Fragment–based Approaches in Drug Discovery, Volume 34. Methods and Principles in Medicinal Chemistry

  • ID: 2183687
  • Book
  • 391 Pages
  • John Wiley and Sons Ltd
1 of 4
Based on recent successes in the modular design of pharmaceutically active ligands, the concept and technology of fragment–based design has quickly pervaded the research departments of pharma companies, large and small. Drug developers everywhere are currently struggling to keep ahead of the competition by applying these methods to speed up the drug discovery.

This first systematic summary of the impact of such approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice–oriented approach, this book by professionals for professionals is indispensable for drug developers in the pharma and biotech sector who need to keep abreast of the latest technologies and strategies in pharmaceutical ligand design. Clearly divided into sections on ligand design, spectroscopic techniques, and screening and drug discovery, the text is backed by numerous case studies.
Note: Product cover images may vary from those shown
2 of 4
PART 1: CONCEPT AND THEORY

The concept of fragment–based ligand design

Multivalency in Ligand Design

Entropic consequences of linking ligands

Location of Binding Sites on Proteins by the Multiple Solvent Crystal Structure Method

PART 2: FRAGMENT LIBRARY DESIGN AND COMPUTATIONAL APPROACHES

Cheminformatics approaches to fragment–based lead discovery

Structural fragments from marketed oral drugs

Fragment docking to proteins with the multi–copy simultaneous search (MCSS) methodology

PART 3: EXPERIMENTAL TECHNIQUES

NMR – guided fragment assembly

SAR by NMR: an analysis of ptency gains realized through fragment–linking and fragment–elaboration strategies for lead generation

Pyramid: an integrated platform for fragment–based drug discovery

Fragment–based lead discovery and optimization using X–ray crystallography

Synergistic use of protein crystallography and solution–phase NMR spectroscopy in structure–based drug design: strategies and tactics

Ligand SAR using electrospray ionization mass spectrometry

Tethering

PART 4: EMERGING TECHNOLOGIES

Click chemistry for drug discovery

Dynamic combinatorial diversity in drug discovery
Note: Product cover images may vary from those shown
3 of 4

Loading
LOADING...

4 of 4
Wolfgang Jahnke
Daniel A. Erlanson
Note: Product cover images may vary from those shown
5 of 4
Note: Product cover images may vary from those shown
Adroll
adroll