A conserved arginine with non‐conserved function is a key determinant of agonist selectivity in α7 nicotinic ACh receptors

dc.creatorMinguez Viñas, Teresa
dc.creatorNielsen, Beatriz Elizabeth
dc.creatorShoemark, Deborah K.
dc.creatorGotti, Cecilia
dc.creatorSessions, Richard B.
dc.creatorMulholland, Adrian J.
dc.creatorBouzat, Cecilia Beatriz
dc.creatorWonnacott, Susan
dc.creatorGallagher, Timothy
dc.creatorBermudez, Isabel
dc.creatorOliveira, Ana Sofia
dc.date.accessioned2021-06-29T13:27:57Z
dc.date.accessioned2022-10-15T12:05:16Z
dc.date.available2021-06-29T13:27:57Z
dc.date.available2022-10-15T12:05:16Z
dc.date.created2021-06-29T13:27:57Z
dc.date.issued2021-04
dc.identifierMinguez Viñas, Teresa; Nielsen, Beatriz Elizabeth; Shoemark, Deborah K.; Gotti, Cecilia; Sessions, Richard B.; et al.; A conserved arginine with non‐conserved function is a key determinant of agonist selectivity in α7 nicotinic ACh receptors; Wiley Blackwell Publishing, Inc; British Journal of Pharmacology; 178; 7; 4-2021; 1651-1668
dc.identifier0007-1188
dc.identifierhttp://hdl.handle.net/11336/135095
dc.identifier1476-5381
dc.identifierCONICET Digital
dc.identifierCONICET
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/4384025
dc.description.abstractThe α7 and α4β2* (“*” denotes possibly assembly with another subunit) nicotinic acetylcholine receptors (nAChRs) are the most abundant nAChRs in the mammalian brain. These receptors are the most targeted nAChRs in drug discovery programmes for brain disorders. However, the development of subtype-specific agonists remains challenging due to the high degree of sequence homology and conservation of function in nAChRs. We have developed C(10) variants of cytisine, a partial agonist of α4β2 nAChR that has been used for smoking cessation. The C(10) methyl analogue used in this study displays negligible affinity for α7 nAChR, while retaining high affinity for α4β2 nAChR.
dc.languageeng
dc.publisherWiley Blackwell Publishing, Inc
dc.relationinfo:eu-repo/semantics/altIdentifier/url/https://onlinelibrary.wiley.com/doi/10.1111/bph.15389
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1111/bph.15389
dc.rightshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.rightsAtribución-NoComercial-CompartirIgual 2.5 Argentina (CC BY-NC-SA 2.5 AR)
dc.subjectAGONIST SELECTIVITY
dc.subjectC(10) CYSTINE DERIVATIVES
dc.subjectCYSTINE
dc.subjectNICOTINIC ACh RECEPTORS
dc.titleA conserved arginine with non‐conserved function is a key determinant of agonist selectivity in α7 nicotinic ACh receptors
dc.typeinfo:eu-repo/semantics/article
dc.typeinfo:ar-repo/semantics/artículo
dc.typeinfo:eu-repo/semantics/publishedVersion


Este ítem pertenece a la siguiente institución