AE 51310 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 G11 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.
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