Exploring Ramachandran and Chi space: Conformationally constrained amino acids and peptides in the design of bioactive polypeptide ligands

S. M. Cowell, Y. S. Lee, J. P. Cain, V. J. Hruby

Research output: Contribution to journalReview article

119 Scopus citations

Abstract

Ligand binding and concomitant changes in receptor structure provide the means to target signal transduction pathways. With appropriate refinement of the ligand's interaction with the " receptor," one in theory could produce ligands that have greater therapeutic benefits. This review will discuss how, when these ligands are amino acids and peptides, the introduction of appropriate conformational constraints provides a powerful strategy for improved drug design. This review will discuss how various constraints on amino acids can provide a powerful tool for ligand design, determination of the three dimensional pharmacophore and new insights into receptor systems and information transduction. Through the use of constrained ligands, new information regarding their interaction with their " receptor" systems, and further refinement of the use of constraints, scientists can produce more beneficial drugs for mankind.

Original languageEnglish (US)
Pages (from-to)2785-2798
Number of pages14
JournalCurrent medicinal chemistry
Volume11
Issue number21
DOIs
StatePublished - Nov 2004

Keywords

  • Constrained amino acids
  • Constrained peptides
  • Drug design
  • Ligand-receptor interactions

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Exploring Ramachandran and Chi space: Conformationally constrained amino acids and peptides in the design of bioactive polypeptide ligands'. Together they form a unique fingerprint.

  • Cite this