Results 261 to 270 of about 130,782 (308)

Pyrrolopyridazine MEK inhibitors

Bioorganic & Medicinal Chemistry Letters, 2006
The 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, Soong-Hoon, Kim, Stephanie A, Barbosa, Tram, Huynh, David R, Tortolani, Kenneth J, Leavitt, Donna D, Wei, Veeraswamy, Manne, Carolyn S, Ricca, Johnni, Gullo-Brown, Michael A, Poss, Wayne, Vaccaro, Mark E, Salvati   +12 more
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MEK inhibitors in RASopathies

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, Pierre, Wolkenstein   +1 more
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Shipping Out MEK Inhibitor Resistance with SHP2 Inhibitors

Cancer Discovery, 2018
Abstract Summary: RAS is one of the most frequently altered oncogenes, yet RAS-driven tumors are largely refractory to anticancer therapies. Fedele and colleagues demonstrate that SHP2 inhibitors prevent adaptive MEK inhibitor resistance; therefore, combining MEK and SHP2 inhibitors represents an exciting new therapeutic approach for the
Pedro Torres-Ayuso, John Brognard
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[BRAF-MEK inhibitor therapy in melanoma].

Magyar onkologia, 2022
We investigated the efficacy and safety of vemurafenib+cobimetinib (V+C) and dabrafenib+trametinib (D+T) based on real-life data. From 2015 and 2018 we have selected 118 BRAF-mutated metastatic melanoma patients, treated with V+C and D+T in our institute.
Kata, Czirbesz, Gitta, Pánczél, Fanni, Baranyai, Mihály, Kispál, Erika, Tóth, Katalin, Bőcs, Tímea, Balatoni, Georgina, Fröhlich, Gabriella, Liszkay   +8 more
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The clinical development of MEK inhibitors

Nature Reviews Clinical Oncology, 2014
Aberrant activation of the RAS-RAF-MEK-ERK1/2 pathway occurs in more than 30% of human cancers. As part of this pathway, MEK1 and MEK2 have crucial roles in tumorigenesis, cell proliferation and inhibition of apoptosis and, therefore, MEK1/2 inhibition is an attractive therapeutic strategy in a number of cancers.
Yujie, Zhao, Alex A, Adjei
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Fused thiophene derivatives as MEK inhibitors

Bioorganic & Medicinal Chemistry Letters, 2012
A number of novel fused thiophene derivatives have been prepared and identified as potent inhibitors of MEK. The SAR data of selected examples and the in vivo profiling of compound 13 h demonstrates the functional activity of this class of compounds in HT-29 PK/PD models.
Victoria E, Laing, Daniel C, Brookings, Rachel J, Carbery, Jose Gascon, Simorte, Martin C, Hutchings, Barry J, Langham, Martin A, Lowe, Rodger A, Allen, Joanne R, Fetterman, James, Turner, Christoph, Meier, Jeff, Kennedy, Mark, Merriman   +12 more
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RAS/RAF/MEK Inhibitors in Oncology

Current Medicinal Chemistry, 2012
The RAS/RAF/MEK signaling pathway plays a central role in mediating both proliferation and survival of cancer cells. These proteins are a group of serine/threonine kinases activated in response to a variety of extracellular stimuli and mediate signal transduction from the cell surface towards both nuclear and cytosolic targets.
P, Rusconi, E, Caiola, M, Broggini
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Severe gastrointestinal toxicity of MEK inhibitors

Melanoma Research, 2019
Gastrointestinal toxicities of MEK inhibitors in melanoma patients are frequent. In clinical trials, the most common digestive adverse events were nausea, vomiting, and diarrhoea. However, severe toxicities such as colitis and gastrointestinal perforation, some with fatal outcomes, have been reported.
Nadim, Mourad, Nelson, Lourenço, Julie, Delyon, Pirayeh, Eftekhari, Philippe, Bertheau, Clara, Allayous, Alice, Ballon, Cécile, Pagès, Matthieu, Allez, Céleste, Lebbé, Barouyr, Baroudjian   +10 more
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Dual RAF–MEK Inhibitor Assessed

Cancer Discovery, 2021
Abstract According to preliminary results from a phase I trial, VS-6766, also known as CH5126766, a first-in-class dual RAF–MEK inhibitor, is safe and has shown some efficacy in solid tumors and multiple myeloma harboring various RAS–RAF mutations.
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OCULAR ADVERSE EVENTS ASSOCIATED WITH MEK INHIBITORS

Retina, 2019
Purpose: Mitogen-activates protein kinase (MAPK) inhibitors, particularly MEK inhibitors, have shifted the treatment paradigm for metastatic BRAF-mutant cutaneous melanoma; however, oncologists, ophthalmologists, and patients have noticed different toxicities of variable importance.
Silvia, Méndez-Martínez, Pilar, Calvo, Oscar, Ruiz-Moreno, Nieves, Pardiñas Barón, Jesús, Leciñena Bueno, María Del Rocío, Gil Ruiz, Luis, Pablo   +6 more
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