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   Articles with "mek1" as a keyword



Caspase 3‐specific cleavage of MEK1 suppresses ERK signaling and sensitizes cells to stress‐induced apoptosis

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recommendations! Published in 2023 at "FEBS Open Bio"

DOI: 10.1002/2211-5463.13574

Abstract: Proper regulation of apoptotic cell death is crucial for normal development and homeostasis in multicellular organisms and is achieved by the balance between pro‐apoptotic processes, such as caspase activation, and pro‐survival signaling, such as extracellular… read more here.

Keywords: apoptosis; stress induced; erk; mek1 ... See more keywords

Phase II study of selumetinib, an orally active inhibitor of MEK1 and MEK2 kinases, in KRASG12R-mutant pancreatic ductal adenocarcinoma

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recommendations! Published in 2021 at "Investigational New Drugs"

DOI: 10.1007/s10637-020-01044-8

Abstract: Background Preclinical evidence has suggested that a subset of pancreatic cancers with the G12R mutational isoform of the KRAS oncogene is more sensitive to MAPK pathway blockade than pancreatic tumors with other KRAS isoforms. We… read more here.

Keywords: inhibitor; orally active; study; selumetinib orally ... See more keywords

Analysis of the ERK Pathway Cysteinome for Targeted Covalent Inhibition of RAF and MEK Kinases

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recommendations! Published in 2023 at "Journal of chemical information and modeling"

DOI: 10.1021/acs.jcim.3c00014

Abstract: The ERK pathway is one of the most important signaling cascades involved in tumorigenesis. So far, eight noncovalent inhibitors of RAF and MEK kinases in the ERK pathway have been approved by the FDA for… read more here.

Keywords: erk pathway; raf mek; analysis; covalent ... See more keywords

Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.

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recommendations! Published in 2022 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.1c02192

Abstract: Mutations in MEK1/2 have been described as a resistance mechanism to BRAF/MEK inhibitor treatment. We report the discovery of a novel ATP-competitive MEK1/2 inhibitor with efficacy in wildtype (WT) and mutant MEK12 models. Starting from… read more here.

Keywords: selective mek1; inhibitor; mek1 inhibitor; atp competitive ... See more keywords

Discovery of a First-in-class Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Degrader.

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recommendations! Published in 2019 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.9b01528

Abstract: MEK1 and MEK2 (also known as MAP2K1 and MAP2K2) are the "gatekeepers" of the ERK signaling output with redundant roles in controlling ERK activity. Numerous inhibitors targeting MEK1/2 have been developed including three FDA-approved drugs.… read more here.

Keywords: degrader; kinase; discovery first; mek1 ... See more keywords

Discovery of Coumarin-Based MEK1/2 PROTAC Effective in Human Cancer Cells.

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recommendations! Published in 2022 at "ACS medicinal chemistry letters"

DOI: 10.1021/acsmedchemlett.2c00446

Abstract: The RAF/MEK/ERK pathway is a crucial signal path which is closely associated with the proliferation, differentiation, and apoptosis of tumors. MEK1/2 is a key kinase target in the pathway, with ERK1/2 acting as the main… read more here.

Keywords: effective human; protac effective; human cancer; mek1 ... See more keywords

Hyperactive MEK1 Signaling in Cortical GABAergic Neurons Promotes Embryonic Parvalbumin Neuron Loss and Defects in Behavioral Inhibition.

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recommendations! Published in 2021 at "Cerebral cortex"

DOI: 10.1093/cercor/bhaa413

Abstract: Many developmental syndromes have been linked to genetic mutations that cause abnormal ERK/MAPK activity; however, the neuropathological effects of hyperactive signaling are not fully understood. Here, we examined whether hyperactivation of MEK1 modifies the development… read more here.

Keywords: hyperactive mek1; mek1 signaling; neuron; parvalbumin ... See more keywords

P1936Selective inhibition of the Mek1/2-Erk1/2 signalling pathway induces the differentiation of human cardiac pericyte-like cells into contractile vascular smooth muscle cells

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recommendations! Published in 2019 at "European Heart Journal"

DOI: 10.1093/eurheartj/ehz748.0683

Abstract: Arteriogenesis is key for tissue repair but whether myocardial stromal cells contribute to this phenomenon remains unknown. Investigate if cardiac pericytes are a druggable target for therapeutic arteriogenesis. The localization of pericyte-like cells (PCs) was… read more here.

Keywords: pericyte like; like cells; pcs; mek1 erk1 ... See more keywords

An acidic loop in the FHA domain of the yeast meiosis-specific kinase Mek1 interacts with a specific motif in a subset of Mek1 substrates.

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recommendations! Published in 2024 at "Genetics"

DOI: 10.1093/genetics/iyae106

Abstract: The meiosis-specific kinase Mek1 regulates key steps in meiotic recombination in the budding yeast, Saccharomyces cerevisiae. MEK1 limits resection at double strand break (DSB) ends and is required for preferential strand invasion into homologs, a… read more here.

Keywords: meiosis specific; specific kinase; mek1; acidic loop ... See more keywords

Chk2 homologue Mek1 limits Exo1-dependent DNA end resection during meiotic recombination in S. cerevisiae.

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recommendations! Published in 2024 at "Genetics"

DOI: 10.1093/genetics/iyae112

Abstract: The conserved Rad2/XPG family 5'-3' exonuclease, Exonuclease 1 (Exo1), plays many roles in DNA metabolism including during resolution of DNA double strand breaks (DSBs) via homologous recombination. Prior studies provided evidence that the end-resection activity… read more here.

Keywords: chk2 homologue; recombination; resection; end resection ... See more keywords

MEK1/2 inhibition prevents DENV and ZIKV infection via disrupting the cytoskeletal vimentin cage required for viral replication.

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recommendations! Published in 2025 at "Journal of molecular cell biology"

DOI: 10.1093/jmcb/mjaf037

Abstract: Flaviviridae Dengue virus (DENV) and Zika virus (ZIKV) have posed significant threats to global public health in the past decades. Despite extensive study on therapeutic strategies against these viruses, effective treatment options are still lacking.… read more here.

Keywords: replication; viral replication; biology; infection ... See more keywords