Receptor-assisted combinatorial chemistry: Thermodynamics and kinetics in drug discovery

Jeremy D. Cheeseman, Andrew D. Corbett, James L. Gleason, Romas J. Kazlauskas

Research output: Contribution to journalReview articlepeer-review

69 Scopus citations

Abstract

Current drug discovery using combinatorial chemistry involves synthesis followed by screening, but emerging methods involve receptor-assistance to combine these steps. Adding stoichiometric amounts of receptor during library synthesis alters the kinetics or thermodynamics of the synthesis in a way that identifies the best-binding library members. Three main methods have emerged thus far in receptor-assisted combinatorial chemistry: dynamic combinatorial libraries, receptor-accelerated synthesis, and a new method, pseudo-dynamic libraries. Pseudo-dynamic libraries apply both thermodynamics and kinetics to amplify library members to easily observable levels, and attain selectivity heretofore unseen in receptor-assisted systems.

Original languageEnglish (US)
Pages (from-to)1708-1716
Number of pages9
JournalChemistry - A European Journal
Volume11
Issue number6
DOIs
StatePublished - Mar 4 2005

Keywords

  • Combinatorial chemistry
  • Drug design
  • Inhibitors
  • Receptors
  • Template synthesis

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