Rational design of novel neurotensin mimetics: Discovery of a pharmacologically unprecedented agent exhibiting concentration-dependent dual effects as antagonist and full agonist

Yuan Ping Pang, Javid Zaidi, Alan P. Kozikowski, Bernadette Cusack, Elliott Richelson

Research output: Contribution to journalArticle

Abstract

We report the rational design of novel neurotensin mimetics through use of the Multiple Template Approach. This approach is based on our notion that a flexible peptide can be replaced by a partially flexible molecule, identified through testing a comparatively small number of molecules possessing a different intrinsic availability of conformations of the native peptide. The Multiple Template Approach has culminated in the discovery of a pharmacologically unprecedented agent, which behaves as a neurotensin antagonist at low concentration and as a full neurotensin agonist at high concentration.

Original languageEnglish (US)
Pages (from-to)433-440
Number of pages8
JournalJournal of Computer-Aided Molecular Design
Volume8
Issue number4
DOIs
StatePublished - Aug 1 1994

Keywords

  • Drug design
  • Multiple Template Approach
  • Neurotensin agonist
  • Neurotensin antagonist

ASJC Scopus subject areas

  • Drug Discovery
  • Computer Science Applications
  • Physical and Theoretical Chemistry

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