Journal of Medicinal Chemistry p. 928 - 940 (2019)
Update date:2022-08-12
Topics:
Nguyen, Duy
Lemos, Clara
Wortmann, Lars
Eis, Knut
Holton, Simon J.
Boemer, Ulf
Moosmayer, Dieter
Eberspaecher, Uwe
Weiske, Joerg
Lechner, Christian
Prechtl, Stefan
Suelzle, Detlev
Siegel, Franziska
Prinz, Florian
Lesche, Ralf
Nicke, Barbara
Nowak-Reppel, Katrin
Himmel, Herbert
Mumberg, Dominik
Von Nussbaum, Franz
Nising, Carl F.
Bauser, Marcus
Haegebarth, Andrea
The availability of a chemical probe to study the role of a specific domain of a protein in a concentration- and time-dependent manner is of high value. Herein, we report the identification of a highly potent and selective ERK5 inhibitor BAY-885 by high-throughput screening and subsequent structure-based optimization. ERK5 is a key integrator of cellular signal transduction, and it has been shown to play a role in various cellular processes such as proliferation, differentiation, apoptosis, and cell survival. We could demonstrate that inhibition of ERK5 kinase and transcriptional activity with a small molecule did not translate into antiproliferative activity in different relevant cell models, which is in contrast to the results obtained by RNAi technology.
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