title: Contemporary paradigms for cholinergic ligand design guided by biological structure.
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.
authors.affiliation: Department of Pharmacology, University of California-San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0636, USA. pwtaylor@ucsd.edu
authors.forename: Palmer
authors.initials: P
authors.lastname: Taylor
authors.forename: Scott B
authors.initials: SB
authors.lastname: Hansen
authors.forename: Todd T
authors.initials: TT
authors.lastname: Talley
authors.forename: Ryan E
authors.initials: RE
authors.lastname: Hibbs
authors.forename: Zoran
authors.initials: Z
authors.lastname: Radić
mesh_terms: D001665:Binding Sites; D015195:Drug Design; D008024:Ligands; D018722:Nicotinic Agonists / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D011487:Protein Conformation; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013997:Time Factors
chemical_list: D008024:Ligands; D018722:Nicotinic Agonists; D011978:Receptors, Nicotinic