Enzymology in Drug Discovery

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· Methods in Enzymology Book 740 · Academic Press
Ebook
258
Pages
Eligible
This book will become available on December 8, 2026. You will not be charged until it is released.

About this ebook

This volume is focused on the application of enzymology to drug discovery, with the overarching objective of introducing the general audience to the important role that enzymology plays in modern, molecular targeted drug discovery. The volume opens with a chapter on the role of enzymes in normal human physiology and the causal role played by aberrant enzyme activity in various disease state. A second chapter provides a comprehensive review of inhibition modalities for therapeutic enzyme inhibitors. From there the volume is composed of chapters that cover two general categories of information: (1) methodologies for studying enzyme-ligand interactions and (2) case studies of molecular targeted drug discovery against specific enzyme targets. Chapters within the first category cover methods such as assay design, the role of structural biology in drug optimization, analysis of slow and tight binding inhibitors, enzyme-inhibitor complex dynamics, and covalent enzyme inactivators. The second category includes case studies of therapeutic inhibitors of various enzyme target classes: proteases, methyltransferases, histone demethylases, helicases, nucleic acid processing enzymes, kinesin motor proteins, and cytochrome P450s. Finally, a chapter is also devoted to therapeutic replacement or repair of defective enzymes. - Highlights key methodologies for the study of enzymes as therapeutic targets - Provides in-depth case studies of enzyme-targeted therapeutic agents - Introduces the reader to the dynamic and multidisciplinary approaches necessary in the search for new medicines
This volume is focused on the application of enzymology to drug discovery, with the overarching objective of introducing the general audience to the important role that enzymology plays in modern, molecular targeted drug discovery. The volume opens with a chapter on the role of enzymes in normal ...

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About the author

After completing studies for the A.B., A.M., and Ph.D. degrees in chemistry at Harvard University, David W. Christianson joined the faculty of the University of Pennsylvania, where he is currently the Roy and Diana Vagelos Professor in Chemistry and Chemical Biology. At Penn, Christianson’s research focuses on the structural and chemical biology of the zinc-dependent histone deacetylases as well as enzymes of terpene biosynthesis. His research accomplishments have been recognized by several awards, including the Pfizer Award in Enzyme Chemistry and the Repligen Award in Chemistry of Biological Processes from the American Chemical Society, a Guggenheim Fellowship, and the Elizabeth S. and Richard M. Cashin Fellowship from the Radcliffe Institute for Advanced Study at Harvard University. Christianson is also a dedicated classroom teacher, and his accomplishments in this regard have been recognized by the Lindback Award for Distinguished Teaching at Penn and a Rhodes Trust Inspirational Educator Award from Oxford University. Christianson has also held visiting professorships in the Department of Biochemistry at Cambridge University and the Department of Chemistry and Chemical Biology at Harvard University. Christianson has served with Prof. Anna Pyle as Co-Editor-in-Chief of Methods in Enzymology since 2015.

Dr. Karen N. Allen works at the Department of Chemistry of the Boston University, the Metcalf Center for Science and Engineering

Robert A. Copeland is a prominent biomedical sciences entrepreneur and executive, with a strong track record of starting, building and leading successful drug discovery organizations. He is widely recognized for his pioneering contributions to precision medicine, enzymology, and oncology drug discovery. Copeland has contributed to the discovery of 21 investigational new drugs that have transitioned to the clinic, five of which are FDA-approved medicines. He has contributed over 200 publications to the scientific literature, holds 14 issued U.S. patents and has authored seven highly acclaimed texts books in the areas of protein sciences, enzymology and drug discovery. He is currently Venture Partner at Altas Venture, an Advisor to Google Ventures, and Adjunct Professor at the Perelman School of Medicine, The University of Pennsylvania. Beyond his career, he is an avid cyclist, bass fisherman and a second-degree black belt in judo, a sport in which he continues to actively participate.

After completing studies for the A.B., A.M., and Ph.D. degrees in chemistry at Harvard University, David W. Christianson joined the faculty of the University of Pennsylvania, where he is currently the Roy and Diana Vagelos Professor in Chemistry and Chemical Biology. At Penn, Christianson’s resea...

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