BRAF kinase inhibitors for treatment of melanoma: developments from early-stage animal studies to Phase II clinical trials

T Fujimura, T Hidaka, Y Kambayashi… - Expert Opinion on …, 2019 - Taylor & Francis
ABSTRACT Introduction: Approximately, 30.4–66.0% of cutaneous melanomas possess a
mutation in the BRAF gene that activates downstream signaling through the mitogen …

Current insights of BRAF inhibitors in cancer: miniperspective

B Agianian, E Gavathiotis - Journal of Medicinal Chemistry, 2018 - ACS Publications
Oncogenic BRAF kinase deregulates the ERK signaling pathway in a large number of
human tumors. FDA-approved BRAF inhibitors for BRAFV600E/K tumors have provided …

Mechanism and inhibition of BRAF kinase

A Gunderwala, N Cope, Z Wang - Current opinion in chemical biology, 2022 - Elsevier
The role of BRAF in tumor initiation has been established, however, the precise mechanism
of autoinhibition has only been illustrated recently by several structural studies. These …

Tumor necrosis factor-α blocks apoptosis in melanoma cells when BRAF signaling is inhibited

VC Gray-Schopfer, M Karasarides, R Hayward… - Cancer research, 2007 - AACR
The protein kinase BRAF, a component of the RAS/RAF/mitogen-activated protein
kinase/extracellular signal-regulated kinase (ERK) kinase (MEK)/ERK signaling pathway …

[HTML][HTML] Emerging BRAF Mutations in Cancer Progression and Their Possible Effects on Transcriptional Networks

M Śmiech, P Leszczyński, H Kono, C Wardell… - Genes, 2020 - mdpi.com
Gene mutations can induce cellular alteration and malignant transformation. Development of
many types of cancer is associated with mutations in the B-raf proto-oncogene (BRAF) gene …

[HTML][HTML] Mutations in the Serine/Threonine Kinase BRAF: Oncogenic Drivers in Solid Tumors

P Roa, NV Bremer, V Foglizzo, E Cocco - Cancers, 2024 - mdpi.com
Simple Summary In this literature review, we explore the milestone events from the
discovery of BRAF mutations to present-day clinical intervention strategies. We delve into …

BRAF mutation and its inhibitors in sarcoma treatment

H Liu, N Nazmun, S Hassan, X Liu, J Yang - Cancer Medicine, 2020 - Wiley Online Library
The mitogen‐activated protein kinase (MAPK) signaling pathway plays a significant role in
mediating cellular physiological activities, such as proliferation, differentiation, apoptosis …

BRAF inhibitors induce metastasis in RAS mutant or inhibitor-resistant melanoma cells by reactivating MEK and ERK signaling

B Sanchez-Laorden, A Viros, MR Girotti… - Science …, 2014 - science.org
Melanoma is a highly metastatic and lethal form of skin cancer. The protein kinase BRAF is
mutated in about 40% of melanomas, and BRAF inhibitors improve progression-free and …

Targeting oncogenic Raf protein-serine/threonine kinases in human cancers

R Roskoski Jr - Pharmacological Research, 2018 - Elsevier
Abstract The Ras-Raf-MEK-ERK signal transduction cascade is arguably the most important
oncogenic pathway in human cancers. Ras-GTP promotes the formation of active …

BRAF, a target in melanoma: implications for solid tumor drug development

KT Flaherty, G McArthur - Cancer, 2010 - Wiley Online Library
The successful translation of therapies targeting signal‐transduction pathways that are
activated by oncogenes has provided a model for molecularly targeted therapy, and the …