Novel curcumin analog (cis-trans curcumin) as ligand to adenosine receptors A_2A and A_2B: potential for therapeutics.

ABSTRACT: All four of the adenosine receptor (AR) subtypes mediate pain and have been targeted by pharmacologists to generate new therapeutics for chronic pain. The vanilloid phytochemicals, which include curcumin, capsaicin, and gingerol, have been shown to alleviate pain. However, there is little to no literature on the interaction of vanilloid phytochemicals with ARs. In this study, photochemical methods were used to generate a novel isomer of curcumin (cis-trans curcumin or CTCUR), and the interactions of both curcumin and CTCUR with the two G_s-linked AR subtypes were studied. Competitive binding assays, docking analysis, and confocal fluorescence microscopy were performed to measure binding affinity; cell survival assays were used to measure toxicity; and cAMP assays were performed t

SUBMITTER: Hamilton LJ 

PROVIDER: S-EPMC7979524 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature