Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain.
Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain.
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DOI：
10.1016/j.bmcl.2016.08.098
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发表时间：
2016-10-15
影响因子：
2.7
通讯作者：
Burke, Terrence R., Jr.
中科院分区：
文献类型：
--
作者：
Zhao, Xue Zhi;Hymel, David;Burke, Terrence R., Jr.
By a process involving initial screening of a set of 87 aldehydes using an oxime ligation-based strategy, we were able to achieve a several-fold affinity enhancement over one of the most potent previously known polo-like kinase 1 (Plk1) polo-box domain (PBD) binding inhibitors. This improved binding may result by accessing a newly identified auxiliary region proximal to a key hydrophobic cryptic pocket on the surface of the protein. Our findings could have general applicability to the design of PBD-binding antagonists.
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影响因子：
4
作者：
Liu F;Park JE;Qian WJ;Lim D;Scharow A;Berg T;Yaffe MB;Lee KS;Burke TR Jr
通讯作者：
Burke TR Jr
影响因子：
2.9
作者：
Qian WJ;Park JE;Grant R;Lai CC;Kelley JA;Yaffe MB;Lee KS;Burke TR Jr
通讯作者：
Burke TR Jr
影响因子：
16.6
作者：
Sledz, Pawel;Stubbs, Christopher J.;Lang, Steffen;Yang, Yong-Qing;McKenzie, Grahame J.;Venkitaraman, Ashok R.;Hyvoenen, Marko;Abell, Chris
通讯作者：
Abell, Chris
针对 polo 样激酶 1 的 polo-box 结构域的最小磷酸肽的结构和功能分析。
影响因子：
16.8
作者：
Yun, Sang-Moon;Moulaei, Tinoush;Lim, Dan;Bang, Jeong K.;Park, Jung-Eun;Shenoy, Shilpa R.;Liu, Fa;Kang, Young H.;Liao, Chenzhong;Soung, Nak-Kyun;Lee, Sunhee;Yoon, Do-Young;Lim, Yoongho;Lee, Dong-Hee;Otaka, Akira;Appella, Ettore;McMahon, James B.;Nicklaus, Marc C.;Burke, Terrence R., Jr.;Yaffe, Michael B.;Wlodawer, Alexander;Lee, Kyung S.
通讯作者：
Lee, Kyung S.
影响因子：
13.8
作者：
Lee KS;Burke TR Jr;Park JE;Bang JK;Lee E
通讯作者：
Lee E