1. Signaling Pathways
  2. GPCR/G Protein
  3. RGS Protein

RGS Protein (RGS蛋白)

RGS (Regulators of G protein signaling) are protein structural domains that activate GTPases for heterotrimeric G-protein alpha-subunits. RGS proteins are multi-functional, GTPase-accelerating proteins that promote GTP hydrolysis by the alpha subunit of heterotrimeric G proteins, thereby inactivating the G protein and rapidly switching off G protein-coupled receptor signaling pathways. Upon activation by GPCRs, heterotrimeric G proteins exchange GDP for GTP, are released from the receptor, and dissociate into free, active GTP-bound alpha subunit and beta-gamma dimer, both of which activate downstream effectors. The response is terminated upon GTP hydrolysis by the alpha subunit, which can then bind the beta-gamma dimer and the receptor. RGS proteins markedly reduce the lifespan of GTP-bound alpha subunits by stabilising the G protein transition state. All RGS proteins contain an RGS-box (or RGS domain), which is required for activity. Some small RGS proteins such as RGS1 and RGS4 are little more than an RGS domain, while others also contain additional domains that confer further functionality.

RGS Protein 相关产品 (2):

目录号 产品名 作用方式 纯度
  • HY-70074
    CCG-63802 Inhibitor
    CCG-63802 是一种选择性,可逆变构的 G 蛋白信号调节子 RGS4 抑制剂。CCG-63802 与 RGS4 特异性结合并阻断 RGS4-Gαo 相互作用,IC50 值为 1.9 μM。
  • HY-70075
    CCG-63808 Inhibitor
    CCG-63808 是可逆的G蛋白信号调节子(RGS)抑制剂。
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