Qualitative differences in disease-associated MEK mutants reveal ...
Jul 13, 2022 · Point-mutations of MEK1, a central component of ERK signaling, are present in cancer and RASopathies, but their precise biological effects remain obscure. Here, we report a …
MEK1 and MEK2 inhibitors and cancer therapy: the long and
Sep 24, 2015 · New drugs that inhibit RAF or MEK1 and MEK2 have recently been approved or are currently undergoing late-stage clinical evaluation. In this Review, we consider the ERK …
MEK1 mutations confer resistance to MEK and B-RAF inhibition
Dec 1, 2009 · We investigated the clinical relevance of MEK dependency in melanoma by massively parallel sequencing of resistant clones generated from a MEK1 random …
c-Myc expression and MEK1-induced Erk2 nuclear localization are ...
Erk2 nuclear localization and c-myc expression promote TGF-β-induced EMT. (A) Immunofluorescent imaging of Erk2 localization (red) in IBC-10a cells transfected with …
Activating mutations in MEK1 enhance homodimerization and
Oct 30, 2018 · Yuan et al. characterized cancer-related mutations in the pathway-mediating kinase MEK1 and found that deletion mutations in a loop portion of the protein promoted …
MEK Guards Proteome Stability and Inhibits Tumor-Suppressive ...
Feb 12, 2015 · Beyond mediating cell-environment interactions, the MEK-HSF1 regulation impacts malignancy. In tumor cells, MEK blockade inactivates HSF1 and thereby provokes …
Defining the KRAS- and ERK-dependent transcriptome in KRAS
Immunoblot analyses showed that MEK1-DD alone was sufficient to prevent loss of phosphorylated and activated ERK1/2 (pERK) after treatment with inhibitors of mutant KRAS …
Light-Activated Kinases Enable Temporal Dissection of Signaling ...
Jan 27, 2011 · We report a general strategy for creating protein kinases in mammalian cells that are poised for very rapid activation by light. By photoactivating a caged version of MEK1, we …
Constitutive Activation of MEK1 Promotes Treg Cell Instability
Dec 12, 2014 · We found that the active form of COT/Tpl2 specifically inhibits the DNA binding activity of Foxp3 through a MEK-ERK-dependent pathway. Moreover, Treg cell-specific …
Structural basis of human Mediator recruitment by the ... - Nature
2 days ago · ERK2-GOF and MEK1-DD sequences were cloned into pColaDUET (Novagen) to obtain the pColaDUET MBP-ERK2-GOF/MEK1DD co-expression vector. All plasmids are …