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Recent updates on GPCR biased agonism
(Elsevier B.V., 2016-10-01)
G protein-coupled receptors (GPCRs) are the most important targets for drug discovery and not surprisingly similar to 40% of all drugs currently in the market act on these receptors. Currently, one of the most active areas ...
Physiological implications of biased signaling at histamine H2 receptors
(Frontiers, 2015-03)
Histamine mediates numerous functions acting through its four receptor subtypes all belonging to the large family of seven transmembrane G-protein coupled receptors. In particular, histamine H2 receptor (H2R) is mainly ...
Signal transduction mechanism of biased ligands at histamine H2 receptors
(Portland Press, 2014-04-01)
7TMRs (seven-transmembrane receptors) exist as conformational collections in which different conformations would lead to differential downstream behaviours such as receptor phosphorylation, G-protein activation and receptor ...
Histamine H2 receptor biased signalling methods
(Springer, 2017)
Advances in the study of G protein coupled receptors (GPCRs) allow understanding of the existence of multiple possible receptor conformational states. Among the wide range of possible events that could be mediated by a ...
Noradrenaline, oxymetazoline and phorbol myristate acetate induce distinct functional actions and phosphorylation patterns of α1A-adrenergic receptors
(2017-12-01)
In LNCaP cells that stably express α1A-adrenergic receptors, oxymetazoline increased intracellular calcium and receptor phosphorylation, however, this agonist was a weak partial agonist, as compared to noradrenaline, for ...
Investigação de agonismo tendencioso em α1A- e α1B-adrenoceptores
(Universidade Estadual Paulista (Unesp), 2012-10-30)
Agonistas induzem ou estabilizam diferentes conformações de receptores com 7 domínios transmembrana (7TMRs) levando à modulação diferencial das atividades desses receptor. Este fenômeno é conhecido como eficácia colateral ...
Investigação de agonismo tendencioso em α1A- e α1B-adrenoceptores
(Universidade Estadual Paulista (Unesp), 2012-10-30)
Agonistas induzem ou estabilizam diferentes conformações de receptores com 7 domínios transmembrana (7TMRs) levando à modulação diferencial das atividades desses receptor. Este fenômeno é conhecido como eficácia colateral ...
Investigação de agonismo tendencioso em α1A- e α1B-adrenoceptores
(Universidade Estadual Paulista (UNESP), 2014)
Biased agonism at histamine H1 receptor: desensitization, internalization and MAPK activation triggered by antihistamines
(Elsevier Science, 2021-04)
Histamine H1 receptor ligands used clinically as antiallergics rank among the most widely prescribed and over-the-counter drugs in the world. They exert the therapeutic actions by blocking the effects of histamine, due to ...
Evaluación de la presencia y actividad de receptores cannabinoides en pulpa dental y odontoblastos humanos
(Universidad Nacional de ColombiaBogotá - Odontología - Maestría en OdontologíaFacultad de OdontologíaBogotá, ColombiaUniversidad Nacional de Colombia - Sede Bogotá, 2022-07-05)
La inflamación, la sensibilidad y el dolor dental continúan siendo un reto en la práctica odontológica, es por esa razón que la búsqueda de alternativas farmacológicas para su control es una necesidad. En ese sentido los ...