Targeting the RAS/RAF/MAPK pathway for cancer therapy: from mechanism to clinical studies

ME Bahar, HJ Kim, DR Kim - Signal transduction and targeted therapy, 2023 - nature.com
Metastatic dissemination of solid tumors, a leading cause of cancer-related mortality,
underscores the urgent need for enhanced insights into the molecular and cellular …

Molecular pathways and mechanisms of BRAF in cancer therapy

PI Poulikakos, RJ Sullivan, R Yaeger - Clinical Cancer Research, 2022 - AACR
With the identification of activating mutations in BRAF across a wide variety of malignancies,
substantial effort was placed in designing safe and effective therapeutic strategies to target …

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 …

Clinical activity of mitogen-activated protein kinase–targeted therapies in patients with non–V600 BRAF-mutant tumors

M Dankner, Y Wang, R Fazelzad, B Johnson… - JCO Precision …, 2022 - ascopubs.org
PURPOSE Non-V600 mutations comprise approximately 35% of all BRAF mutations in
cancer. Many of these mutations have been identified as oncogenic drivers and can be …

BRAFΔβ3-αC in-frame deletion mutants differ in their dimerization propensity, HSP90 dependence, and druggability

M Lauinger, D Christen, RFU Klar, C Roubaty… - Science …, 2023 - science.org
In-frame BRAF exon 12 deletions are increasingly identified in various tumor types. The
resultant BRAFΔβ3-αC oncoproteins usually lack five amino acids in the β3-αC helix linker …

Challenges and Opportunities in the Crusade of BRAF Inhibitors: From 2002 to 2022

AK Singh, P Sonawane, A Kumar, H Singh… - ACS …, 2023 - ACS Publications
Serine/threonine-protein kinase B-Raf (BRAF; RAF= rapidly accelerated fibrosarcoma) plays
an important role in the mitogen-activated protein kinase (MAPK) signaling cascade …

Cell-specific models reveal conformation-specific RAF inhibitor combinations that synergistically inhibit ERK signaling in pancreatic cancer cells

T Sevrin, H Imoto, S Robertson, N Rauch, U Dyn'ko… - Cell reports, 2024 - cell.com
Pancreatic ductal adenocarcinoma (PDAC) presents significant challenges for targeted
clinical interventions due to prevalent KRAS mutations, rendering PDAC resistant to RAF …

New prospectives on treatment opportunities in RASopathies

BD Gelb, ME Yohe, C Wolf… - American Journal of …, 2022 - Wiley Online Library
The RASopathies are a group of clinically defined developmental syndromes caused by
germline variants of the RAS/mitogen‐activated protein (MAPK) cascade. The prototypic …

Inhibition of the RAF/MEK/ERK signaling cascade in pancreatic cancer: recent advances and future perspectives

C Adamopoulos, DD Cave… - International Journal of …, 2024 - mdpi.com
Pancreatic cancer represents a formidable challenge in oncology, primarily due to its
aggressive nature and limited therapeutic options. The prognosis of patients with pancreatic …

Dual inhibition of BRAF-MAPK and STAT3 signaling pathways in resveratrol-suppressed anaplastic thyroid cancer cells with BRAF mutations

MD Lu, H Li, JH Nie, S Li, HS Ye, TT Li, ML Wu… - International Journal of …, 2022 - mdpi.com
Anaplastic thyroid cancer is an extremely lethal malignancy without reliable treatment.
BRAFV600E point mutation is common in ATCs, which leads to MAPK signaling activation …