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从黑曼巴蛇毒液中分离出的一种肽——钙抑素,是L型钙通道的特异性阻滞剂。

Calciseptine, a peptide isolated from black mamba venom, is a specific blocker of the L-type calcium channel.

作者信息

de Weille J R, Schweitz H, Maes P, Tartar A, Lazdunski M

机构信息

Institut de Pharmacologie Moléculaire et Cellulaire, Centre National de la Recherche Scientifique, Valbonne, France.

出版信息

Proc Natl Acad Sci U S A. 1991 Mar 15;88(6):2437-40. doi: 10.1073/pnas.88.6.2437.

Abstract

The venom of the black mamba contains a 60-amino acid peptide called calciseptine. The peptide has been fully sequenced. It is a smooth muscle relaxant and an inhibitor of cardiac contractions. Its physiological action resembles that of drugs, such as the 1,4-dihydropyridines, which are important in the treatment of cardiovascular diseases. Calciseptine, like the 1,4-dihydropyridines, selectively blocks L-type Ca2+ channels and is totally inactive on other voltage-dependent Ca2+ channels such as N-type and T-type channels. To our knowledge, it is the only natural polypeptide that has been shown to be a specific inhibitor of L-type Ca2+ channels.

摘要

黑曼巴蛇的毒液中含有一种名为钙通道阻滞剂的60个氨基酸的肽。该肽已被完全测序。它是一种平滑肌松弛剂和心脏收缩抑制剂。其生理作用类似于药物,如1,4-二氢吡啶类药物,这些药物在心血管疾病治疗中很重要。钙通道阻滞剂与1,4-二氢吡啶类药物一样,选择性地阻断L型钙通道,而对其他电压依赖性钙通道(如N型和T型通道)完全无活性。据我们所知,它是唯一已被证明是L型钙通道特异性抑制剂的天然多肽。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baa2/51247/97146ed56bfa/pnas01056-0412-a.jpg

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