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The development of novel polypharmacological agents targeting the multiple binding sites of nicotinic acetylcholine receptors

dc.contributor.authorReyes-Parada M.
dc.contributor.authorIturriaga-Vasquez P.
dc.date.accessioned2020-09-02T22:26:59Z
dc.date.available2020-09-02T22:26:59Z
dc.date.issued2016
dc.identifier10.1080/17460441.2016.1227317
dc.identifier.citation11, 10, 969-981
dc.identifier.issn17460441
dc.identifier.urihttps://hdl.handle.net/20.500.12728/6011
dc.descriptionIntroduction: Polypharmacology, which refers to the ability of a molecule to simultaneously interact with multiple target proteins, is shifting the drug discovery process from a ‘one-drug-one-target’ paradigm to a conceptual framework in which the multitarget profile of small molecules is proactively pursued. Nicotinic acetylcholine receptors (nAChRs) appear as attractive targets for the design of polypharmacological agents. These proteins participate in the regulation of multiple physiological processes and impressive progress has been made regarding their structure and function. Moreover, they contain several ligand binding sites, and a number of compounds including orthosteric and allosteric ligands, have been described. Areas covered: The authors provide an overview of some of these topics and briefly discuss the mechanisms of action of some known promiscuous drugs that act at nAChRs, with the idea that this analysis will serve to guide the development of novel polypharmacological agents with a wide spectrum of actions. Expert opinion: The authors anticipate that many innovative drugs will be compounds intentionally designed to have polypharmacological properties. Furthermore, the authors suggest that although the search for multitarget drugs acting at the orthosteric site of nAChRs will remain an interesting option, allosteric sites of these receptors exhibit a much greater polypharmacological potential. © 2016 Informa UK Limited, trading as Taylor & Francis Group.
dc.language.isoen
dc.publisherTaylor and Francis Ltd
dc.subjectAllosteric sites
dc.subjectmultitarget
dc.subjectnAChRs
dc.subjectnicotinic acetylcholine receptors
dc.subjectorthosteric sites
dc.subjectpolypharmacology
dc.subject1,2,3,5 tetrahydro 5 methyl 1 (3 pyridylcarbamoyl)pyrrolo[2,3 f]indole
dc.subject3,4 methylenedioxymethamphetamine
dc.subject4 [[2 (1 methyl 2 pyrrolidinyl)ethyl]thio]phenol
dc.subjectamfebutamone
dc.subjectanalgesic agent
dc.subjectanandamide
dc.subjectanticonvulsive agent
dc.subjectantidepressant agent
dc.subjectcarbamazepine
dc.subjectcodeine
dc.subjectepibatidine
dc.subjectgalantamine
dc.subjectketamine
dc.subjectmemantine
dc.subjectmethadone
dc.subjectmethamphetamine
dc.subjectneuroleptic agent
dc.subjectnicotinic agent
dc.subjectnicotinic receptor
dc.subjectopiate
dc.subjectopiate agonist
dc.subjectpsychostimulant agent
dc.subjectserotonin 3 antagonist
dc.subjecttramadol
dc.subjecttropisetron
dc.subjectvarenicline
dc.subjectligand
dc.subjectnicotinic receptor
dc.subjectallosterism
dc.subjectbinding site
dc.subjectdrug mechanism
dc.subjecthuman
dc.subjectligand binding
dc.subjectnonhuman
dc.subjectpolypharmacology
dc.subjectpriority journal
dc.subjectReview
dc.subjectsmoking cessation
dc.subjectanimal
dc.subjectbinding site
dc.subjectdrug design
dc.subjectdrug development
dc.subjectdrug effects
dc.subjectmetabolism
dc.subjectmolecularly targeted therapy
dc.subjectpolypharmacology
dc.subjectprocedures
dc.subjectAnimals
dc.subjectBinding Sites
dc.subjectDrug Design
dc.subjectDrug Discovery
dc.subjectHumans
dc.subjectLigands
dc.subjectMolecular Targeted Therapy
dc.subjectPolypharmacology
dc.subjectReceptors, Nicotinic
dc.titleThe development of novel polypharmacological agents targeting the multiple binding sites of nicotinic acetylcholine receptors
dc.typeReview


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