一种潜在的2型糖尿病药物靶点G蛋白偶联受体
人胰高血糖素类B G蛋白偶联受体(GCGR)
是62kDa蛋白质,属于B类G蛋白偶联受体家族。GCGR是2型糖尿病的潜在药物靶点,并且在葡萄糖稳态和2型糖尿病的病理生理学中起关键作用。
人胰高血糖素类B G蛋白偶联受体被胰高血糖素激活,并且是B类G蛋白偶联受体家族的成员,与Gαi,Gs和较小程度的Gαq 偶联。受体的刺激导致腺苷酸环化酶的活化和细胞内cAMP水平的增加。在人类中,胰高血糖素受体由GCGR基因编码。
胰高血糖素受体主要在肝脏和肾脏中表达,在心脏,脂肪组织,脾脏,胸腺,肾上腺,胰腺,大脑皮层和胃肠道中发现较少量。
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Reference
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