FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2156912338> ?p ?o ?g. }

• W2156912338 abstract "We examined the effects on allosteric modulation and ligand binding of the mutation of amino acid residues of the human A(3) adenosine receptor (A(3)AR) that are hypothesized to be near one of three loci: the putative sodium binding site, the putative ligand binding site, and the DRY motif in transmembrane helical domain 3. The effects of three heterocyclic allosteric modulators [the imidazoquinoline 2-cyclopentyl-4-phenylamino-1H-imidazo[4,5-c]quinoline (DU124183), the pyridinylisoquinoline 4-methoxy-N-[7-methyl-3-(2-pyridinyl)-1-isoquinolinyl]benzamide (VUF5455), and the amiloride analog 5-(N,N-hexamethylene)-amiloride] on the dissociation of the agonist radioligand, N(6)- (4-amino-3-[(125)I]iodobenzyl)-5'-N-methylcarboxamidoadenosine, were compared at wild-type (WT) and mutant A(3)ARs. The F182A(5.43) and N274A(7.45) mutations eliminated the allosteric effects of all three modulators but had little effect on agonist binding. The N30A(1.50) and D58N(2.50) mutations abolished the allosteric effects of DU124183 and VUF5455, but not HMA, whereas the D107N(3.49) mutation abolished the effects of DU124183, but not HMA or VUF5455. The T94A(3.36), H95A(3.37), K152A(EL2), W243A(6.48), L244A(6.49), and S247A(6.52) mutations did not influence allosteric effects of the modulators. Sodium ions (100 mM), which modulate agonist binding at a variety of receptors, caused an approximately 80% inhibition of agonist binding in WT A(3)ARs but did not show any effect on D58N(2.50), D107N(3.49), and F182A(5.43) mutant receptors. In contrast, NaCl induced a modest increase of agonist binding in N30A(1.50) and N274A(7.45) mutant receptors. NaCl decreased the dissociation rate of the antagonist radioligand [(3)H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2.1-i]purin-5-one (PSB-11) at the WT A(3)ARs, but not the D58N(2.50) mutant receptor. The results were interpreted using a rhodopsin-based molecular model of the A(3)AR to suggest multiple binding modes of the allosteric modulators." @default.
• W2156912338 created "2016-06-24" @default.
• W2156912338 creator A5036007966 @default.
• W2156912338 creator A5053622077 @default.
• W2156912338 creator A5081127099 @default.
• W2156912338 creator A5083852937 @default.
• W2156912338 creator A5091587615 @default.
• W2156912338 creator A5091896594 @default.
• W2156912338 date "2003-05-01" @default.
• W2156912338 modified "2023-10-15" @default.
• W2156912338 title "Identification of Essential Residues Involved in the Allosteric Modulation of the Human A3Adenosine Receptor" @default.
• W2156912338 cites W1539774089 @default.
• W2156912338 cites W1590230654 @default.
• W2156912338 cites W1917800502 @default.
• W2156912338 cites W1963725788 @default.
• W2156912338 cites W1987883959 @default.
• W2156912338 cites W1988298211 @default.
• W2156912338 cites W1992958260 @default.
• W2156912338 cites W1993438049 @default.
• W2156912338 cites W2012666355 @default.
• W2156912338 cites W2016407435 @default.
• W2156912338 cites W2020564581 @default.
• W2156912338 cites W2023708421 @default.
• W2156912338 cites W2031476108 @default.
• W2156912338 cites W2042239308 @default.
• W2156912338 cites W2046311259 @default.
• W2156912338 cites W2050146073 @default.
• W2156912338 cites W2052570719 @default.
• W2156912338 cites W2074309655 @default.
• W2156912338 cites W2074631079 @default.
• W2156912338 cites W2075101183 @default.
• W2156912338 cites W2095775529 @default.
• W2156912338 cites W2098686294 @default.
• W2156912338 cites W2106140689 @default.
• W2156912338 cites W2114935719 @default.
• W2156912338 cites W2118338007 @default.
• W2156912338 cites W2128635872 @default.
• W2156912338 cites W2149963584 @default.
• W2156912338 cites W2153758876 @default.
• W2156912338 cites W2166225079 @default.
• W2156912338 cites W2170038549 @default.
• W2156912338 cites W2171828296 @default.
• W2156912338 cites W2176076159 @default.
• W2156912338 cites W2187251803 @default.
• W2156912338 cites W2199838004 @default.
• W2156912338 cites W2384135000 @default.
• W2156912338 cites W2398650198 @default.
• W2156912338 cites W2404994572 @default.
• W2156912338 cites W2419620389 @default.
• W2156912338 cites W4293247451 @default.
• W2156912338 doi "https://doi.org/10.1124/mol.63.5.1021" @default.
• W2156912338 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4367541" @default.
• W2156912338 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12695530" @default.
• W2156912338 hasPublicationYear "2003" @default.
• W2156912338 type Work @default.
• W2156912338 sameAs 2156912338 @default.
• W2156912338 citedByCount "76" @default.
• W2156912338 countsByYear W21569123382012 @default.
• W2156912338 countsByYear W21569123382013 @default.
• W2156912338 countsByYear W21569123382014 @default.
• W2156912338 countsByYear W21569123382015 @default.
• W2156912338 countsByYear W21569123382016 @default.
• W2156912338 countsByYear W21569123382017 @default.
• W2156912338 countsByYear W21569123382018 @default.
• W2156912338 countsByYear W21569123382019 @default.
• W2156912338 countsByYear W21569123382021 @default.
• W2156912338 countsByYear W21569123382022 @default.
• W2156912338 crossrefType "journal-article" @default.
• W2156912338 hasAuthorship W2156912338A5036007966 @default.
• W2156912338 hasAuthorship W2156912338A5053622077 @default.
• W2156912338 hasAuthorship W2156912338A5081127099 @default.
• W2156912338 hasAuthorship W2156912338A5083852937 @default.
• W2156912338 hasAuthorship W2156912338A5091587615 @default.
• W2156912338 hasAuthorship W2156912338A5091896594 @default.
• W2156912338 hasBestOaLocation W21569123382 @default.
• W2156912338 hasConcept C104317684 @default.
• W2156912338 hasConcept C107824862 @default.
• W2156912338 hasConcept C116569031 @default.
• W2156912338 hasConcept C118892022 @default.
• W2156912338 hasConcept C143065580 @default.
• W2156912338 hasConcept C166342909 @default.
• W2156912338 hasConcept C170493617 @default.
• W2156912338 hasConcept C178790620 @default.
• W2156912338 hasConcept C185592680 @default.
• W2156912338 hasConcept C2776038425 @default.
• W2156912338 hasConcept C2778938600 @default.
• W2156912338 hasConcept C2779608910 @default.
• W2156912338 hasConcept C50254741 @default.
• W2156912338 hasConcept C537181965 @default.
• W2156912338 hasConcept C55493867 @default.
• W2156912338 hasConcept C67847695 @default.
• W2156912338 hasConcept C71240020 @default.
• W2156912338 hasConcept C86803240 @default.
• W2156912338 hasConcept C98274493 @default.
• W2156912338 hasConceptScore W2156912338C104317684 @default.
• W2156912338 hasConceptScore W2156912338C107824862 @default.
• W2156912338 hasConceptScore W2156912338C116569031 @default.
• W2156912338 hasConceptScore W2156912338C118892022 @default.
• W2156912338 hasConceptScore W2156912338C143065580 @default.
• W2156912338 hasConceptScore W2156912338C166342909 @default.

• next