%0 Journal Article
%T Unnatural Tripeptides as Potent Positive Allosteric Modulators of T1R2/T1R3
%J -
%D 2019
%R https://doi.org/10.1021/acsmedchemlett.9b00051
%X T1R2/T1R3 belongs to G protein coupled receptors, which recognizes diverse natural and synthetic sweeteners. A novel class of positive allosteric modulators (PAMs) of T1R2/T1R3 was identified through high-throughput screening campaign. Comparing the structure of the potent compound with previously known PAM, we classified the structure of known PAM into three parts, defined as ˇ°headˇ±, ˇ°linkerˇ±, and ˇ°tailˇ±. We then investigated the linker¨Ctail structure. It was suggested by molecular docking models of T1R2/T1R3 that an amine that we introduced in the tail was the key for interaction with the receptor binding pocket. We thus synthesized various molecules and found unnatural tripeptide-PAMs, which potently enhance the sweetness of sucrose in sensory evaluation tests
%U https://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00051