Ontology highlight
ABSTRACT:
SUBMITTER: Maruoka H
PROVIDER: S-EPMC2935147 | biostudies-literature | 2010 Jun
REPOSITORIES: biostudies-literature
Maruoka Hiroshi H Barrett Matthew O MO Ko Hyojin H Tosh Dilip K DK Melman Artem A Burianek Lauren E LE Balasubramanian Ramachandran R Berk Barkin B Costanzi Stefano S Harden T Kendall TK Jacobson Kenneth A KA
Journal of medicinal chemistry 20100601 11
The P2Y(6) receptor is a cytoprotective G-protein-coupled receptor (GPCR) activated by UDP (EC(50) = 0.30 microM). We compared and combined modifications to enhance P2Y(6) receptor agonist selectivity, including ribose ring constraint, 5-iodo and 4-alkyloxyimino modifications, and phosphate modifications such as alpha,beta-methylene and extension of the terminal phosphate group into gamma-esters of UTP analogues. The conformationally constrained (S)-methanocarba-UDP is a full agonist (EC(50) = 0 ...[more]