Non-proteinogenic amino acids in the pThr-2 position of a pentamer peptide that confer high binding affinity for the polo box domain (PBD) of polo-like kinase 1 (Plk1).
Non-proteinogenic amino acids in the pThr-2 position of a pentamer peptide that confer high binding affinity for the polo box domain (PBD) of polo-like kinase 1 (Plk1).
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DOI：
10.1016/j.bmcl.2012.10.093
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发表时间：
2012-12-15
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：
Qian, Wen-Jian;Park, Jung-Eun;Lee, Kyung S.;Burke, Terrence R., Jr.
We report herein that incorporating long-chain alkylphenyl-containing non-proteinogenic amino acids in place of His at the pT-2 position of the parent polo-like kinase 1 (Plk1) polo box domain (PBD)-binding pentapeptide, PLHSpT (1a) increases affinity. For certain analogues, approximately two orders-of-magnitude improvement in affinity was observed. Although, none of the new analogues was as potent as our previously described peptide 1b, in which the pT-2 histidine imidazole ring is alkylated at its π nitrogen (N3), our current finding that the isomeric His(N1)-analogue (1c) binds with approximately 50-fold less affinity than 1b, indicates the positional importance of attachment to the His imidazole ring. Our demonstration that a range of modified residues at the pT-2 position can enhance binding affinity, should facilitate the development of minimally-sized Plk1 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：
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：
14.8
作者：
Liu, Fa;Park, Jung-Eun;Qian, Wen-Jian;Lim, Dan;Graeber, Martin;Berg, Thorsten;Yaffe, Michael B.;Lee, Kyung S.;Burke, Terrence R., Jr.
通讯作者：
Burke, Terrence R., Jr.
影响因子：
8
作者：
Park, Jung-Eun;Soung, Nak-Kyun;Johmura, Yoshikazu;Kang, Young H.;Liao, Chenzhong;Lee, Kyung H.;Park, Chi Hoon;Nicklaus, Marc C.;Lee, Kyung S.
通讯作者：
Lee, Kyung S.