Article
Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosides.
Biochemistry - 26 Jun 2007
Palaniappan Krishnan K, Gao Zhan-Guo, Ivanov Andrei A, Greaves Rebecca, Adachi Hayamitsu, Besada Pedro, Kim Hea Ok, Kim Ae Yil, Choe Seung Ah, Jeong Lak Shin, Jacobson Kenneth A
Abstract excerpt
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...
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