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Multiple binding sites in the nicotinic acetylcholine receptors: An opportunity for polypharmacolgy

dc.contributor.authorIturriaga-Vásquez P.
dc.contributor.authorAlzate-Morales J.
dc.contributor.authorBermudez I.
dc.contributor.authorVaras R.
dc.contributor.authorReyes-Parada M.
dc.date.accessioned2020-09-02T22:20:40Z
dc.date.available2020-09-02T22:20:40Z
dc.date.issued2015
dc.identifier10.1016/j.phrs.2015.08.018
dc.identifier.citation101, , 9-17
dc.identifier.issn10436618
dc.identifier.urihttps://hdl.handle.net/20.500.12728/4960
dc.descriptionFor decades, the development of selective compounds has been the main goal for chemists and biologists involved in drug discovery. However, diverse lines of evidence indicate that polypharmacological agents, i.e. those that act simultaneously at various protein targets, might show better profiles than selective ligands, regarding both efficacy and side effects. On the other hand, the availability of the crystal structure of different receptors allows a detailed analysis of the main interactions between drugs and receptors in a specific binding site. Neuronal nicotinic acetylcholine receptors (nAChRs) constitute a large and diverse family of ligand-gated ion channels (LGICs) that, as a product of its modulation, regulate neurotransmitter release, which in turns produce a global neuromodulation of the central nervous system. nAChRs are pentameric protein complexes in such a way that expression of compatible subunits can lead to various receptor assemblies or subtypes. The agonist binding site, located at the extracellular region, exhibits different properties depending on the subunits that conform the receptor. In the last years, it has been recognized that nAChRs could also contain one or more allosteric sites which could bind non-classical nicotinic ligands including several therapeutically useful drugs. The presence of multiple binding sites in nAChRs offers an interesting possibility for the development of novel polypharmacological agents with a wide spectrum of actions. © 2015 Elsevier Ltd. All rights reserved.
dc.language.isoen
dc.publisherAcademic Press
dc.subjectAllosteric ligands
dc.subjectDrug design
dc.subjectMedicinal chemistry
dc.subjectNicotinic receptor
dc.subjectOrthosteric ligands
dc.subjectPolypharmacology
dc.subject1,1 dimethyl 4 phenylpiperazinium
dc.subject1,2,3,5 tetrahydro 5 methyl 1 (3 pyridylcarbamoyl)pyrrolo[2,3 f]indole
dc.subject3 (2 azetidinylmethoxy)pyridine
dc.subjectamfebutamone
dc.subjectcarbamazepine
dc.subjectchlorpheniramine
dc.subjectepibatidine
dc.subjectgalantamine
dc.subjectligand gated ion channel
dc.subjectlobeline
dc.subjectmepyramine
dc.subjectneurotransmitter
dc.subjectnicotinic receptor
dc.subjectrivanicline
dc.subjectvarenicline
dc.subjectligand
dc.subjectnicotinic agent
dc.subjectnicotinic receptor
dc.subjectallosterism
dc.subjectAlzheimer disease
dc.subjectbinding site
dc.subjectcentral nervous system
dc.subjectdepression
dc.subjectdrug design
dc.subjectepilepsy
dc.subjecthuman
dc.subjectneuromodulation
dc.subjectneurotransmitter release
dc.subjectnonhuman
dc.subjectpolypharmacology
dc.subjectpriority journal
dc.subjectprotein assembly
dc.subjectprotein binding
dc.subjectprotein expression
dc.subjectprotein family
dc.subjectreceptor binding
dc.subjectreceptor upregulation
dc.subjectReview
dc.subjecttobacco dependence
dc.subjectanimal
dc.subjectbinding site
dc.subjectbrain
dc.subjectchemical structure
dc.subjectchemistry
dc.subjectdrug effects
dc.subjectmetabolism
dc.subjectnerve cell
dc.subjectpolypharmacology
dc.subjectAllosteric Regulation
dc.subjectAnimals
dc.subjectBinding Sites
dc.subjectBrain
dc.subjectHumans
dc.subjectLigands
dc.subjectModels, Molecular
dc.subjectNeurons
dc.subjectNicotinic Agonists
dc.subjectPolypharmacology
dc.subjectReceptors, Nicotinic
dc.titleMultiple binding sites in the nicotinic acetylcholine receptors: An opportunity for polypharmacolgy
dc.typeReview


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