葡萄糖激酶和葡萄糖激酶激活剂

Life metabolism Pub Date : 2023-07-13 eCollection Date: 2023-10-01 DOI:10.1093/lifemeta/load031
Changhong Li, Yi Zhang, Li Chen, Xiaoying Li
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引用次数: 0

摘要

葡萄糖激酶(GK)作为胰腺和肝脏中的葡萄糖传感器,在葡萄糖稳态中起着关键作用。GK功能丧失导致高血糖,功能获得导致先天性高胰岛素性低血糖。我们推测,胰岛和肝脏中GK mRNA和蛋白水平的逐渐丧失可能是2型糖尿病发病的关键机制。GK激活剂(GKA)作为一种抗糖尿病药物的开发已经进行了几十年的努力。GKA早期发展的失败是由于对GKA作用模式的认识有限。dorzagliatin治疗2型糖尿病的成功,为GK为T2D患者胰岛和肝脏潜在缺陷的修复建立良好的模型带来了新的希望。
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Glucokinase and glucokinase activator.

Glucokinase (GK) plays a pivotal role in glucose homeostasis as the glucose sensor in the pancreas and liver. Loss of function of GK results in hyperglycemia, and gain of function causes congenital hyperinsulinemic hypoglycemia. We speculate that the progressive loss of GK at both messenger RNA (mRNA) and protein levels in the islets and liver would be the key mechanism for Type 2 diabetes (T2D) pathogenesis. The development of GK activator (GKA) as an anti-diabetic drug has been endeavored for several decades. The failure of the early development of GKAs is due to the limitation of understanding the mode of GKA action. The success of dorzagliatin in the treatment of T2D has brought new hope for GK in setting a good model for repairing the underlying defects in the pancreatic islets and liver of T2D patients.

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