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单词 G protein coupled receptors
释义

G protein coupled receptors

中文百科

G蛋白偶联受体 G protein–coupled receptor

(重定向自G protein coupled receptors)
G蛋白偶联受体的七跨膜α螺旋结构
由β2肾上腺素所激活的G蛋白偶联受体与Gs蛋白复合体的晶体结构(PDB 3SN6)。红色部分显示的是受体,绿色的是Gα亚基,青色的是Gβ亚基,而黄色的是Gγ亚基。可以看到Gα亚基的C端处于一个由第五和第六跨膜螺旋之间的膜内环向外移动所产生的空穴之中。

G蛋白偶联受体G Protein-Coupled ReceptorsGPCRs),是一大类膜蛋白受体的统称。这类受体的共同点是其立体结构中都有七个跨膜α螺旋,且其肽链的C端和连接第5和第6个跨膜螺旋的胞内环上都有G蛋白(鸟苷酸结合蛋白)的结合位点。目前为止,研究显示G蛋白偶联受体只见于真核生物之中,而且参与了很多细胞信号转导过程。在这些过程中,G蛋白偶联受体能结合细胞周围环境中的化学物质并激活细胞内的一系列信号通路,最终引起细胞状态的改变。已知的与G蛋白偶联受体结合的配体包括气味,费洛蒙,激素,神经递质,趋化因子等等。这些受体可以是小分子的糖类,脂质,多肽,也可以是蛋白质等生物大分子。一些特殊的G蛋白偶联受体也可以被非化学性的刺激源激活,例如在感光细胞中的视紫红质可以被光所激活。与G蛋白偶联受体相关的疾病为数众多,并且大约40%的现代药物都以G蛋白偶联受体作为靶点。

英语百科

G protein–coupled receptor G蛋白偶联受体

(重定向自G protein coupled receptors)
The seven-transmembrane α-helix structure of a G protein–coupled receptor
Two-dimensional schematic of a generic GPCR set in a Lipid Raft. Click the image for higher resolution to see details regarding the locations of important structures.
Cartoon depicting the basic concept of GPCR Conformational Activation. Ligand binding disrupts an ionic lock between the E/DRY motif of TM-3 and acidic residues of TM-6. As a result, the GPCR reorganizes to allow activation of G-alpha proteins. The side perspective is a view from above and to the side of the GPCR as it is set in the plasma membrane (the membrane lipids have been omitted for clarity). The intracellular perspective shows the view looking up at the plasma membrane from inside the cell.[41]

G protein–coupled receptors (GPCRs), also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein–linked receptors (GPLR), constitute a large protein family of receptors, that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times.

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更新时间:2025/6/18 3:19:19