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首页> 外文期刊>American Journal of Physiology >Desensitization of canonical transient receptor potential channel 5 by protein kinase C.
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Desensitization of canonical transient receptor potential channel 5 by protein kinase C.

机译：蛋白激酶C使典型瞬时受体电位通道5脱敏。

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摘要

The classic type of transient receptor potential channel (TRPC) is a molecular candidate for Ca(2+)-permeable cation channel in mammalian cells. TRPC5 is desensitized rapidly after activation by G protein-coupled receptor. Herein we report our investigation into the desensitization of mTRPC5 and localization of the molecular determinants of this desensitization using mutagenesis. TRPC5 was initially activated by muscarinic stimulation using 100 microM carbachol (CCh) and then decayed rapidly even in the presence of CCh (desensitization). Increased EGTA or omission of MgATP in the pipette solution slowed the rate of this desensitization. The protein kinase C (PKC) inhibitors, 1 microM chelerythrine, 100 nM GF109203X, or PKC peptide inhibitor (19-36), inhibited this desensitization of TRPC5 activated by 100 microM CCh. When TRPC5 current was activated by intracellular GTPgammaS, PKC inhibitors prevented TRPC5 desensitization and the mutation of TRPC5 T972 to alanine slowed the desensitization process dramatically. We conclude that the desensitization of TRPC5 occurs via PKC phosphorylation and suggest that threonine at residue 972 of mouse TRPC5 might be required for its phosphorylation by PKC.
机译：瞬时受体电位通道（TRPC）的经典类型是哺乳动物细胞中Ca（2 +）-可渗透阳离子通道的分子候选物。 TRPC5在被G蛋白偶联受体激活后迅速脱敏。在此，我们报告了我们对mTRPC5脱敏性的研究以及使用诱变技术对该脱敏性分子决定因素的定位。 TRPC5最初是通过使用100 microM卡巴胆碱（CCh）进行毒蕈碱刺激而激活的，然后即使在存在CCh（脱敏）的情况下也迅速降解。移液器中EGTA增加或MgATP缺失会减慢这种脱敏的速度。蛋白激酶C（PKC）抑制剂，1 microM白屈菜红碱，100 nM GF109203X或PKC肽抑制剂（19-36）抑制了被100 microM CCh激活的TRPC5的脱敏。当胞内GTPγS激活TRPC5电流时，PKC抑制剂阻止了TRPC5脱敏，并且TRPC5 T972向丙氨酸的突变极大地减缓了脱敏过程。我们得出的结论是，TRPC5的脱敏作用是通过PKC磷酸化而发生的，并且表明PKC的磷酸化可能需要小鼠TRPC5 972残基上的苏氨酸。

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