FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2065207694> ?p ?o ?g. }

• W2065207694 endingPage "7448" @default.
• W2065207694 startingPage "7437" @default.
• W2065207694 abstract "His272 (7.43) in the seventh transmembrane domain (TM7) of the human A3 adenosine receptor (AR) interacts with the 3‘ position of nucleosides, based on selective affinity enhancement at a H272E mutant A3 AR (neoceptor) of 3‘-ureido, but not 3‘-OH, adenosine analogues. Here, mutation of the analogous H278 of the human A1 AR to Ala, Asp, Glu, or Leu enhanced the affinity of novel 2‘- and 3‘-ureido adenosine analogues, such as 10 (N6-cyclopentyl-3‘-ureido-3‘-deoxyadenosine), by >100-fold, while decreasing the affinity or potency of adenosine and other 3‘-OH adenosine analogues. His278 mutant receptors produced a similar enhancement regardless of the charge character of the substituted residue, implicating steric rather than electrostatic factors in the gain of function, a hypothesis supported by rhodopsin-based molecular modeling. It was also demonstrated that this interaction was orientationally specific; i.e., mutations at the neighboring Thr277 did not enhance the affinity for a series of 2‘- and 3‘-ureido nucleosides. Additionally, H-bonding groups placed on substituents at the N6 or 5‘ position demonstrated no enhancement in the mutant receptors. These reengineered human A1 ARs revealed orthogonality similar to that of the A3 but not the A2A AR, in which mutation of the corresponding residue, His278, to Asp did not enhance nucleoside affinity. Functionally, the H278D A1 AR was detectable only in a measure of membrane potential and not in calcium mobilization. This neoceptor approach should be useful for the validation of molecular modeling and the dissection of promiscuous GPCR signaling." @default.
• W2065207694 created "2016-06-24" @default.
• W2065207694 creator A5005713090 @default.
• W2065207694 creator A5006225135 @default.
• W2065207694 creator A5009684320 @default.
• W2065207694 creator A5017503475 @default.
• W2065207694 creator A5027166115 @default.
• W2065207694 creator A5036007966 @default.
• W2065207694 creator A5039708869 @default.
• W2065207694 creator A5074200367 @default.
• W2065207694 creator A5074447360 @default.
• W2065207694 creator A5089763876 @default.
• W2065207694 creator A5091587615 @default.
• W2065207694 date "2007-06-01" @default.
• W2065207694 modified "2023-10-15" @default.
• W2065207694 title "Probing the Binding Site of the A₁ Adenosine Receptor Reengineered for Orthogonal Recognition by Tailored Nucleosides" @default.
• W2065207694 cites W1497573731 @default.
• W2065207694 cites W1534993950 @default.
• W2065207694 cites W1540099187 @default.
• W2065207694 cites W1540109635 @default.
• W2065207694 cites W1547703436 @default.
• W2065207694 cites W1564690392 @default.
• W2065207694 cites W1592077035 @default.
• W2065207694 cites W1674184175 @default.
• W2065207694 cites W1963725788 @default.
• W2065207694 cites W1971024460 @default.
• W2065207694 cites W1971496273 @default.
• W2065207694 cites W1973056533 @default.
• W2065207694 cites W1974468894 @default.
• W2065207694 cites W1982263546 @default.
• W2065207694 cites W1985598247 @default.
• W2065207694 cites W1991255999 @default.
• W2065207694 cites W1993438049 @default.
• W2065207694 cites W2011805684 @default.
• W2065207694 cites W2013448155 @default.
• W2065207694 cites W2020586420 @default.
• W2065207694 cites W2030726671 @default.
• W2065207694 cites W2040166532 @default.
• W2065207694 cites W2041366274 @default.
• W2065207694 cites W2044616249 @default.
• W2065207694 cites W2049864289 @default.
• W2065207694 cites W2050146073 @default.
• W2065207694 cites W2059594639 @default.
• W2065207694 cites W2061785801 @default.
• W2065207694 cites W2063929711 @default.
• W2065207694 cites W2068775735 @default.
• W2065207694 cites W2069812375 @default.
• W2065207694 cites W2072532414 @default.
• W2065207694 cites W2074631079 @default.
• W2065207694 cites W2076204109 @default.
• W2065207694 cites W2078723380 @default.
• W2065207694 cites W2082904424 @default.
• W2065207694 cites W2086248928 @default.
• W2065207694 cites W2096380133 @default.
• W2065207694 cites W2100998296 @default.
• W2065207694 cites W2105624539 @default.
• W2065207694 cites W2106861254 @default.
• W2065207694 cites W2114779636 @default.
• W2065207694 cites W2119265045 @default.
• W2065207694 cites W2119692371 @default.
• W2065207694 cites W2124336386 @default.
• W2065207694 cites W2128635872 @default.
• W2065207694 cites W2131124255 @default.
• W2065207694 cites W2149963584 @default.
• W2065207694 cites W2404994572 @default.
• W2065207694 cites W2417738505 @default.
• W2065207694 cites W2900768805 @default.
• W2065207694 doi "https://doi.org/10.1021/bi7001828" @default.
• W2065207694 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3140710" @default.
• W2065207694 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17542617" @default.
• W2065207694 hasPublicationYear "2007" @default.
• W2065207694 type Work @default.
• W2065207694 sameAs 2065207694 @default.
• W2065207694 citedByCount "15" @default.
• W2065207694 countsByYear W20652076942013 @default.
• W2065207694 countsByYear W20652076942017 @default.
• W2065207694 countsByYear W20652076942020 @default.
• W2065207694 countsByYear W20652076942021 @default.
• W2065207694 countsByYear W20652076942022 @default.
• W2065207694 crossrefType "journal-article" @default.
• W2065207694 hasAuthorship W2065207694A5005713090 @default.
• W2065207694 hasAuthorship W2065207694A5006225135 @default.
• W2065207694 hasAuthorship W2065207694A5009684320 @default.
• W2065207694 hasAuthorship W2065207694A5017503475 @default.
• W2065207694 hasAuthorship W2065207694A5027166115 @default.
• W2065207694 hasAuthorship W2065207694A5036007966 @default.
• W2065207694 hasAuthorship W2065207694A5039708869 @default.
• W2065207694 hasAuthorship W2065207694A5074200367 @default.
• W2065207694 hasAuthorship W2065207694A5074447360 @default.
• W2065207694 hasAuthorship W2065207694A5089763876 @default.
• W2065207694 hasAuthorship W2065207694A5091587615 @default.
• W2065207694 hasBestOaLocation W20652076942 @default.
• W2065207694 hasConcept C104317684 @default.
• W2065207694 hasConcept C118892022 @default.
• W2065207694 hasConcept C12554922 @default.
• W2065207694 hasConcept C135285700 @default.
• W2065207694 hasConcept C143065580 @default.
• W2065207694 hasConcept C170493617 @default.

• next