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岗田酸的自缔合:结构和药理学意义。

Self-association of okadaic acid: structural and pharmacological significance.

机构信息

University Institute for Bio-Organic Chemistry "Antonio González"-IUBO, University of La Laguna-ULL, Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain.

出版信息

Mar Drugs. 2013 May 29;11(6):1866-77. doi: 10.3390/md11061866.

Abstract

Okadaic acid (OA) has been an invaluable pharmacological tool in the study of cellular signaling. The great affinity of this polyether for its targets together with its high specificity to inhibit certain protein phosphatases enables the differential study of these proteins. Crystallographic structures of protein phosphatases in complex with OA show a 1:1 protein to toxin ratio. Nevertheless, it has been found that OA is able to self-associate under certain conditions although very little is known about the importance of this phenomenon. Here we review the available knowledge on the latter topic and we report on the existence of an unusual self-associated tetrameric form. The structure of these oligomers is proposed based on spectroscopic data and molecular modeling calculations.

摘要

冈田酸(OA)在细胞信号转导研究中是一种非常有价值的药理学工具。这种多醚与靶标具有很强的亲和力,并且对抑制某些蛋白磷酸酶具有很高的特异性,使得这些蛋白能够得到差异性研究。与 OA 结合的蛋白磷酸酶的晶体结构显示出 1:1 的蛋白与毒素比例。然而,已经发现 OA 在某些条件下能够自缔合,尽管人们对这种现象的重要性知之甚少。在这里,我们回顾了这方面的现有知识,并报告了存在一种不寻常的自缔合四聚体形式。这些低聚物的结构是基于光谱数据和分子建模计算提出的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/647f/3721210/cad3bfc77c90/marinedrugs-11-01866-g001.jpg

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