CaM激酶II（290-309），钙调蛋白拮抗剂

CaM激酶II（290-309），钙调蛋白拮抗剂是一种有效的，合成的CaMKII肽抑制剂（Ca | 2+ | /钙调蛋白依赖性蛋白激酶II），其来源于大鼠脑50-kDa alpha的cDNA序列亚基。该抑制肽的使用阐明了钙调蛋白的结合和抑制域，以及CaMKII的初始自磷酸化位点（Thr286），IC | 50 |为52 nM。该肽产物与CaM（钙调蛋白）紧密结合，并抑制其他需要钙调蛋白的酶，例如PDE（磷酸二酯酶）和PP2B（钙调神经磷酸酶）。研究人员在STC-1细胞中使用了该产品，以研究L型钙通道的调节 CaM Kinase II (290-309), Calmodulin Antagonist is a potent, synthetic peptide inhibitor of CaMKII (Ca|2+|/calmodulin-dependent protein kinase II), which was derived from the cDNA sequence of the rat brain 50-kDa alpha subunit. The use of this inhibitory peptide elucidated the calmodulin binding and inhibitory domains, as well as the initial autophosphorylation site (Thr286) of CaMKII with an IC|50|of 52 nM. This peptide product binds CaM (calmodulin) tightly and inhibits additional calmodulin-requiring enzymes, such as PDE (phosphodiesterase) and PP2B (calcineurin). Investigators used this product in STC-1 cells to study the regulation of L-type calcium channels and found the inhibitory peptide to block whole cell calcium currents. Additional research in T84 cells showed that this peptide reduced chloride current by approximately 70% without effect on the channels in parotid acinar cells.

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