MEK1 and MEK2 inhibitors and cancer therapy: the long and
2015年9月24日 · 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 …
Activating mutations in MEK1 enhance homodimerization and
2018年10月30日 · A partial disruption of the dimer interface by GG (N78G and V224G) or AA (F311A and L314A) mutations reduced the activity of MEK1(ΔIHLEIK) as predicted, whereas …
Qualitative differences in disease-associated MEK mutants reveal ...
2022年7月13日 · Here, we report a mutant MEK1 structure that uncovers the mechanisms underlying abnormal activities of cancer- and RASopathy-associated MEK1 mutants. These …
Light-Activated Kinases Enable Temporal Dissection of Signaling ...
2011年1月27日 · 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, …
MEK1 mutations confer resistance to MEK and B-RAF inhibition
2009年12月1日 · Functional characterization of MEK1 resistance mutations identified in vitro. Growth inhibition curves of parental A375 (solid black), A375 cells expressing primary or …
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 …
MEK Guards Proteome Stability and Inhibits Tumor-Suppressive ...
2015年2月12日 · Here, we report that RAS-MEK-ERK signaling critically regulates the PSR. It is MEK that phosphorylates and activates HSF1. MEK inhibition destabilizes the proteome, …
“基因说”之三：MEK1 - 搜狐
2015年12月6日 · MEK1（MAP kinase kinase 1或mitogen-activated proteinkinase kinase 1），也叫 MAP2K1或MAPKK1，中文是丝裂原活化蛋白激酶激酶1，是Ras-Raf-MEK-ERK通路中重 …
Regulated SUMOylation and Ubiquitination of DdMEK1 Is …
We identified the MEK1-interacting protein MIP1 and present genetic and biochemical evidence that MIP1 functions as a MEK1-specific E3 ubiquitin ligase and controls MEK1's nuclear …
Activation of MEK1 or MEK2 isoform is sufficient to fully transform ...
2008年11月17日 · In this study, we show that constitutive activation of MEK1 or MEK2 isoform, as observed in 44% of colorectal cancers, is sufficient to fully transform normal intestinal epithelial …