Registro completo de metadatos
| Campo DC | Valor | Lengua/Idioma |
|---|---|---|
| dc.creator | Arias, Hugo Rubén | - |
| dc.creator | Feuerbach, Dominik | - |
| dc.creator | Ortells, Marcelo Oscar | - |
| dc.date | 2018-03-08T19:52:38Z | - |
| dc.date | 2018-03-08T19:52:38Z | - |
| dc.date | 2015-07 | - |
| dc.date | 2018-03-08T19:02:27Z | - |
| dc.date.accessioned | 2019-04-29T15:29:34Z | - |
| dc.date.available | 2019-04-29T15:29:34Z | - |
| dc.date.issued | 2018-03-08T19:52:38Z | - |
| dc.date.issued | 2018-03-08T19:52:38Z | - |
| dc.date.issued | 2015-07 | - |
| dc.date.issued | 2018-03-08T19:02:27Z | - |
| dc.identifier | Arias, Hugo Rubén; Feuerbach, Dominik; Ortells, Marcelo Oscar; Functional and structural interaction of (-)-lobeline with human α4β2 and α4β4 nicotinic acetylcholine receptor subtypes; Pergamon-Elsevier Science Ltd; International Journal Of Biochemistry And Cellular Biology; 64; 7-2015; 15-24 | - |
| dc.identifier | 1357-2725 | - |
| dc.identifier | http://hdl.handle.net/11336/38315 | - |
| dc.identifier | CONICET Digital | - |
| dc.identifier | CONICET | - |
| dc.identifier.uri | http://rodna.bn.gov.ar:8080/jspui/handle/bnmm/295130 | - |
| dc.description | To determine the pharmacologic activity of (-)-lobeline between human (h)α4β2 and hα4β4 nicotinic acetylcholine receptors (AChRs), functional and structural experiments were performed. The Ca2+ influx results established that (-)-lobeline neither actives nor enhances the function of the studied AChR subtypes, but competitively inhibits hα4β4 AChRs with potency ∼10-fold higher than that for hα4β2 AChRs. This difference is due to a higher binding affinity for the [3H]cytisine sites at hα4β4 compared to hα4β2 AChRs, which, in turn, can be explained by our molecular dynamics (MD) results: (1) higher stability of (-)-lobeline and its hydrogen bonds within the α4β4 pocket compared to the α4β2 pocket, (2) (-)-lobeline promotes Loop C to cap the binding site at the α4β4 pocket, but forces Loop C to get apart from the α4β2 pocket, precluding the gating process elicited by agonists, and (3) the orientation of (-)-lobeline within the α4β4, but not the α4β2, subpocket, promoted by the t-(or t+) rotameric state of α4-Tyr98, remains unchanged during the whole MD simulation. This study gives a detailed view of the molecular and dynamics events evoked by (-)-lobeline supporting the differential binding affinity and subsequent inhibitory potency between hα4β2 and hα4β4 AChRs, and supports the possibility that the latter subtype is also involved in its activity. | - |
| dc.description | Fil: Arias, Hugo Rubén. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. California Northstate University. College of Medicine. Department of Medical Education; Estados Unidos | - |
| dc.description | Fil: Feuerbach, Dominik. Novartis Institutes for Biomedical Research. Neuroscience Research; Suiza | - |
| dc.description | Fil: Ortells, Marcelo Oscar. Universidad de Buenos Aires. Facultad de Medicina; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Morón; Argentina | - |
| dc.format | application/pdf | - |
| dc.format | application/pdf | - |
| dc.language | eng | - |
| dc.publisher | Pergamon-Elsevier Science Ltd | - |
| dc.relation | info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.biocel.2015.03.003 | - |
| dc.relation | info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S1357272515000722 | - |
| dc.rights | info:eu-repo/semantics/restrictedAccess | - |
| dc.rights | https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ | - |
| dc.source | reponame:CONICET Digital (CONICET) | - |
| dc.source | instname:Consejo Nacional de Investigaciones Científicas y Técnicas | - |
| dc.source | instacron:CONICET | - |
| dc.subject | (-)-LOBELINE | - |
| dc.subject | ACETYLCHOLINE RECEPTORS | - |
| dc.subject | CA<SUP>2+</SUP>INFLUX | - |
| dc.subject | COMPETITIVE ANTAGONIST | - |
| dc.subject | HUMAN Α4 Β2 AND Α4 Β4 NICOTINIC | - |
| dc.subject | MOLECULAR MODELING | - |
| dc.subject | Otras Ciencias Biológicas | - |
| dc.subject | Ciencias Biológicas | - |
| dc.subject | CIENCIAS NATURALES Y EXACTAS | - |
| dc.title | Functional and structural interaction of (-)-lobeline with human α4β2 and α4β4 nicotinic acetylcholine receptor subtypes | - |
| dc.type | info:eu-repo/semantics/article | - |
| dc.type | info:eu-repo/semantics/publishedVersion | - |
| dc.type | info:ar-repo/semantics/articulo | - |
| Aparece en las colecciones: | CONICET | |
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