Description
AE 51310 (433966-92-8) is a potent antagonist of the GPCR OPN4/melanopsin (Ki = 0.096 nM human OPN4).1 OPN4 regulates circadian rhythms, pupil functions, melatonin expression, cognition, and sleep. OPN4 has been found to bind Ga11 in lung cancer cells modulating PKC activation leading to activation of BRAF/MEK/ERK signaling pathways. AE 51310 decreased the growth and proliferation of both LG17 and LG55 lung cancer tumors in mouse xenograft models.2
References
Jones et al. (2013), Small-molecule antagonists of melanopsin-mediated phototransduction; Nat. Chem. Biol. 9 630
Wang et al. (2020), Targeting Opsin4/Melanopsin with a Novel Small Molecule Suppresses PKC/RAF/MEK/ERK Signaling and Inhibits Lung Adenocarcinoma Progression; Mol. Cancer Res. 18 1028
