Targeting RAF kinases for cancer therapy: BRAF-mutated melanoma and beyond

M Holderfield, MM Deuker, F McCormick… - Nature Reviews …, 2014 - nature.com
The identification of mutationally activated BRAF in many cancers altered our conception of
the part played by the RAF family of protein kinases in oncogenesis. In this Review, we …

Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma

C Montagut, SV Sharma, T Shioda, U McDermott… - Cancer research, 2008 - AACR
Activating BRAF kinase mutations arise in∼ 7% of all human tumors, and preclinical studies
have validated the RAF–mitogen-activated protein/extracellular signal-regulated kinase …

Therapeutic strategies for inhibiting oncogenic BRAF signaling

E Halilovic, DB Solit - Current opinion in pharmacology, 2008 - Elsevier
Mitogen-activated protein kinase (MAPK) activation is a common property of human cancers
and is often due to activating mutations in the BRAF and RAS genes. BRAF kinase domain …

Raf kinases in cancer–roles and therapeutic opportunities

G Maurer, B Tarkowski, M Baccarini - Oncogene, 2011 - nature.com
Raf are conserved, ubiquitous serine/protein kinases discovered as the cellular elements
hijacked by transforming retroviruses. The three mammalian RAF proteins (A, B and CRAF) …

Classifying BRAF alterations in cancer: new rational therapeutic strategies for actionable mutations

M Dankner, AAN Rose, S Rajkumar, PM Siegel… - Oncogene, 2018 - nature.com
Abstract The RAS–RAF–MEK–ERK signaling cascade is among the most frequently mutated
pathways in human cancer. Approximately 50% of melanoma patients possess a druggable …

New perspectives for targeting RAF kinase in human cancer

Z Karoulia, E Gavathiotis, PI Poulikakos - Nature Reviews Cancer, 2017 - nature.com
The discovery that a subset of human tumours is dependent on mutationally deregulated
BRAF kinase intensified the development of RAF inhibitors to be used as potential …

BRAF mutations in melanoma: biological aspects, therapeutic implications, and circulating biomarkers

G Castellani, M Buccarelli, MB Arasi, S Rossi… - Cancers, 2023 - mdpi.com
Simple Summary Cutaneous melanoma represents the most aggressive form of skin cancer
and its occurrence, development, and progression are based on the accumulation of several …

[HTML][HTML] Overcoming resistance to BRAF inhibitors

I Arozarena, C Wellbrock - Annals of translational medicine, 2017 - ncbi.nlm.nih.gov
The discovery of activating mutations in the serine/threonine (S/T) kinase BRAF followed by
a wave of follow-up research manifested that the MAPK-pathway plays a critical role in …

BRAF as therapeutic target in melanoma

C Wellbrock, A Hurlstone - Biochemical pharmacology, 2010 - Elsevier
BRAF is a member of the RAF kinase family, which acts in the ERK/MAP kinase pathway, a
signalling cascade that regulates cellular proliferation, differentiation and survival. Single …

Tumor adaptation and resistance to RAF inhibitors

P Lito, N Rosen, DB Solit - Nature medicine, 2013 - nature.com
RAF kinase inhibitors have substantial therapeutic effects in patients with BRAF-mutant
melanoma. However, only rarely do tumors regress completely, and the therapeutic effects …