Results 21 to 30 of about 130,251 (209)

Binimetinib inhibits MEK and is effective against neuroblastoma tumor cells with low NF1 expression. [PDF]

, 2016
BackgroundNovel therapies are needed for children with high-risk and relapsed neuroblastoma. We hypothesized that MAPK/ERK kinase (MEK) inhibition with the novel MEK1/2 inhibitor binimetinib would be effective in neuroblastoma preclinical models ...
Liu, Yin, Scorsone, Kathleen A, Woodfield, Sarah E, Zage, Peter E, Zhang, Linna   +4 more
core   +2 more sources

In vivo E2F reporting reveals efficacious schedules of MEK1/2–CDK4/6 targeting and mTOR–s6 resistance mechanisms [PDF]

, 2018
Targeting cyclin-dependent kinases 4/6 (CDK4/6) represents a therapeutic option in combination with BRAF inhibitor and/or MEK inhibitor (MEKi) in melanoma; however, continuous dosing elicits toxicities in patients. Using quantitative and temporal in vivo
Aplin, Andrew E., Cheng, Phil F., Chervoneva, Inna, Davies, Michael A., Dummer, Reinhard, Ertel, Adam, Fortina, Paolo, Hookim, Kim, Kleiber, Ines, Kwong, Lawrence N., Levesque, Mitch P., Nikbakht, Neda, Patel, Prem, Purwin, Timothy J., Teh, Jessica L. F.   +14 more
core   +1 more source

MEK inhibition suppresses B regulatory cells and augments anti-tumor immunity.

PLoS ONE, 2019
Mitogen-activated protein kinase (MAPK) kinase (MEK) is an integral component of the RAS pathway and a therapeutic target in RAS-driven cancers. Although tumor responses to MEK inhibition are rarely durable, MEK inhibitors have shown substantial activity
Mark Yarchoan, Aditya A Mohan, Lauren Dennison, Teena Vithayathil, Amanda Ruggieri, Gregory B Lesinski, Todd D Armstrong, Nilofer S Azad, Elizabeth M Jaffee   +8 more
doaj   +1 more source

Co-targeting HGF/cMET Signaling with MEK Inhibitors in Metastatic Uveal Melanoma. [PDF]

, 2017
Patients with metastatic uveal melanoma usually die within 1 year of diagnosis, emphasizing an urgent need to develop new treatment strategies. The liver is the most common site of metastasis.
Aplin, Andrew E., Cheng, Hanyin, Chua, Vivian, Davies, Michael A., Kageyama, Ken, Liao, Connie, Purwin, Timothy J., Sato, Takami, Terai, Mizue   +8 more
core   +2 more sources

Combined Treatment with MEK and mTOR Inhibitors is Effective in In Vitro and In Vivo Models of Hepatocellular Carcinoma. [PDF]

, 2019
Background: Hepatocellular carcinoma (HCC) is the most common primary liver cancer histotype, characterized by high biological aggressiveness and scarce treatment options.
Calvisi, Diego F, Che, Li, Chen, Xin, Evert, Matthias, Hu, Junjie, Liu, Xianqiong, Lu, Xinjun, Song, Xinhua, Su, Tao, Utpatel, Kirsten, Wang, Jingxiao, Wang, Pan, Xu, Meng, Zhang, Jie, Zhang, Yi   +14 more
core   +1 more source

A phase I pharmacokinetic and pharmacodynamic study of the oral mitogen-activated protein kinase kinase (MEK) inhibitor, WX-554, in patients with advanced solid tumours [PDF]

, 2016
Purpose: We performed a multi-centre phase I study to assess the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of the orally available small molecule mitogen-activated protein kinase kinase (MEK) 1/2 inhibitor, WX-554, and to determine the ...
Allen, Rodger, Anthoney, Alan, Banerji, Udai, Bevan, Paul, Boddy, Alan V., Buerkle, Markus, Coyle, Vicky, Cresti, Nicola, Dean, Emma, Drew, Yvette, Evans, T.R. Jefferey, Greystoke, Alastair, Griffin, Melanie J., Jamieson, David, Mala, Carola, Merriman, Mark, Plummer, Ruth, Ranson, Malcolm, Rodgers, Lisa, Sludden, Julieann, Swales, Karen, Wilson, Richard H.   +21 more
core   +2 more sources

Combined MEK/MDM2 inhibition demonstrates antitumor efficacy in TP53 wild-type thyroid and colorectal cancers with MAPK alterations

Scientific Reports, 2022
Most tumors with activating MAPK (mitogen-activated protein kinase) pathway alterations respond poorly to MEK inhibitors alone. Here, we evaluated combination therapy with MEK inhibitor selumetinib and MDM2 inhibitor KRT-232 in TP53 wild-type and MAPK ...
Seyed Pairawan, Argun Akcakanat, Scott Kopetz, Coya Tapia, Xiaofeng Zheng, Huiqin Chen, Min Jin Ha, Yasmeen Rizvi, Vijaykumar Holla, Jing Wang, Kurt W. Evans, Ming Zhao, Naifa Busaidy, Bingliang Fang, Jack A. Roth, Ecaterina Ileana Dumbrava, Funda Meric-Bernstam   +16 more
doaj   +1 more source

Combining MEK and SRC inhibitors for treatment of colorectal cancer demonstrate increased efficacy in vitro but not in vivo

PLoS ONE, 2023
Metastatic colorectal cancer (mCRC) is the second leading cause of cancer deaths in the United States. More than 50% of patients with mCRC harbor mutations of the oncogenic driver RAS (KRAS or NRAS).
Fan Fan, Susmita Ghosh, Reid Powell, Jason Roszik, Yongsun Park, Mary Sobieski, Alexey Sorokin, Clifford Stephan, Scott Kopetz, Lee M. Ellis, Rajat Bhattacharya   +10 more
doaj   +2 more sources

Cobimetinib- and vemurafenib-induced granulomatous dermatitis and erythema induratum: A case report

SAGE Open Medical Case Reports, 2019
Metastatic melanoma is an aggressive malignancy. Survival can be increased with the combination of BRAF and MEK inhibition. BRAF inhibitor-induced cutaneous toxicities can be attenuated with MEK inhibition.
Marco AJ Iafolla, Jennifer Ramsay, Judy Wismer, Elaine McWhirter   +3 more
doaj   +1 more source

Crosstalk between PI3 Kinase/PDK1/Akt/Rac1 and Ras/Raf/MEK/ERK Pathways Downstream PDGF Receptor

Cellular Physiology and Biochemistry, 2013
Background/Aims: Our earlier studies suggested crosstalk between IRS/PI3 kinase/PDK1/Akt/Rac1/ROCK and (Shc2/Grb2/SOS)/Ras/Raf/MEK/ERK pathways downstream PDGF-ββ receptor responsible for chemotaxis and proliferation of malignant mesothelioma cells.
Emma Tabe Eko Niba, Hisao Nagaya, Takeshi Kanno, Ayako Tsuchiya, Akinobu Gotoh, Chiharu Tabata, Kohzo Kuribayashi, Takashi Nakano, Tomoyuki Nishizaki   +8 more
doaj   +1 more source