Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor

[Image: see text] The nonclassical extracellular signal-related kinase 5 (ERK5) mitogen-activated protein kinase pathway has been implicated in increased cellular proliferation, migration, survival, and angiogenesis; hence, ERK5 inhibition may be an attractive approach for cancer treatment. However,...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9109144/
https://www.ncbi.nlm.nih.gov/pubmed/35468293
http://dx.doi.org/10.1021/acs.jmedchem.1c01756

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