Pocai Alessandro
Janssen Research and Devolopment, Cardiovascular and Metabolic Disease, 1516 Welsh and McKean Roads, Spring House, PA 19477, USA.
Mol Metab. 2013 Dec 14;3(3):241-51. doi: 10.1016/j.molmet.2013.12.001. eCollection 2014 Jun.
Oxyntomodulin (OXM) is a peptide hormone released from the gut in post-prandial state that activates both the glucagon-like peptide-1 receptor (GLP1R) and the glucagon receptor (GCGR) resulting in superior body weight lowering to selective GLP1R agonists. OXM reduces food intake and increases energy expenditure in humans. While activation of the GCGR increases glucose production posing a hyperglycemic risk, the simultaneous activation of the GLP1R counteracts this effect. Acute OXM infusion improves glucose tolerance in T2DM patients making dual agonists of the GCGR and GLP1R new promising treatments for diabetes and obesity with the potential for weight loss and glucose lowering superior to that of GLP1R agonists.
胃泌酸调节素(OXM)是一种在餐后状态下从肠道释放的肽类激素,它可激活胰高血糖素样肽-1受体(GLP1R)和胰高血糖素受体(GCGR),从而比选择性GLP1R激动剂更有效地降低体重。OXM可减少人类的食物摄入量并增加能量消耗。虽然GCGR的激活会增加葡萄糖生成,带来高血糖风险,但GLP1R的同时激活可抵消这种作用。急性输注OXM可改善2型糖尿病患者的葡萄糖耐量,使GCGR和GLP1R的双重激动剂成为治疗糖尿病和肥胖症的新的有前景的疗法,其减肥和降低血糖的潜力优于GLP1R激动剂。