Enzymology in Drug Discovery

Inbunden, Engelska, 2027

2 839 kr

Kommande

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

Produktinformation

Utgivningsdatum2027-04-15
Mått152 x 229 x undefined mm
FormatInbunden
SpråkEngelska
SerieMethods in Enzymology
Antal sidor258
FörlagElsevier Science
MedarbetareRobert Copeland
ISBN9780443521621

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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.

1. Molecules of Life: The Critical Role of Enzymes in Health and DiseaseRachel Grimley2. Inhibition Modalities for Therapeutic Enzyme InhibitorsShane M. Buker3. Assay Design for Enzyme Targets in Drug Discovery: From Hit Identification to Lead OptimizationCharlene Bashore4. Covalent Hit Discovery and Characterization by Label-Free ApproachesBharath Srinivasan5. Slow and Tight-Binding Enzyme InhibitionPeter Tonge6. Structure-based drug discovery of enzyme-inhibitor complexes using protein X-ray crystallographyMargarita Tararina, Nicolas Szapiel, Max Ruzanov and Kevin Kish7. High-Throughput Evaluation of Enzyme Inhibition DynamicsAmaury Fernandez8. Protease inhibitors as therapeuticsTom Meek9. Experimental Methods for Detecting Methyltransferase Activity and Characterization of InhibitorsAravind Basavapathruni and Zachary Gurard-Levin10. Experimental Approaches to Histone Demethylase Biology: Purification, Detection and Functional ReadoutsJohnathan Whetstine11. DNA and RNA helicase inhibitors as therapeuticsJennifer Castro12. Inhibitors of nucleic acid processing as therapeuticsIsrael Canadas, Yaiza Jimenez and Takahiko Murayama13. Mechanistic Characterization of Heterbifunctional Modalities Using Biochemical MethodsArgyrides Argyrou14. Proximity Detection Assays for Identifying and Characterizing Molecular Glues of Target Proteins and E3 LigasesTim Wigle15. Structural Biology of the Axon Degeneration Executioner SARM1: Insights into Regulation, Enzymology and InhibitionRobert Hughes16. Kinesin motor protein inhibitors as therapeuticsMaureen Lynes and Brian Andrew Sparling17. Beyond PARP1: Enzymology, Biology and Therapeutic Targeting of PARPs 4–16Tim J. Mitchison18. Drug Metabolism and Disposition: The Role of Metabolic EnzymesBenjamin Barlock and Rohitash Jamwal19. Utilization of In Vitro Assays for CYP Inhibition and Induction to Enable Clinical Drug-Drug Interaction Risk AssessmentNigel J. Waters and Panos Hatsis20. Methods to Create Therapeutics by Replacing or Repairing Defective EnzymesCharles Albright