Results 21 to 30 of about 78,382 (206)

Trametinib with or without vemurafenib in BRAF mutated non-small cell lung cancer.

PLoS ONE, 2015
V-Raf Murine Sarcoma Viral Oncogene Homolog B (BRAF) mutated lung cancer is relatively aggressive and is resistant to currently available therapies. In a recent phase II study for patients with BRAF-V600E non-small cell lung cancer (NSCLC), BRAF V600E ...
Monika Joshi, Shawn J Rice, Xin Liu, Bruce Miller, Chandra P Belani   +4 more
doaj   +1 more source

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

Biological challenges of BRAF inhibitor therapy [PDF]

Molecular Oncology, 2011
Activating mutations in BRAF, a constituent of the map kinase pathway, were first discovered as being most prevalent in melanoma in 2002. Only recently have potent and selective, orally available inhibitors of BRAF emerged for clinical testing and demonstrated clear evidence of tumor regression in the majority of patients whose tumors harbor a BRAF ...
Igor, Puzanov, Patrick, Burnett, Keith T, Flaherty   +2 more
openaire   +2 more sources

BRAF Inhibitors in BRAF-Mutated Colorectal Cancer: A Systematic Review

Journal of Clinical Medicine, 2023
Colorectal cancer (CRC) is the second-leading cause of cancer-related deaths globally. BRAF mutation is present in about 10% of CRC patients and is associated with a poor response to chemotherapy. These patients have a relatively poor prognosis. This review aims to assess the efficacy and safety of BRAF inhibitors in BRAF-mutated CRC patients.
Wajeeha Aiman, Muhammad Ashar Ali, Samer Jumean, Ummul Asfeen, Jose Garcia, Murad Quirem, Amaar Ahmad, Mohammad Nabil Rayad, Osama Alkhlaifat, Bader Al Omour, Venkata S. Chemarthi, Michael Maroules, Gunwant Guron, Hamid Shaaban   +13 more
openaire   +2 more sources

BRAF Inhibitors: Molecular Targeting and Immunomodulatory Actions [PDF]

Cancers, 2020
The BRAF inhibitors vemurafenib, dabrafenib and encorafenib are used in the treatment of patients with BRAF-mutant melanoma. They selectively target BRAF kinase and thus interfere with the mitogen-activated protein kinase (MAPK) signalling pathway that regulates the proliferation and survival of melanoma cells. In addition to their molecularly targeted
Ilaria Proietti, Nevena Skroza, Simone Michelini, Alessandra Mambrin, Veronica Balduzzi, Nicoletta Bernardini, Anna Marchesiello, Ersilia Tolino, Salvatore Volpe, Patrizia Maddalena, Marco Fraia, Giorgio Mangino, Giovanna Romeo, Concetta Potenza   +13 more
openaire   +2 more sources

Discovery of BRAF/HDAC Dual Inhibitors Suppressing Proliferation of Human Colorectal Cancer Cells

Frontiers in Chemistry, 2022
The combination of histone deacetylase inhibitor and BRAF inhibitor (BRAFi) has been shown to enhance the antineoplastic effect and reduce the progress of BRAFi resistance.
Yingjun Li, Yongjun Huang, Huimin Cheng, Fang Xu, Ruxi Qi, Botao Dai, Yujian Yang, Zhengchao Tu, Lijie Peng, Zhang Zhang   +9 more
doaj   +1 more source

Concurrent MEK targeted therapy prevents MAPK pathway reactivation during BRAFV600E targeted inhibition in a novel syngeneic murine glioma model. [PDF]

, 2016
Inhibitors of BRAFV600E kinase are currently under investigations in preclinical and clinical studies involving BRAFV600E glioma. Studies demonstrated clinical response to such individualized therapy in the majority of patients whereas in some patients ...
Berger, Mitchel S, Daynac, Mathieu, Grossauer, Stefan, James, C David, Koeck, Katharina, McMahon, Martin, Meyers, Ian D, Murphy, Nicole E, Nicolaides, Theodore P, Petritsch, Claudia K, Phillips, Joanna J, Truffaux, Nathalene, Truong, Albert Y   +12 more
core   +1 more source

Beneficial effects of vemurafenib on craniopharyngioma carrying BRAF-V600E mutation [PDF]

Jichu yixue yu linchuang
Objective To evaluate the efficacy and adverse reactions of BRAF inhibitor vermorafenib on the treatment of refractory craniopharyngioma carrying BRAF-V600E mutation.
WANG Xi, YE Ting, NIE Min, WU Xueyan, MAO Jiangfeng
doaj   +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

Inhibitors of BRAF dimers using an allosteric site

Nature Communications, 2020
FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which limits their clinical efficacy in tumors expressing BRAFV600E mutant monomers. Here the authors identify FDA-approved Ponatinib as an effective inhibitor of BRAF monomers and dimers and ...
Xiomaris M. Cotto-Rios, Bogos Agianian, Nadege Gitego, Emmanouil Zacharioudakis, Orsi Giricz, Yang Wu, Yiyu Zou, Amit Verma, Poulikos I. Poulikakos, Evripidis Gavathiotis   +9 more
doaj   +1 more source