Design of peptide and peptidomimetic ligands with novel pharmacological activity profiles

Victor J. Hruby, Minying Cai

Research output: Contribution to journalReview articlepeer-review

43 Scopus citations


Peptide hormones and neurotransmitters are of central importance in most aspects of intercellular communication and are involved in virtually all degenerative diseases. In this review, we discuss physicochemical approaches to the design of novel peptide and peptidomimetic agonists, antagonists, inverse agonists, and related compounds that have unique biological activity profiles, reduced toxic side effects, and, if desired, the ability to cross the blood-brain barrier. Designing ligands for specific biological and medical needs is emphasized, as is the close collaboration of chemists and biologists to maximize the chances for success. Special emphasis is placed on the use of conformational (φ-ψ space) and topographical (χ space) considerations in design.

Original languageEnglish (US)
Pages (from-to)557-580
Number of pages24
JournalAnnual review of pharmacology and toxicology
StatePublished - Jan 2013


  • blood-brain barrier
  • conformation and biological activity
  • peptide hormones
  • peptide neurotransmitters
  • peptide pharmacophores
  • peptide stability
  • topographical structures

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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