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首页> 外文期刊>Acta crystallographica, Section F. Structural biology and crystallization communications >Structure of the beta-form of human MK2 in complex with the non-selective kinase inhibitor TEI-L03090
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Structure of the beta-form of human MK2 in complex with the non-selective kinase inhibitor TEI-L03090

机译：与非选择性激酶抑制剂TEI-L03090结合的人MK2β形式的结构

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摘要

Mitogen-activated protein kinase-activated protein kinase 2 (MK2 or MAPKAP-K2), a serine/threonine kinase from the p38 mitogen-activated protein kinase signalling pathway, plays an important role in the production of TNF-alpha and other cytokines. In a previous report, it was shown that MK2 in complex with the selective inhibitor TEI-I01800 adopts an alpha-helical glycine-rich loop that is induced by the stable nonplanar conformer of TEI-I01800. To understand the mechanism of the structural change, the structure of MK2 bound to TEI-L03090, which lacks the key substituent found in TEI-I01800, was determined. MK2-TEI-L03090 has a beta-sheet glycine-rich loop in common with other kinases, as predicted. This result suggests that a small compound can induce a drastic conformational change in the target protein structure and can be used to design potent and selective inhibitors.
机译：丝裂原激活的蛋白激酶激活的蛋白激酶2（MK2或MAPKAP-K2），一种来自p38丝裂原激活的蛋白激酶信号传导途径的丝氨酸/苏氨酸激酶，在TNF-α和其他细胞因子的产生中起重要作用。在先前的报道中，表明与选择性抑制剂TEI-I01800复合的MK2采用了由TEI-I01800的稳定的非平面构象异构体诱导的富含α-螺旋的富含甘氨酸的环。为了理解结构变化的机理，确定了与TEI-L03090结合的MK2的结构，该结构缺少TEI-I01800中发现的关键取代基。如所预测的，MK2-TEI-L03090具有与其他激酶相同的富含β-折叠的富含甘氨酸的环。该结果表明，小的化合物可以诱导靶蛋白结构发生剧烈的构象变化，并且可以用于设计有效的和选择性的抑制剂。

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