降钙素基因相关肽在T47D细胞系降钙素受体上的作用。
Action of calcitonin gene-related peptide at the calcitonin receptor of the T47D cell line.
作者信息
Raue F, Schneider H G, Zink A, Ziegler R
机构信息
Abteilung Innere Med. I, Endokrinologie und Stoffwechsel, Universität Heidelberg, Germany.
出版信息
Horm Metab Res. 1987 Nov;19(11):563-4. doi: 10.1055/s-2007-1011882.
Some effects of calcitonin (CT) can also be produced by calcitonin gene-related peptide (CGRP), an alternative product of the calcitonin gene. This might be mediated by interaction of CGRP at the CT-receptor site. The human breast cancer cell line T47D possesses well characterized CT-receptors (KD = 2.3 x 10(-10) M for 125I salmon CT). 50% inhibition of 125I-sCT binding was achieved with 10(-9) M sCT, 5 x 10(-6) M rat CGRP and 10(-5) M human CGRP. Half maximal cAMP production in T47D cells was seen with 6 x 10(-10) M sCT, 5 x 10(-6) M rCGRP and 10(-5) M hCGRP. Binding and displacement capacity as well as the biological activity of CT and CGRP seems to correlate well. These findings suggest that CGRP in pharmacological doses acts via the CT-receptor. This could be explained by the homology and conformational similarities between CT and CGRP.
降钙素基因相关肽（CGRP）是降钙素基因的另一种产物，它也能产生一些降钙素（CT）的作用。这可能是由CGRP在CT受体位点的相互作用介导的。人乳腺癌细胞系T47D具有特征明确的CT受体（125I标记的鲑鱼降钙素的解离常数KD = 2.3×10^(-10) M）。10^(-9) M的鲑鱼降钙素（sCT）、5×10^(-6) M的大鼠CGRP和10^(-5) M的人CGRP可实现对125I-sCT结合的50%抑制。在T47D细胞中，6×10^(-10) M的sCT、5×10^(-6) M的大鼠CGRP（rCGRP）和10^(-5) M的人CGRP（hCGRP）可使cAMP产生达到半数最大效应。CT和CGRP的结合与置换能力以及生物活性似乎具有良好的相关性。这些发现表明，药理剂量的CGRP通过CT受体发挥作用。这可以用CT和CGRP之间的同源性和构象相似性来解释。
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