5Z-7-氧代玉米烯醇以前所未有的方式与丝裂原活化蛋白激酶激酶7（MAP2K7）的半胱氨酸218共价结合。
5Z-7-Oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner.
作者信息
Sogabe Yuri, Matsumoto Takashi, Hashimoto Takuma, Kirii Yasuyuki, Sawa Masaaki, Kinoshita Takayoshi
机构信息
Graduate School of Science, Osaka Prefecture University, 1-1 Gakuen-cho, Naka-ku, Sakai, Osaka 599-8531, Japan.
Rigaku Corporation, 3-9-12 Matsubara-cho, Akishima, Tokyo 196-8666, Japan.
出版信息
Bioorg Med Chem Lett. 2015 Feb 1;25(3):593-6. doi: 10.1016/j.bmcl.2014.12.011. Epub 2014 Dec 13.
5Z-7-Oxozeaenol (5Z7O) is a covalent bonding inhibitor against the several protein kinases (e.g., ERK2 and TAK1) that possess a free cysteine at the gatekeeper-2 position. In addition to this cysteine, MAP2K7 has three other cysteine residues that are candidate for covalent bonding by the inhibitor 5Z7O. The crystal structure of the MAP2K7/5Z7O complex revealed that the inhibitor binds to MAP2K7 at a cysteine residue located at the end of the hinge region and not at the gatekeeper-2 residue. The structural insights into the interaction of 5Z7O with MAP2K7 should aid the development of 5Z7O derivatives with improved potency and selectivity.
5Z-7-氧代泽兰醇（5Z7O）是一种针对几种在守门人-2位置具有游离半胱氨酸的蛋白激酶（如ERK2和TAK1）的共价结合抑制剂。除了这个半胱氨酸外，MAP2K7还有其他三个半胱氨酸残基，它们是抑制剂5Z7O共价结合的候选位点。MAP2K7/5Z7O复合物的晶体结构表明，该抑制剂在位于铰链区末端的一个半胱氨酸残基处与MAP2K7结合，而不是在守门人-2残基处。对5Z7O与MAP2K7相互作用的结构洞察应有助于开发具有更高效力和选择性的5Z7O衍生物。
Zotero 插件