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GPR81是乳酸的特异性受体,具有调节脂肪细胞发育和分化、抑制脂肪分解、抑制炎性反应,以及调节脑能量代谢、脑血流量和神经元功能的协同变化等生物学功能。GPR81生物学功能的分子机制包括:(1)通过GPR81/Gi/c AMP信号转导通路抑制脂肪分解和调节脑能量代谢、脑血流量和神经元功能的协同变化;(2)通过GPR81/β-arrestin 2/NF-κB及GPR81/β-arrestin 2/NLRP3信号通路抑制巨噬细胞炎性反应。GPR81功能异常与肥胖、血脂异常、胰岛素抵抗、糖耐量减低和2型糖尿病密切相关,还可能参与了颞叶癫痫、中枢性疲乏及缺血性脑血管疾病的发生发展。就乳酸受体GPR81在脂质代谢、炎性反应及中枢神经系统中的作用进行综述。
GPR81 is a specific receptor for lactic acid and has biological functions such as regulating adipocyte development and differentiation, inhibiting lipolysis, inhibiting inflammatory responses, and regulating synergistic changes in brain energy metabolism, cerebral blood flow and neuronal function. The molecular mechanisms of GPR81 biological function include: (1) inhibition of lipolysis and regulation of brain energy metabolism, cerebral blood flow, and neuronal co-ordination through the GPR81 / Gi / c AMP signal transduction pathway; (2) -arrestin 2 / NF-κB and GPR81 / β-arrestin 2 / NLRP3 signaling pathway to inhibit macrophage inflammatory response. GPR81 dysfunction and obesity, dyslipidemia, insulin resistance, impaired glucose tolerance and type 2 diabetes are closely related, may also be involved in the temporal lobe epilepsy, central fatigue and ischemic cerebrovascular disease development. The role of lactic acid receptor GPR81 in lipid metabolism, inflammatory response and central nervous system is reviewed.