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Structure-based Design of Drugs and Other Bioactive Molecules: Tools and Strategies / Edition 1

Structure-based Design of Drugs and Other Bioactive Molecules: Tools and Strategies / Edition 1

by Arun K. Ghosh, Sandra Gemma
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Product Details

ISBN-13: 9783527333653
Publisher: Wiley
Publication date: 08/11/2014
Pages: 474
Product dimensions: 6.90(w) x 9.80(h) x 1.20(d)

About the Author

Arun K. Ghosh received his BS and MS in Chemistry at the University of Calcutta and the Indian Institute of Technology, Kanpur, respectively. He obtained his Ph.D. (1985) at the University of Pittsburgh. He then pursued post-doctoral research with Professor E. J. Corey at Harvard University (1985-1988). He was a research fellow at Merck Research Laboratories prior to joining the University of Illinois, Chicago as an assistant Professor in 1994. In 2005, he moved to Purdue University where he is currently the Ian P. Rothwell Distinguished Professor of Chemistry and Medicinal Chemistry. His notable honors include: ACS Medicinal Chemistry Hall of Fame, National Institutes of Health MERIT Award, CRSI medal from the Chemical Research Society of India, IUPAC Richter Award, ACS Arthur C. Cope Scholar Award, ACS Robert Scarborough Medicinal Chemistry Award, American Association for the Advancement of Science, University of Illinois University Scholar, National Merit Scholar of India. He has published over 260 research papers, edited a book on aspartic acid proteases and holds numerous patents. His research interests include diverse areas of organic, bioorganic, and medicinal chemistry with particular emphasis on organic synthesis and protein-structure-based design of biomolecules.

Sandra Gemma graduated cum Laude in Medicinal Chemistry at the School of Pharmacy of the University of Siena (1998) where she also received her Ph.D. degree (2003). She was a post-doctoral fellow at the Department of Chemistry of the University of Illinois at Chicago in Professor Ghosh's laboratory (2004 to 2005). She then moved back to the University of Siena where she was appointed as an Assistant Professor at the Department of Biotechnology, Chemistry and Pharmacy (2006-present). She also visited the Department of Chemistry at Purdue University as a research assistant in the Ghosh group (2008 and 2012). In 2014, Dr. Gemma received the National scientific qualification for the role of Associate Professor. Her research activity is currently focused on the structure- and ligand-based design of therapeutic agents, anti-HIV and anti-Alzheimer therapeutics, ligands for GPCRs and ion channels, and antimalarial drugs. She has authored more than 65 papers and patents in these fields.

Table of Contents

From Traditional Medicine to Modern Drugs: Historical Perspective of Structure-Based Drug Design

Design of Inhibitors of Aspartic Acid Proteases
Design of Serine Protease Inhibitors
Design of Proteosome Inhibitors
Design of Cysteine Protease Inhibitors
Design of Metalloprotease Inhibitors
Structure-Based Design of Protein Kinase Inhibitors
Protein X-Ray Crystallography in Structure-Based Drug Design
Structure-Based Design Strategies for Targeting G-Protein Coupled Receptors (GPCRs)

Angiotensin-Converting Enzyme Inhibitors for the Treatment of Hypertension: Design and Discovery of Captopril
HIV-1 Protease Inhibitors for the Treatment of HIV Infection and AIDS: Design of Saquinavir, and Darunavir
Protein Kinase Inhibitor Drugs for Targeted Cancer Therapy: Design and Discovery of Imatinib, Nilotinib and Dasatinib
NS3/4A Serine Protease Inhibitors for the Treatment of HCV: Design and Discovery of Boceprevir and Telaprevir
Proteasome Inhibitors for the Treatment of Relapsed Multiple Myeloma: Design and Discovery of Bortezomib and Carfilzomib
Direct Thrombin Inhibitors as Anticoagulant Drugs
Development of Direct Thrombin Inhibitor, Dabigatran Etexilate, as an Anticoagulant Drug
Non-Nucleoside HIV Reverse Transcriptase Inhibitors for the Treatment of HIV/AIDS: Design and Development of Etravirine and Rilpivirine
Renin Inhibitor for the Treatment of Hypertension: Design and Discovery of Aliskiren
Neuraminidase Inhibitors for the Treatment of Influenza: Design and Discovery of Zanamivir and Oseltamivir
Carbonic Anhydrase Inhibitors for the Treatment of Glaucoma: Design and Discovery of Dorzolamide
Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease: Preclinical and Clinical Inhibitors


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