Pseudodynamic combinatorial libraries: A receptor-assisted approach for drug discovery

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

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

Abstract

Enzyme protection: An irreversible solid-phase, aqueous peptide coupling resulted in the formation of a library of eight dipeptides, while an irreversible protease-catalyzed hydrolysis destroyed them. Those dipeptides that bound to carbonic anhydrase were protected from destructions. Six cycles of active ester addition produced only the best-binding dipeptide (> 100:1) in 29% yield.

Original languageEnglish (US)
Pages (from-to)2432-2436
Number of pages5
JournalAngewandte Chemie - International Edition
Volume43
Issue number18
DOIs
StatePublished - Apr 26 2004

Keywords

  • Combinatorial chemistry
  • Drug design
  • Enzyme inhibitors
  • Kinetics
  • Receptors

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