Modulation of ERK5 Activity as a Therapeutic Anti-Cancer Strategy.
Modulation of ERK5 Activity as a Therapeutic Anti-Cancer Strategy.
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DOI：
10.1021/acs.jmedchem.3c00072
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发表时间：
2023-04-13
影响因子：
7.3
通讯作者：
Cano, Celine
中科院分区：
文献类型：
--
作者：
Miller, Duncan C.;Harnor, Suzannah J.;Martin, Mathew P.;Noble, Richard A.;Wedge, Stephen R.;Cano, Celine
细胞外信号调节激酶5（ERK 5）信号通路是四种常规的丝裂原活化蛋白（MAP）激酶通路之一。ERK5的遗传扰动表明，ERK5活性的调节可能在癌症化疗中具有治疗潜力。这个微型透视检查ERK5作为癌症药物靶点的证据，ERK5的结构，以及ERK5激酶结构域抑制剂的结构不同化学型的演变。新出现的ERK5药理学的复杂性进行了讨论，包括混杂现象的矛盾ERK5激活的小分子ERK5抑制剂。最近的发展和生物学评价的影响，有效的和选择性的双功能降解ERK 5和未来的机会，ERK调制也进行了探讨。
The extracellular signal-regulated kinase 5 (ERK5) signaling pathway is one of four conventional mitogen-activated protein (MAP) kinase pathways. Genetic perturbation of ERK5 has suggested that modulation of ERK5 activity may have therapeutic potential in cancer chemotherapy. This Miniperspective examines the evidence for ERK5 as a drug target in cancer, the structure of ERK5, and the evolution of structurally distinct chemotypes of ERK5 kinase domain inhibitors. The emerging complexities of ERK5 pharmacology are discussed, including the confounding phenomenon of paradoxical ERK5 activation by small-molecule ERK5 inhibitors. The impact of the recent development and biological evaluation of potent and selective bifunctional degraders of ERK5 and future opportunities in ERK modulation are also explored.
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影响因子：
6.7
作者：
Deng, Xianming;Elkins, Jonathan M.;Zhang, Jinwei;Yang, Qingkai;Erazo, Tatiana;Gomez, Nestor;Choi, Hwan Geun;Wang, Jinhua;Dzamko, Nicolas;Lee, Jiing-Dwan;Sim, Taebo;Kim, NamDoo;Alessi, Dario R.;Lizcano, Jose M.;Knapp, Stefan;Gray, Nathanael S.
通讯作者：
Gray, Nathanael S.
影响因子：
4.8
作者：
Inesta-Vaquera, Francisco A.;Campbell, David G.;Cuenda, A.
通讯作者：
Cuenda, A.
影响因子：
7.3
作者：
Miller, Duncan C.;Reuillon, Tristan;Molyneux, Lauren;Blackburn, Timothy;Cook, Simon J.;Edwards, Noel;Endicott, Jane A.;Golding, Bernard T.;Griffin, Roger J.;Hardcastle, Ian;Harnor, Suzannah J.;Heptinstall, Amy;Lochhead, Pamela;Martin, Mathew P.;Martin, Nick C.;Myers, Stephanie;Newell, David R.;Noble, Richard A.;Phillips, Nicole;Rigoreau, Laurent;Thomas, Huw;Tucker, Julie A.;Wang, Lan-Zhen;Waring, Michael J.;Wong, Ai-Ching;Wedge, Stephen R.;Noble, Martin E. M.;Cano, Celine
通讯作者：
Cano, Celine
影响因子：
11.2
作者：
Loveridge CJ;Mui EJ;Patel R;Tan EH;Ahmad I;Welsh M;Galbraith J;Hedley A;Nixon C;Blyth K;Sansom O;Leung HY
通讯作者：
Leung HY
影响因子：
4.8
作者：
Kamakura, S;Moriguchi, T;Nishida, E
通讯作者：
Nishida, E