fragment-based ligand discovery

Marcus Fischer, Roderick E. Hubbard

Research output: Contribution to journalLiterature reviewpeer-review

Abstract

Over the past five years, fragment-based ligand discovery has come of age. A number of compounds that evolved from fragments have entered the clinic, and the approach is increasingly accepted as an additional route to identifying new hit compounds in pharmaceutical discovery and inhibitor design. This review will summarize the current methods and ideas prevalent in the area. We will discuss the key concepts and advantages of fragment-based discovery, the approaches adopted in designing fragment libraries, the experimental methods that have been optimized for detecting fragment binding, and the strategies for evolving fragments to hit and lead compounds.

Original languageEnglish
Pages (from-to)22-30
Number of pages9
JournalMOLECULAR INTERVENTIONS
Volume9
Issue number1
DOIs
Publication statusPublished - 1 Feb 2009

Keywords

  • DRUG DISCOVERY
  • PROMISCUOUS INHIBITORS
  • KINASE INHIBITOR
  • BINDING-SITES
  • NMR
  • DESIGN
  • PROTEINS
  • AFFINITY
  • SAR
  • LINKING

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