Open AccessSynthesis of 3′-ureidoadenosines and their high binding affinity at the mutant A3 adenosine receptor
Author(s) -
Ae Yil Kim,
Hea Ok Kim,
Myoung Jung Kim,
Moon Woo Chun,
Kang Man Lee,
Kenneth A. Jacobson,
Lak Shin Jeong
Publication year - 2005
Publication title -
nucleic acids symposium series
Language(s) - English
Resource type - Journals
eISSN - 1746-8272
pISSN - 0261-3166
DOI - 10.1093/nass/49.1.105
Subject(s) - mutant , adenosine , adenosine receptor , chemistry , receptor , biochemistry , agonist , gene
For the purpose of developing optimal neoceptor-neoagonist pair, 3'-ureidoadenosine derivatives were synthesized. Among compounds tested, 2-chloro-3'-ureido-N6-(3-iodobenzyl)adenosine (10b) showed the best binding affinity (Ki = 0.20 microM) at the H272E mutant A3 AR, but was inactive at the natural A3 AR.
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