TGR5 agonists for diabetes treatment: a patent review and clinical advancements (2012-present).

Preclinical studies have suggested a key role for the TGR5 receptor in GLP-1 secretion and have shown promising outcomes such as weight loss, anti-inflammatory, anti-diabetic effects. Along with the evaluation of semisynthetic derivatives, synthetic compounds can also be considered as a possible avenue for the discovery of novel TGR5 agonists. Currently, few TGR5 agonists have reached the clinical trial stage, and, likely, we will soon discover a novel TGR5 modulator with fewer adverse effects. In silico studies can be performed with these scaffolds ranging from steroidal to heterocyclic rings to discover selective and safe TGR5 agonists.