Liganded Gq/11-activating GPCRs act as GEFs for Gq/11
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G alpha q protein (or Gq/11) consists of four family members (G-alpha 11, -alpha 14, -alpha 15 and -alpha q). It activates phospholipase C (PLC) (Dowal L et al, 2006). PLC hydrolyzes phosphatidylinositol (PIP2) to diacyl glycerol (DAG) and inositol triphosphate (IP3). DAG acts as a second messenger that activates protein kinase C (PKC) and IP3 can bind to IP3 receptors, particular calcium channels in the endoplasmic reticulum (ER). Calcium flow causes the cytosolic concentration of calcium to increase, causing a cascade of intracellular changes and activity.
Gαq蛋白(或称Gq/11)由四个家族成员组成,包括G-α11、G-α14、G-α15和G-αq。该蛋白能够激活磷脂酶C(PLC)(Dowal L 等人,2006年)。PLC催化磷脂酰肌醇(PIP2)水解生成二酰甘油(DAG)和肌醇三磷酸(IP3)。DAG作为一种第二信使,激活蛋白激酶C(PKC),而IP3能够与IP3受体结合,尤其是内质网(ER)中的钙通道。钙流的增加导致细胞质中钙浓度升高,引发一系列细胞内变化和活动。
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