Regulatory role of C‐terminus in the G‐protein coupling of the metabotropic glutamate receptor 1
Regulatory role of C‐terminus in the G‐protein coupling of the metabotropic glutamate receptor 1
复制标题
C 末端在代谢型谷氨酸受体 1 G 蛋白偶联中的调节作用
作者：
M. Tateyama;Y. Kubo
代谢型谷氨酸受体1α（mGlu 1 α）的信号传导特性不同于短形式剪接变体。这可能是由于近端C尾暴露了一簇带正电荷的氨基酸残基RRKK所致，认为其被mGlu 1 α的长C尾掩盖。我们发现，RRKK残基，暴露时，减弱Gq耦合和降低的基础活动和表面表达的mGlu 1，与以前的结果一致。此外，这些残基消除了mGlu 1的Gi/o偶联，但不影响谷氨酸诱导的二聚体重排和mGlu 1的蛋白激酶A依赖性调节。这些结果表明，RRKK残基不会抑制谷氨酸结合后的构象变化和蛋白质对发生G蛋白偶联的细胞内环的可及性，而是根据G蛋白的类型以不同的方式作为G蛋白偶联的抑制结构域。
The signaling property of metabotropic glutamate receptor 1α (mGlu1α) is different from that of short‐form splice variants. This could be caused by the exposure of a cluster of positively charged amino acid residues, RRKK, in the proximal C‐tail which is thought to be masked by the long C‐tail of mGlu1α. We found that the RRKK residues, when exposed, attenuate Gq coupling and decrease the basal activity and the surface expression of mGlu1, in agreement with previous results. Moreover, these residues abolish the Gi/o coupling of mGlu1, but do not affect glutamate‐induced dimeric rearrangement and protein kinase A‐dependent modulation of mGlu1. These results suggest that the RRKK residues do not inhibit the conformational change upon glutamate binding and protein accessibility to the intracellular loops where G‐protein coupling occurs, but rather act as an inhibitory domain against G‐protein coupling in a different manner depending on the type of G protein.
DOI：
10.1073/pnas.85.22.8747
发表时间：
1988-11-01
影响因子：
11.1
作者：
SUPATTAPONE, S;DANOFF, SK;SNYDER, SH
通讯作者：
SNYDER, SH