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Cardiac Monitoring for Patients Undergoing Treatment With MEK Inhibitor Monotherapy. [PDF]
Curr Oncol RepMenteer J +5 more
europepmc +1 more source
Encorafenib‐associated acantholytic dermatosis in collision with eccrine squamous syringometaplasia
JDDG: Journal der Deutschen Dermatologischen Gesellschaft, EarlyView.
Francisco Meraz‐Torres +5 more
wiley +1 more source
Allosteric MEK Inhibitors Act on BRAF/MEK Complexes to Block MEK Activation
Proceedings of the National Academy of Sciences of the United States of America, 2021 Significance Drugs that inhibit specific kinases now represent one of the main classes of targeted therapies. A majority of drug development efforts in this space focus on a given kinase in isolation as the target. However, our work demonstrates that in the context of the RAF/MEK/ERK pathway, the relevant target for compounds ...
Eunyoung Park +2 more
exaly +5 more sources
Cancer Cell, 2014 MEK inhibitors are clinically active in BRAFV600E melanomas but only marginally so in KRAS mutant tumors. Here, we found that MEK inhibitors suppress ERK signaling more potently in BRAFV600E, than in KRAS mutant tumors.
Michael Saborowski +2 more
exaly +2 more sources
Current Development Status of MEK Inhibitors
Molecules, 2017 The current development status of mitogen-activated protein kinase kinase (MEK) inhibitors, including the preclinical data and clinical study progress, has been summarized in this review.
Hongqi Tian, Ying Cheng
exaly +2 more sources
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Current Opinion in Oncology, 2020
Purpose of review An early understanding of the role of the Ras/Raf/MEK/ERK signalling pathway in regulating cell proliferation has set the stage for the development of several potent and selective MEK inhibitors (MEKi). MEKi represent promising therapies for RAS-driven neoplasias and RASopathies associated with increased Ras ...
Christina, Bergqvist +1 more
openaire +2 more sources
Purpose of review An early understanding of the role of the Ras/Raf/MEK/ERK signalling pathway in regulating cell proliferation has set the stage for the development of several potent and selective MEK inhibitors (MEKi). MEKi represent promising therapies for RAS-driven neoplasias and RASopathies associated with increased Ras ...
Christina, Bergqvist +1 more
openaire +2 more sources
Pyrrolopyridazine MEK inhibitors
Bioorganic & Medicinal Chemistry Letters, 2006The synthesis and SAR of a series of pyrrolopyridazine MEK inhibitors are reported. Optimal activity was achieved by incorporation of a 4-phenoxyaniline substituent at C4 and an acylated amine at C6.
Zhong, Chen +12 more
openaire +2 more sources
Bioorganic and Medicinal Chemistry Letters, 2009
An approach and preliminary results for utilizing legacy MEK inhibitors as templates for a reiterative structural based design and synthesis of novel, type III NCKIs (non-classical kinase inhibitors) is described. Evidence is provided that the MEK-pocket or pockets closely related to it may exist in kinases other than MEK.
Jeff Ohren
exaly +3 more sources
An approach and preliminary results for utilizing legacy MEK inhibitors as templates for a reiterative structural based design and synthesis of novel, type III NCKIs (non-classical kinase inhibitors) is described. Evidence is provided that the MEK-pocket or pockets closely related to it may exist in kinases other than MEK.
Jeff Ohren
exaly +3 more sources
Science's STKE, 2001
The Ras-Raf-MEK [(mitogen-activated protein kinase (MAPK) or extracellular signal-regulated kinase (ERK) kinase]-MAPK signaling pathway controls the activation of many cellular functions. Recent reports of Raf-1-deficient mice have indicated that MEK may not be an important downstream substrate for Raf-1 and that, in fact, Raf-1 is important for ...
M S, Murakami, D K, Morrison
openaire +2 more sources
The Ras-Raf-MEK [(mitogen-activated protein kinase (MAPK) or extracellular signal-regulated kinase (ERK) kinase]-MAPK signaling pathway controls the activation of many cellular functions. Recent reports of Raf-1-deficient mice have indicated that MEK may not be an important downstream substrate for Raf-1 and that, in fact, Raf-1 is important for ...
M S, Murakami, D K, Morrison
openaire +2 more sources
MEK in cancer and cancer therapy
Pharmacology & Therapeutics, 2014The mitogen-activated extracellular signal-regulated kinase (MEK) pathway is one of the best-characterized kinase cascades in cancer cell biology. It is triggered by either growth factors or activating mutations of major oncogenic proteins in this pathway, the most common being Ras and Raf.
Cindy, Neuzillet +5 more
openaire +2 more sources