. Clinical Studies in Women with Androgenic Disorders. Other 5α-Reductase Inhibitors. Conclusion. Peroxisome Proliferator-Activated Receptor (PPAR) γ Agonists for Diabetes, D.E. Moller and D.A. Greene: Introduction. Mechanism of Action of Peroxisome Proliferator-Activated Receptor (PPAR) γ Agonists. Clinical Experience with PPARγ Agonists. Conclusions and Future Directions. Discovery and Clinical Development of HIV-1 Protease Inhibitors, J. Huff and J. Kahn: Introduction. Selection and Validation of HIV-1 Protease as a Therapeutic Target. Development of HIV-1 Protease Inhibitors. Structure-Based Design. Inhibitor Identification through Broad-Based Screening. Mechanism-Based Strategy. Future Directions for Discovery. HIV-1 Protease Inhibitors: The Clinical Perspective. Clinical Development Milestones. Issues of Ongoing Concern for the Clinical Use of HIV-1 Protease Inhibitors. Rational Treatment Combinations That Include HIV-1 Protease Inhibitors. Future Considerations for HIV-1 Protease Inhibitors. Conclusions. Calcineurin Inhibitors and the Generalization of the Presenting Protein Strategy, K.W. Vogel, R. Briesewitz, T.J. Wandless, and G.R. Crabtree: Calcineurin, Calcineurin Inhibitors, and the Effects of Inhibition of Calcineurin. Inhibition by Immunophilin/Immunosuppressant Complexes: The Presenting Protein Strategy. Generalization of the Presenting Protein Strategy. Conclusions. Pure Selective Estrogen Receptor Modulators, New Molecules Having Absolute Cell Specificity Ranging from Pure Antiesotrogenic to Complete Estrogen-Like Activities, F. Labrie, C. Labrie, A. Bélanger, V. Giguere, J. Simard, Y. Mérand, S. Gauthier, V. Luu-The, B. Candas, C. Martel, and S. Luo: Introduction. Women's Health Needs. The Estrogen Receptors and Their Multiple Gene Activation Mechanisms. Classes of Antiestrogens. Properties of EM-652 (SCH 57068) and EM-800 (SCH 57050). Monoclonal Antibody Therapy, J.W. Park and J. Smolen: Introduction. General Aspects of Monoclonal Antibody Therapy. Monoclonal Antibody Therapy in Organ Transplantation. Monoclonal Antibody Therapy in Cardiac Disease. Monoclonal Antibody Therapy in Infectious Diseases. Monoclonal Antibody Therapy in Rheumatologic and Autoimmune Diseases. Monoclonal Antibody Therapy of Cancer. Conclusion. Glucan Synthase Inhibitors as Antifungal Agents, M.B. Kurtz and J.H. Rex: Introduction and Background. The Fungal Cell Wall Is An Attractive Target. Early Research on Cell-Wall Active Agents. The Pneumocandins: Mycology and Parasitology Collide. Development of Amino Compounds. Current Compounds in Clinical Development. Outlook. Chapter References. Author Index. Subject Index.


Strategies to reduce medical uncertainty and build evidence have become critical to the advancement of medical knowledge and modern medical practice. As new techniques and strategies have arisen, so has the need for a current reference work. Drug Discovery and Design examines the latest research in the development of these new strategies. Some of the topics covered include angiotensin converting enzyme inhibitors, HIV protease inhibitors, PPAR agonists for diabetes, and glucan synthase antifungal agents.


Biochemists, molecular biologists, pharmaceutical and biomedical researchers.


No. of pages:
© Academic Press 2001
9th April 2001
Academic Press
eBook ISBN:


"This volume will be of interest to medicinal chemists, particularly those involved in drug discovery programs. ...Perhaps among the most interesting lessons to be learned from this text is that we are asking a lot from the drug design and discovery process, and that we are very often able to deliver." @source:—-Richard A. Hudson, University of Toledo, in JOURNAL OF MEDICINAL CHEMISTRY (2001) @from:PRAISE FOR THE SERIES @qu:"The authority, originality, and editing of the reviews are first class." @source:—-NATURE @qu:"The Advances in Protein Chemistry series has been a major factor in the education of protein chemists." @source:—-JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Ratings and Reviews

About the Serial Editors

Frederic Richards

Affiliations and Expertise

Yale University, New Haven, Connecticut, U.S.A.

David Eisenberg

Affiliations and Expertise

University of California, Los Angeles, U.S.A.

Peter Kim

Affiliations and Expertise

Massachusetts Institute of Technology, Whitehead Institute for Biomedical Research, Howard Hughes Medical Institute Research Laboratories, Cambridge, U.S.A.

About the Serial Volume Editor

Edward Scolnick

Affiliations and Expertise

Merck and Co., Inc., West Point, Pennsylvania, U.S.A.