| Title : Glucagon-like peptide-1 analogs: Miracle drugs are blooming? - Gong_2024_Eur.J.Med.Chem_269_116342 |
| Author(s) : Gong B , Yao Z , Zhou C , Wang W , Sun L , Han J |
| Ref : Eur Journal of Medicinal Chemistry , 269 :116342 , 2024 |
| Abstract : Glucagon-like peptide-1 (GLP-1), secreted by L cells in the small intestine, assumes a central role in managing type 2 diabetes mellitus (T2DM) and obesity. Its influence on insulin secretion and gastric emptying positions it as a therapeutic linchpin. However, the limited applicability of native GLP-1 stems from its short half-life, primarily due to glomerular filtration and the inactivating effect of dipeptidyl peptidase-IV (DPP-IV). To address this, various structural modification strategies have been developed to extend GLP-1's half-life. Despite the commendable efficacy displayed by current GLP-1 receptor agonists, inherent limitations persist. A paradigm shift emerges with the advent of unimolecular multi-agonists, such as the recently introduced tirzepatide, wherein GLP-1 is ingeniously combined with other gastrointestinal hormones. This novel approach has captured the spotlight within the diabetes and obesity research community. This review summarizes the physiological functions of GLP-1, systematically explores diverse structural modifications, delves into the realm of unimolecular multi-agonists, and provides a nuanced portrayal of the developmental prospects that lie ahead for GLP-1 analogs. |
| ESTHER : Gong_2024_Eur.J.Med.Chem_269_116342 |
| PubMedSearch : Gong_2024_Eur.J.Med.Chem_269_116342 |
| PubMedID: 38531211 |
Gong B, Yao Z, Zhou C, Wang W, Sun L, Han J (2024)
Glucagon-like peptide-1 analogs: Miracle drugs are blooming?
Eur Journal of Medicinal Chemistry
269 :116342
Gong B, Yao Z, Zhou C, Wang W, Sun L, Han J (2024)
Eur Journal of Medicinal Chemistry
269 :116342