Modern Approaches in Drug Discovery

Modern Approaches in Drug Discovery, Volume 611, the latest release in the Methods in Enzymology series, highlights new advances in the field, with this new volume presenting interesting chapters on topics such as Target Identification and Validation, Cell Painting/High Content Imaging, Target ID using chemical probes, Mining the microbiome for targets, Data driven approaches for diversity and drug-likeness, Affinity-based screening, Fragment screening (X-ray), Array-based approaches, Hit-to-lead: assessment and improvement of drug-like properties, Hit assessment and prioritization, Lead Optimization: fine tuning and risk mitigation, and more.

Autorentext
Dr. Charles Lesburg works at Merck Research Laboratories, Boston, MA, USA

Inhalt

1. Risk Management in Early Discovery Medicinal Chemistry
   Gurpreet Singh, Jayme L. Dahlin and Michael A. Walters
   2. Target Identification Using Chemical Probes
   Moses Moustakim, Suet Ling Felce, Nancy Zaarour, Gillian Farnie, Fiona E. McCann and Paul E. Brennan
   3. Mining the Microbiome for Drug Targets
   Qi Wang, Fangming Yang and Huijue Jia
   4. Screening Library Design
   Stephanie Kay Ashenden
   5. Design of a Fragment Screening Library
   Ashley Taylor, Bradley C. Doak and Martin J. Scanlon
   6. Genetically Encoded Cyclic Peptide Libraries: From Hit to Lead and Beyond
   Jacob Valentine and Ali Tavassoli
   7. A Guide to Run Affinity Screens Using Differential Scanning Fluorimetry and Surface Plasmon Resonance Assays
   Christian Bergsdorf and Kirk Wright
   8. Second-Harmonic Generation (SHG) for Conformational Measurements: Assay Development, Optimization, and Screening
   Tracy A. Young, Ben Moree, Margaret T. Butko, Bason Clancy, Mary Geck Do, Tarun Gheyi, John Strelow, Juan J. Carrillo and Joshua Salafsky
   9. An Array-Based Ligand Discovery Platform for Proteins With Short Half-Lives
   Becky S. Leifer, Shelby K. Doyle, André Richters, Helen L. Evans and Angela N. Koehler
   10. High Content, Phenotypic Assays and Screens for Compounds Modulating Cellular Processes in Primary Neurons
   Miklos Kepiro, Boglarka H. Varkuti and Ronald L. Davis
   11. Achieving a Good Crystal System for Crystallographic X-Ray Fragment Screening
   Patrick M. Collins, Alice Douangamath, Romain Talon, Alexandre Dias, Jose Brandao-Neto, Tobias Krojer and Frank von Delft
   12. Hit-to-Lead: Hit Validation and Assessment
   Kirk E. Hevener, JinHong Ren, Russell Pesavento, Kiira Ratia, Hyun Lee and Michael E. Johnson
   13. Knowledge-Based Approaches to Off-Target Screening
   Daniel R. McMasters