[HTML][HTML] Tumor Cell Resistance to the Inhibition of BRAF and MEK1/2

W Chen, JI Park - International Journal of Molecular Sciences, 2023 - mdpi.com
BRAF is one of the most frequently mutated oncogenes, with an overall frequency of about
50%. Targeting BRAF and its effector mitogen-activated protein kinase kinase 1/2 (MEK1/2) …

[HTML][HTML] Targeting oncogenic BRAF: past, present, and future

A Zaman, W Wu, TG Bivona - Cancers, 2019 - mdpi.com
Identifying recurrent somatic genetic alterations of, and dependency on, the kinase BRAF
has enabled a “precision medicine” paradigm to diagnose and treat BRAF-driven tumors …

Defining and targeting BRAF mutations in solid tumors

BR Halle, DB Johnson - Current Treatment Options in Oncology, 2021 - Springer
Opinion Statement BRAF mutations are present in up to 8% of human cancers, and
comprise a viable therapeutic target in many patients harboring these mutations. Specific …

Toxicities from BRAF and MEK Inhibitors: Strategies to Maximize Therapeutic Success

M Wang, RJ Sullivan, MJ Mooradian - Current Oncology Reports, 2024 - Springer
Abstract Purpose of Review This report highlights several of the recent therapeutic
advancements in the treatment of BRAF-mutant tumors, discusses the most common …

Gatekeeper mutations mediate resistance to BRAF-targeted therapies

S Whittaker, R Kirk, R Hayward, A Zambon… - Science translational …, 2010 - science.org
BRAF is a serine-threonine–specific protein kinase that is mutated in 2% of human cancers.
Oncogenic BRAF is a validated therapeutic target that constitutively activates mitogen …

BRAF inhibitor therapy for melanoma, thyroid and colorectal cancers: development of resistance and future prospects

M Atiqur Rahman, A Salajegheh… - Current cancer drug …, 2014 - ingentaconnect.com
BRAF is a major oncoprotein and oncogenic mutations in BRAF are found in a significant
number of cancers, including melanoma, thyroid cancer, colorectal cancer and others …

BRAF—A tumour-agnostic drug target with lineage-specific dependencies

AJ Hanrahan, Z Chen, N Rosen, DB Solit - Nature Reviews Clinical …, 2024 - nature.com
In June 2022, the FDA granted Accelerated Approval to the BRAF inhibitor dabrafenib in
combination with the MEK inhibitor trametinib for the treatment of adult and paediatric …

[HTML][HTML] Potential therapeutic strategies to overcome acquired resistance to BRAF or MEK inhibitors in BRAF mutant cancers

RB Corcoran, J Settleman, JA Engelman - Oncotarget, 2011 - ncbi.nlm.nih.gov
Recent clinical trials with selective inhibitors of the BRAF and MEK kinases have shown
promising results in patients with tumors harboring BRAF V600 mutations. However, as has …

[HTML][HTML] BRAF inhibitors in clinical oncology

V Morris, S Kopetz - F1000prime reports, 2013 - ncbi.nlm.nih.gov
Activating mutations of the BRAF oncogene are present in approximately 5-10% of all
human malignancies and lead to constitutive activation of the mitogen activated protein …

BRAF mutations: signaling, epidemiology, and clinical experience in multiple malignancies

RD Hall, RR Kudchadkar - Cancer Control, 2014 - journals.sagepub.com
Background Mutations in BRAF were first reported in 2002. Since that time, the molecular
basis for oncogenic signaling has been elucidated in multiple malignancies. The …