FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2000781683> ?p ?o ?g. }

• W2000781683 endingPage "319" @default.
• W2000781683 startingPage "307" @default.
• W2000781683 abstract "Activation of G protein-coupled receptors involves major conformational changes of the receptor protein ranging from the extracellular transmitter binding site to the intracellular G protein binding surface. GPCRs such as the muscarinic acetylcholine receptors are commonly probed with radioantagonists rather than radioagonists due to better physicochemical stability, higher affinity, and indifference towards receptor coupling states of the former. Here we introduce tritiated iperoxo, a superagonist at muscarinic M₂ receptors with very high affinity. In membrane suspensions of transfected CHO-cells, [³H]iperoxo - unlike the common radioagonists [³H]acetylcholine and [³H]oxotremorine M - allowed labelling of each of the five muscarinic receptor subtypes in radioagonist displacement and saturation binding studies. [³H]iperoxo revealed considerable differences in affinity between the even- and the odd-numbered muscarinic receptor subtypes with affinities for the M₂ and M₄ receptor in the picomolar range. Probing ternary complex formation on the M₂ receptor, [³H]iperoxo dissociation was not influenced by an archetypal allosteric inverse agonist, reflecting activation-related rearrangement of the extracellular loop region. At the inner side of M₂, the preferred Gi protein acted as a positive allosteric modulator of [³H]iperoxo binding, whereas Gs and Gq were neutral in spite of their robust coupling to the activated receptor. In intact CHO-hM₂ cells, endogenous guanylnucleotides promoted receptor/G protein-dissociation resulting in low-affinity agonist binding which, nevertheless, was still reported by [³H]iperoxo. Taken together, the muscarinic superagonist [³H]iperoxo is the best tool currently available for direct probing activation-related conformational transitions of muscarinic receptors." @default.
• W2000781683 created "2016-06-24" @default.
• W2000781683 creator A5001570276 @default.
• W2000781683 creator A5014699496 @default.
• W2000781683 creator A5027547347 @default.
• W2000781683 creator A5041124848 @default.
• W2000781683 creator A5051799439 @default.
• W2000781683 creator A5054216760 @default.
• W2000781683 creator A5054989005 @default.
• W2000781683 creator A5063567773 @default.
• W2000781683 creator A5068257865 @default.
• W2000781683 creator A5070492902 @default.
• W2000781683 creator A5075533722 @default.
• W2000781683 date "2014-08-01" @default.
• W2000781683 modified "2023-10-12" @default.
• W2000781683 title "New insight into active muscarinic receptors with the novel radioagonist [3H]iperoxo" @default.
• W2000781683 cites W1507101852 @default.
• W2000781683 cites W1521405901 @default.
• W2000781683 cites W1556070936 @default.
• W2000781683 cites W1601065938 @default.
• W2000781683 cites W1775749144 @default.
• W2000781683 cites W1964773764 @default.
• W2000781683 cites W1969027187 @default.
• W2000781683 cites W1975985866 @default.
• W2000781683 cites W1976140850 @default.
• W2000781683 cites W1983534052 @default.
• W2000781683 cites W1987755014 @default.
• W2000781683 cites W1987883959 @default.
• W2000781683 cites W1988097700 @default.
• W2000781683 cites W1989208794 @default.
• W2000781683 cites W1989971979 @default.
• W2000781683 cites W1999774383 @default.
• W2000781683 cites W2003620627 @default.
• W2000781683 cites W2021834385 @default.
• W2000781683 cites W2028645925 @default.
• W2000781683 cites W2044775506 @default.
• W2000781683 cites W2047038784 @default.
• W2000781683 cites W2047144511 @default.
• W2000781683 cites W2048999929 @default.
• W2000781683 cites W2049662715 @default.
• W2000781683 cites W2051994079 @default.
• W2000781683 cites W2054384158 @default.
• W2000781683 cites W2073324778 @default.
• W2000781683 cites W2073654245 @default.
• W2000781683 cites W2074631079 @default.
• W2000781683 cites W2077936290 @default.
• W2000781683 cites W2078402446 @default.
• W2000781683 cites W2086106584 @default.
• W2000781683 cites W2087135060 @default.
• W2000781683 cites W2087372220 @default.
• W2000781683 cites W2088155357 @default.
• W2000781683 cites W2106630611 @default.
• W2000781683 cites W2109014958 @default.
• W2000781683 cites W2116151143 @default.
• W2000781683 cites W2118333549 @default.
• W2000781683 cites W2130141176 @default.
• W2000781683 cites W2132746917 @default.
• W2000781683 cites W2135008467 @default.
• W2000781683 cites W2139129258 @default.
• W2000781683 cites W2143455502 @default.
• W2000781683 cites W2150634831 @default.
• W2000781683 cites W2152126634 @default.
• W2000781683 cites W2160991890 @default.
• W2000781683 cites W2167857702 @default.
• W2000781683 doi "https://doi.org/10.1016/j.bcp.2014.05.012" @default.
• W2000781683 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24863257" @default.
• W2000781683 hasPublicationYear "2014" @default.
• W2000781683 type Work @default.
• W2000781683 sameAs 2000781683 @default.
• W2000781683 citedByCount "15" @default.
• W2000781683 countsByYear W20007816832015 @default.
• W2000781683 countsByYear W20007816832017 @default.
• W2000781683 countsByYear W20007816832018 @default.
• W2000781683 countsByYear W20007816832019 @default.
• W2000781683 countsByYear W20007816832020 @default.
• W2000781683 countsByYear W20007816832021 @default.
• W2000781683 countsByYear W20007816832022 @default.
• W2000781683 crossrefType "journal-article" @default.
• W2000781683 hasAuthorship W2000781683A5001570276 @default.
• W2000781683 hasAuthorship W2000781683A5014699496 @default.
• W2000781683 hasAuthorship W2000781683A5027547347 @default.
• W2000781683 hasAuthorship W2000781683A5041124848 @default.
• W2000781683 hasAuthorship W2000781683A5051799439 @default.
• W2000781683 hasAuthorship W2000781683A5054216760 @default.
• W2000781683 hasAuthorship W2000781683A5054989005 @default.
• W2000781683 hasAuthorship W2000781683A5063567773 @default.
• W2000781683 hasAuthorship W2000781683A5068257865 @default.
• W2000781683 hasAuthorship W2000781683A5070492902 @default.
• W2000781683 hasAuthorship W2000781683A5075533722 @default.
• W2000781683 hasConcept C116289061 @default.
• W2000781683 hasConcept C12554922 @default.
• W2000781683 hasConcept C135285700 @default.
• W2000781683 hasConcept C166342909 @default.
• W2000781683 hasConcept C170493617 @default.
• W2000781683 hasConcept C185592680 @default.
• W2000781683 hasConcept C207723603 @default.
• W2000781683 hasConcept C2778824757 @default.
• W2000781683 hasConcept C2778938600 @default.

• next