FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2092050340> ?p ?o ?g. }

• W2092050340 endingPage "4263" @default.
• W2092050340 startingPage "4253" @default.
• W2092050340 abstract "Despite their opposite effects on signal transduction, the nonapeptide hormone arginine‐vasopressin (AVP) and its V 1a receptor‐selective cyclic peptide antagonist d(CH 2 ) 5 [Tyr(Me)2]AVP display homologous primary structures, differing only at residues 1 and 2. These structural similarities led us to hypothesize that both ligands could interact with the same binding pocket in the V 1a receptor. To determine receptor residues responsible for discriminating binding of agonist and antagonist ligands, we performed site‐directed mutagenesis of conserved aromatic and hydrophilic residues as well as nonconserved residues, all located in the transmembrane binding pocket of the V 1a receptor. Mutation of aromatic residues of transmembrane region VI (W304, F307, F308) reduced affinity for the d(CH 2 ) 5 [Tyr(Me)2]AVP and markedly decreased affinity for the unrelated strongly hydrophobic V 1a ‐selective nonpeptide antagonist SR 49059. Replacement of these aromatic residues had no effect on AVP binding, but increased AVP‐induced coupling efficacy of the receptor for its G protein. Mutating hydrophilic residues Q108, K128 and Q185 in transmembrane regions II, III and IV, respectively, led to a decrease in affinity for both agonists and antagonists. Finally, the nonconserved residues T333 and A334 in transmembrane region VII, controlled the V 1a /V 2 binding selectivity for both nonpeptide and cyclic peptide antagonists. Thus, because conserved aromatic residues of the V 1a receptor binding pocket seem essential for antagonists and do not contribute at all to the binding of agonists, we propose that these residues differentiate agonist vs. antagonist ligand binding." @default.
• W2092050340 created "2016-06-24" @default.
• W2092050340 creator A5005673694 @default.
• W2092050340 creator A5028794237 @default.
• W2092050340 creator A5030780775 @default.
• W2092050340 creator A5036979652 @default.
• W2092050340 creator A5044535698 @default.
• W2092050340 creator A5061144307 @default.
• W2092050340 creator A5062762928 @default.
• W2092050340 creator A5064518842 @default.
• W2092050340 creator A5074765522 @default.
• W2092050340 creator A5079883467 @default.
• W2092050340 creator A5089955760 @default.
• W2092050340 date "2000-07-01" @default.
• W2092050340 modified "2023-10-16" @default.
• W2092050340 title "Conserved aromatic residues in the transmembrane region VI of the V_1avasopressin receptor differentiate agonist vs. antagonist ligand binding" @default.
• W2092050340 cites W1581548318 @default.
• W2092050340 cites W1591158701 @default.
• W2092050340 cites W1614960091 @default.
• W2092050340 cites W1866285812 @default.
• W2092050340 cites W1970736649 @default.
• W2092050340 cites W1985937682 @default.
• W2092050340 cites W1986288669 @default.
• W2092050340 cites W1988074381 @default.
• W2092050340 cites W1996996770 @default.
• W2092050340 cites W2001051130 @default.
• W2092050340 cites W2011295101 @default.
• W2092050340 cites W2012638283 @default.
• W2092050340 cites W2019807914 @default.
• W2092050340 cites W2023166473 @default.
• W2092050340 cites W2027467507 @default.
• W2092050340 cites W2033116575 @default.
• W2092050340 cites W2033388874 @default.
• W2092050340 cites W2035010803 @default.
• W2092050340 cites W2043813981 @default.
• W2092050340 cites W2044173369 @default.
• W2092050340 cites W2044500605 @default.
• W2092050340 cites W2057640040 @default.
• W2092050340 cites W2062176518 @default.
• W2092050340 cites W2062583603 @default.
• W2092050340 cites W2064195360 @default.
• W2092050340 cites W2069828003 @default.
• W2092050340 cites W2070821979 @default.
• W2092050340 cites W2073295308 @default.
• W2092050340 cites W2076175580 @default.
• W2092050340 cites W2090119198 @default.
• W2092050340 cites W2091666217 @default.
• W2092050340 cites W2093383312 @default.
• W2092050340 cites W2100573158 @default.
• W2092050340 cites W2101653844 @default.
• W2092050340 cites W2142750494 @default.
• W2092050340 cites W2146101256 @default.
• W2092050340 cites W2163865126 @default.
• W2092050340 cites W2168782248 @default.
• W2092050340 doi "https://doi.org/10.1046/j.1432-1033.2000.01472.x" @default.
• W2092050340 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10866830" @default.
• W2092050340 hasPublicationYear "2000" @default.
• W2092050340 type Work @default.
• W2092050340 sameAs 2092050340 @default.
• W2092050340 citedByCount "58" @default.
• W2092050340 countsByYear W20920503402012 @default.
• W2092050340 countsByYear W20920503402013 @default.
• W2092050340 countsByYear W20920503402016 @default.
• W2092050340 countsByYear W20920503402018 @default.
• W2092050340 countsByYear W20920503402019 @default.
• W2092050340 countsByYear W20920503402020 @default.
• W2092050340 countsByYear W20920503402021 @default.
• W2092050340 countsByYear W20920503402022 @default.
• W2092050340 countsByYear W20920503402023 @default.
• W2092050340 crossrefType "journal-article" @default.
• W2092050340 hasAuthorship W2092050340A5005673694 @default.
• W2092050340 hasAuthorship W2092050340A5028794237 @default.
• W2092050340 hasAuthorship W2092050340A5030780775 @default.
• W2092050340 hasAuthorship W2092050340A5036979652 @default.
• W2092050340 hasAuthorship W2092050340A5044535698 @default.
• W2092050340 hasAuthorship W2092050340A5061144307 @default.
• W2092050340 hasAuthorship W2092050340A5062762928 @default.
• W2092050340 hasAuthorship W2092050340A5064518842 @default.
• W2092050340 hasAuthorship W2092050340A5074765522 @default.
• W2092050340 hasAuthorship W2092050340A5079883467 @default.
• W2092050340 hasAuthorship W2092050340A5089955760 @default.
• W2092050340 hasConcept C107824862 @default.
• W2092050340 hasConcept C116569031 @default.
• W2092050340 hasConcept C118892022 @default.
• W2092050340 hasConcept C135285700 @default.
• W2092050340 hasConcept C170493617 @default.
• W2092050340 hasConcept C185592680 @default.
• W2092050340 hasConcept C24530287 @default.
• W2092050340 hasConcept C2776885963 @default.
• W2092050340 hasConcept C2778938600 @default.
• W2092050340 hasConcept C55493867 @default.
• W2092050340 hasConcept C71240020 @default.
• W2092050340 hasConcept C90474776 @default.
• W2092050340 hasConceptScore W2092050340C107824862 @default.
• W2092050340 hasConceptScore W2092050340C116569031 @default.
• W2092050340 hasConceptScore W2092050340C118892022 @default.
• W2092050340 hasConceptScore W2092050340C135285700 @default.
• W2092050340 hasConceptScore W2092050340C170493617 @default.

• next