Table3.

Summary of known agonists of AdipoR1/R2 and molecules that could potentially be exploited clinically

Molecule	Comments	Reference
ADP355	Binds to both AdipoR1/R2 with greater affinity for AdipoR1. In vivo, ADP355 inhibits orthotopic human BC xenograft growth by 31%, with an acceptable safety profile. May activate signalling pathways similarly to gAcrp. The group tried to optimize ADP355's effects in 2015 and increased agonistic activity by a factor of 5-10	166,167
AdipoRon	Binds to AdipoR1/R2 at low micromolar concentrations. Has similar effects to APN on the muscle and liver	168
Naturally occurring compounds	Most active AdipoR1 ligands-matairesinol, arctiin, (-)-arctigenin and gramine. Most active AdipoR2 ligands- parthenolide, taxifoliol, deoxyschizandrin and syringin	169
Efatutazone	A selective PPARγ agonist showed promise in phase 1 trials, but phase 2 trials were disappointing with poor efficacy shown	171-174
Rivoglitazone	Shown to have beneficial effects on insulin resistance, type 2 diabetes and atherosclerosis in vivo via APN modulation. Effects on cancer have not been studied to date	176,177
Troglitazone	Has been shown to prevent tumor cell invasion in vivo. Phase 2 trials have been disappointing showing little clinical value	175,178,181,182
Δ2-Troglitazone	Synthetic derivative of troglitazone more potent than troglitazone. But not found to have any clinical value as of yet	179,180