FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3015269188> ?p ?o ?g. }

• W3015269188 endingPage "113961" @default.
• W3015269188 startingPage "113961" @default.
• W3015269188 abstract "It has been reported that muscarinic type-2 receptors (M2R) are voltage sensitive in an agonist-specific manner. In this work, we studied the effects of membrane potential on the interaction of M2R with the superagonist iperoxo (IXO), both functionally (using the activation of the ACh-gated K+ current (IKACh) in cardiomyocytes) and by molecular dynamics (MD) simulations. We found that IXO activated IKACh with remarkable high potency and clear voltage dependence, displaying a larger effect at the hyperpolarized potential. This result is consistent with a greater affinity, as validated by a slower (τ = 14.8 ± 2.3 s) deactivation kinetics of the IXO-evoked IKACh than that at the positive voltage (τ = 6.7 ± 1.2 s). The voltage-dependent M2R-IXO interaction induced IKACh to exhibit voltage-dependent features of this current, such as the ‘relaxation gating’ and the modulation of rectification. MD simulations revealed that membrane potential evoked specific conformational changes both at the external access and orthosteric site of M2R that underlie the agonist affinity change provoked by voltage on M2R. Moreover, our experimental data suggest that the ‘tyrosine lid’ (Y104, Y403, and Y426) is not the previously proposed voltage sensor of M2R. These findings provide an insight into the structural and functional framework of the biased signaling induced by voltage on GPCRs." @default.
• W3015269188 created "2020-04-17" @default.
• W3015269188 creator A5001541806 @default.
• W3015269188 creator A5008680377 @default.
• W3015269188 creator A5045669482 @default.
• W3015269188 creator A5048420627 @default.
• W3015269188 creator A5057770335 @default.
• W3015269188 creator A5058472088 @default.
• W3015269188 creator A5065265136 @default.
• W3015269188 creator A5090020641 @default.
• W3015269188 date "2020-07-01" @default.
• W3015269188 modified "2023-10-08" @default.
• W3015269188 title "Voltage-induced structural modifications on M2 muscarinic receptor and their functional implications when interacting with the superagonist iperoxo" @default.
• W3015269188 cites W1486438269 @default.
• W3015269188 cites W1507101852 @default.
• W3015269188 cites W1563859273 @default.
• W3015269188 cites W1587969012 @default.
• W3015269188 cites W1969027187 @default.
• W3015269188 cites W1973534594 @default.
• W3015269188 cites W1981021420 @default.
• W3015269188 cites W1981864581 @default.
• W3015269188 cites W1983622758 @default.
• W3015269188 cites W1991512318 @default.
• W3015269188 cites W2001695617 @default.
• W3015269188 cites W2020782494 @default.
• W3015269188 cites W2021520922 @default.
• W3015269188 cites W2021597184 @default.
• W3015269188 cites W2035759650 @default.
• W3015269188 cites W2049662715 @default.
• W3015269188 cites W2057228671 @default.
• W3015269188 cites W2057327972 @default.
• W3015269188 cites W2062934002 @default.
• W3015269188 cites W2066414494 @default.
• W3015269188 cites W2067174909 @default.
• W3015269188 cites W2074219666 @default.
• W3015269188 cites W2077376582 @default.
• W3015269188 cites W2081693079 @default.
• W3015269188 cites W2085544850 @default.
• W3015269188 cites W2088978287 @default.
• W3015269188 cites W2146991322 @default.
• W3015269188 cites W2159760589 @default.
• W3015269188 cites W2206954826 @default.
• W3015269188 cites W2327358015 @default.
• W3015269188 cites W2474393700 @default.
• W3015269188 cites W2512562801 @default.
• W3015269188 cites W2527392925 @default.
• W3015269188 cites W2529166446 @default.
• W3015269188 cites W2530696470 @default.
• W3015269188 cites W2612598385 @default.
• W3015269188 cites W2794209945 @default.
• W3015269188 cites W2889402136 @default.
• W3015269188 cites W2953107349 @default.
• W3015269188 cites W2962701388 @default.
• W3015269188 doi "https://doi.org/10.1016/j.bcp.2020.113961" @default.
• W3015269188 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32272111" @default.
• W3015269188 hasPublicationYear "2020" @default.
• W3015269188 type Work @default.
• W3015269188 sameAs 3015269188 @default.
• W3015269188 citedByCount "3" @default.
• W3015269188 countsByYear W30152691882020 @default.
• W3015269188 countsByYear W30152691882022 @default.
• W3015269188 countsByYear W30152691882023 @default.
• W3015269188 crossrefType "journal-article" @default.
• W3015269188 hasAuthorship W3015269188A5001541806 @default.
• W3015269188 hasAuthorship W3015269188A5008680377 @default.
• W3015269188 hasAuthorship W3015269188A5045669482 @default.
• W3015269188 hasAuthorship W3015269188A5048420627 @default.
• W3015269188 hasAuthorship W3015269188A5057770335 @default.
• W3015269188 hasAuthorship W3015269188A5058472088 @default.
• W3015269188 hasAuthorship W3015269188A5065265136 @default.
• W3015269188 hasAuthorship W3015269188A5090020641 @default.
• W3015269188 hasConcept C12554922 @default.
• W3015269188 hasConcept C169760540 @default.
• W3015269188 hasConcept C170493617 @default.
• W3015269188 hasConcept C181911157 @default.
• W3015269188 hasConcept C185592680 @default.
• W3015269188 hasConcept C194544171 @default.
• W3015269188 hasConcept C2778938600 @default.
• W3015269188 hasConcept C33789571 @default.
• W3015269188 hasConcept C55493867 @default.
• W3015269188 hasConcept C86803240 @default.
• W3015269188 hasConceptScore W3015269188C12554922 @default.
• W3015269188 hasConceptScore W3015269188C169760540 @default.
• W3015269188 hasConceptScore W3015269188C170493617 @default.
• W3015269188 hasConceptScore W3015269188C181911157 @default.
• W3015269188 hasConceptScore W3015269188C185592680 @default.
• W3015269188 hasConceptScore W3015269188C194544171 @default.
• W3015269188 hasConceptScore W3015269188C2778938600 @default.
• W3015269188 hasConceptScore W3015269188C33789571 @default.
• W3015269188 hasConceptScore W3015269188C55493867 @default.
• W3015269188 hasConceptScore W3015269188C86803240 @default.
• W3015269188 hasFunder F4320311777 @default.
• W3015269188 hasLocation W30152691881 @default.
• W3015269188 hasOpenAccess W3015269188 @default.
• W3015269188 hasPrimaryLocation W30152691881 @default.
• W3015269188 hasRelatedWork W1556946175 @default.
• W3015269188 hasRelatedWork W1999125786 @default.
• W3015269188 hasRelatedWork W2000749144 @default.

• next