Contemporary paradigms for cholinergic ligand design guided by biological structure

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1875-7. doi: 10.1016/j.bmcl.2003.10.072.

Abstract

The identification of the various nicotinic receptor subtypes, when coupled with the recent development of three-dimensional structures of surrogate extracellular receptor domains, offers new opportunities to design nicotinic ligands. Conformation and fluctuations in receptor structure are critical to ligand selectivity, and we present here how a flexible receptor template can be used in the development of selective ligands affecting cholinergic neurotransmission.

Publication types

  • Review

MeSH terms

  • Binding Sites
  • Drug Design*
  • Ligands
  • Nicotinic Agonists / chemical synthesis*
  • Nicotinic Agonists / metabolism
  • Nicotinic Agonists / pharmacology*
  • Protein Conformation
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / metabolism
  • Structure-Activity Relationship
  • Time Factors

Substances

  • Ligands
  • Nicotinic Agonists
  • Receptors, Nicotinic