Ligand identification for G-protein-coupled receptors: a lead generation perspective

Curr Opin Chem Biol. 2004 Jun;8(3):287-96. doi: 10.1016/j.cbpa.2004.04.008.

Abstract

This review addresses strategies for the generation of ligands for G-protein-coupled receptors outside classical high-throughput screening and literature based approaches. These range from the chemical intuition-based strategies of endogenous ligand elaboration and privileged structure decoration to the in silico approaches of virtual screening and de novo design. Examples are cited where supporting pharmacological data has been presented.

Publication types

  • Review

MeSH terms

  • Combinatorial Chemistry Techniques / methods*
  • Computational Biology
  • Databases, Factual
  • Drug Design
  • Imidazoles / chemistry
  • Ligands
  • Molecular Structure
  • Piperidines / chemistry
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / drug effects
  • Receptors, G-Protein-Coupled / metabolism*
  • Receptors, Histamine H3 / metabolism
  • Thiourea / analogs & derivatives*
  • Thiourea / chemistry

Substances

  • Imidazoles
  • Ligands
  • Piperidines
  • Receptors, G-Protein-Coupled
  • Receptors, Histamine H3
  • Thiourea
  • clobenpropit