Structure-based design of a pathway-specific nuclear import inhibitor
Structure-based design of a pathway-specific nuclear import inhibitor
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DOI：
10.1038/nsmb1229
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发表时间：
2007-05-01
影响因子：
16.8
通讯作者：
Chook, Yuh Min
中科院分区：
文献类型：
--
作者：
Cansizoglu, Ahmet E.;Lee, Brittany J.;Chook, Yuh Min
Kap β 2（也称为转运蛋白）识别PY核定位信号（NLS），这是一类新的具有R/H/Kx（（2-5））PY基序的NLS。在这里，我们表明，KAPB 2复合物含有疏水性和碱性PY-NLS，作为分类的一个额外的N-末端基序的组成，收敛在结构上只在共识基序，这解释了配体的多样性。基于这些数据和补充的生化分析，我们设计了一种Kap β 2特异性核输入抑制剂M9 M。
Kap beta 2 (also called transportin) recognizes PY nuclear localization signal (NLS), a new class of NLS with a R/H/Kx((2-5))PY motif. Here we show that Kapb2 complexes containing hydrophobic and basic PY-NLSs, as classified by the composition of an additional N-terminal motif, converge in structure only at consensus motifs, which explains ligand diversity. On the basis of these data and complementary biochemical analyses, we designed a Kap beta 2-specific nuclear import inhibitor, M9M.