Article
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
Journal of medicinal chemistry - 4 May 2006
Gao Zhan-Guo, Duong Heng T, Sonina Tatiana, Kim Soo-Kyung, Van Rompaey Philippe, Van Calenbergh Serge, Mamedova Liaman, Kim Hea Ok, Kim Myong Jung, Kim Ae Yil, Liang Bruce T, Jeong Lak Shin, Jacobson Kenneth A
Abstract excerpt
An alternative approach to overcome the inherent lack of specificity of conventional agonist therapy can be the reengineering of the GPCRs and their agonists. A reengineered receptor (neoceptor) could be selectively activated by a modified agonist, but not by the endogenous agonist. Assisted by rhodopsin-based molecular modeling, we pinpointed mutations of the A(3) adenosine receptor (AR) for selective affinity...
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