Results 51 to 60 of about 82,604 (202)

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

Allosteric coupling asymmetry mediates paradoxical activation of BRAF by type II inhibitors

eLife
The type II class of RAF inhibitors currently in clinical trials paradoxically activate BRAF at subsaturating concentrations. Activation is mediated by induction of BRAF dimers, but why activation rather than inhibition occurs remains unclear.
Damien M Rasmussen, Manny M Semonis, Joseph T Greene, Joseph M Muretta, Andrew R Thompson, Silvia Toledo Ramos, David D Thomas, William CK Pomerantz, Tanya S Freedman, Nicholas M Levinson   +9 more
doaj   +1 more source

A case of new-onset vitiligo in a patient on tofacitinib and brief review of paradoxical presentations with other novel targeted therapies [PDF]

, 2020
With recent advancements in the understanding of vitiligo pathogenesis, Janus kinase (JAK) inhibitors have emerged as a promising new treatment modality, but their effects remain incompletely elucidated.
Alikhan, Mujahed, Jogi, Reena, Nguyen, Julie K, Patel, Anisha B, Schlichte, Megan J   +4 more
core  

BRAF Inhibitors for BRAF V600E Mutant Colorectal Cancers: Literature Survey and Case Report

Case Reports in Surgery, 2018
The main method of fighting against colon cancer is targeted treatment. BRAF inhibitors, which are accepted as standard treatment for V600E mutant malign melanomas, are the newest approach for targeted treatment of V600E mutant colorectal cancers.
Yasar Subutay Peker, Mehmet Fatih Can, Ismail Hakki Ozerhan, Gokhan Yagci, Nazif Zeybek, Kutan Kavakli, Sedat Gurkok, Alper Gozubuyuk, Onur Genc, Gokhan Erdem, Ahmet Ozet, Mustafa Gerek, Yusuf Peker   +12 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

Anaplastic Thyroid Carcinoma Histologically Mimicking a Plasmacytoma. [PDF]

, 2020
Anaplastic (undifferentiated) thyroid carcinoma (ATC) is a rare malignancy which may arise from transformation of a pre-existing differentiated carcinoma. We report the unique case where a lesion of thyroid origin presented with the histological features
Mo, Joshua H, Tan, Donald, Tjoa, Tjoson, Wang, Beverly Y, Zhao, Xiaohui S   +4 more
core   +1 more source

Clinical and economic analysis of treatment sequences with prolgolimab and BRAF/MEK inhibitors in adult patients with metastatic or unresectable cutaneous melanoma

Фармакоэкономика
Objective: evaluation of the comparative pharmacoeconomic effectiveness of treatment sequences with prolgolimab as the first line and combination therapy with BRAF/MEK inhibitors as the second line versus a regimen with BRAF/MEK inhibitors as the first ...
S. K. Zyryanov, K. V. Orlova
doaj   +1 more source

Concurrent MEK2 Mutation and BRAF Amplification Confer Resistance to BRAF and MEK Inhibitors in Melanoma

Cell Reports, 2013
Although BRAF and MEK inhibitors have proven clinical benefits in melanoma, most patients develop resistance. We report a de novo MEK2-Q60P mutation and BRAF gain in a melanoma from a patient who progressed on the MEK inhibitor trametinib and did not ...
Jessie Villanueva, Jeffrey R. Infante, Clemens Krepler, Patricia Reyes-Uribe, Minu Samanta, Hsin-Yi Chen, Bin Li, Rolf K. Swoboda, Melissa Wilson, Adina Vultur, Mizuho Fukunaba-Kalabis, Bradley Wubbenhorst, Thomas Y. Chen, Qin Liu, Katrin Sproesser, Douglas J. DeMarini, Tona M. Gilmer, Anne-Marie Martin, Ronen Marmorstein, David C. Schultz, David W. Speicher, Giorgos C. Karakousis, Wei Xu, Ravi K. Amaravadi, Xiaowei Xu, Lynn M. Schuchter, Meenhard Herlyn, Katherine L. Nathanson   +27 more
doaj   +1 more source

Response and Resistance to Paradox-Breaking BRAF Inhibitor in Melanomas [PDF]

, 2018
FDA-approved BRAF inhibitors produce high response rates and improve overall survival in patients with BRAF V600E/K-mutant melanoma, but are linked to pathologies associated with paradoxical ERK1/2 activation in wild-type BRAF cells.
Aplin, Andrew E., Berger, Adam C., Bollag, Gideon, Davies, Michael A., Goldberg, Allison F., Hartsough, Edward J., Knudsen, Karen E., Kugel, Curtis H., Purwin, Timothy J., Schiewer, Matthew J., Vido, Michael J.   +10 more
core   +1 more source

BRAF- and MEK-targeted small molecule inhibitors exert enhanced antimelanoma effects in combination with oncolytic reovirus through ER stress [PDF]

, 2015
Reovirus type 3 (Dearing) (RT3D) infection is selective for cells harboring a mutated/activated RAS pathway. Therefore, in a panel of melanoma cell lines (including RAS mutant, BRAF mutant and RAS/BRAF wild-type), we assessed therapeutic combinations ...
Aadil A Khan, Adel Jebar, Alan Melcher, Bollag, Boyce, Carew, Chandra, Chapman, Comins, da Rocha Dias, David Mansfield, Davies, Dhomen, Eleni Karapanagiotou, Fiona Errington-Mais, Flaherty, Flaherty, Galanis, Gollamudi, Grainne McEntee, Hardev Pandha, Heidorn, Heinemann, Hu, Jiang, Jiang, Joan Kyula, Karapanagiotou, Kelly, Kevin J Harrington, Kyula, Lolkema, Malin Pedersen, Mandarà, Marciniak, Martin McLaughlin, Matt Coffey, McArthur, Michelle Wilkinson, Pandha, Richard Marais, Richard Vile, Roulstone, Sei, Sosman, Strong, Tabas, Tay, Tsaytler, Twigger, Victoria Roulstone, Vidal, Young   +52 more
core   +1 more source