RAF-MEK-ERK pathway in cancer evolution and treatment

R Ullah, Q Yin, AH Snell, L Wan - Seminars in cancer biology, 2022 - Elsevier
Abstract The RAF-MEK-ERK signaling cascade is a well-characterized MAPK pathway
involved in cell proliferation and survival. The three-layered MAPK signaling cascade is …

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 …

[HTML][HTML] Global characterization of macrophage polarization mechanisms and identification of M2-type polarization inhibitors

L He, JH Jhong, Q Chen, KY Huang, K Strittmatter… - Cell reports, 2021 - cell.com
Macrophages undergoing M1-versus M2-type polarization differ significantly in their cell
metabolism and cellular functions. Here, global quantitative time-course proteomics and …

[HTML][HTML] Perturbation-response genes reveal signaling footprints in cancer gene expression

M Schubert, B Klinger, M Klünemann, A Sieber… - Nature …, 2018 - nature.com
Aberrant cell signaling can cause cancer and other diseases and is a focal point of drug
research. A common approach is to infer signaling activity of pathways from gene …

Anti-cancer chalcones: Structural and molecular target perspectives

DK Mahapatra, SK Bharti, V Asati - European journal of medicinal chemistry, 2015 - Elsevier
Abstract Chalcone or (E)-1, 3-diphenyl-2-propene-1-one scaffold remained a fascination
among researchers in the 21st century due to its simple chemistry, ease of synthesis and a …

The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma

EM Van Allen, N Wagle, A Sucker, DJ Treacy… - Cancer discovery, 2014 - AACR
Most patients with BRAF V600-mutant metastatic melanoma develop resistance to selective
RAF kinase inhibitors. The spectrum of clinical genetic resistance mechanisms to RAF …

[HTML][HTML] Targeting cancer with kinase inhibitors

S Gross, R Rahal, N Stransky… - The Journal of …, 2015 - Am Soc Clin Investig
Kinase inhibitors have played an increasingly prominent role in the treatment of cancer and
other diseases. Currently, more than 25 oncology drugs that target kinases have been …

Targeting the MAPK–RAS–RAF signaling pathway in cancer therapy

L Santarpia, SM Lippman… - Expert opinion on …, 2012 - Taylor & Francis
Introduction: The MAPK pathway comprises several key signaling components and
phosphorylation events that play a role in tumorigenesis. These activated kinases transmit …

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

CM Johannessen, JS Boehm, SY Kim, SR Thomas… - Nature, 2010 - nature.com
Oncogenic mutations in the serine/threonine kinase B-RAF (also known as BRAF) are found
in 50–70% of malignant melanomas. Pre-clinical studies have demonstrated that the B-RAF …

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

PI Poulikakos, C Zhang, G Bollag, KM Shokat, N Rosen - Nature, 2010 - nature.com
Tumours with mutant BRAF are dependent on the RAF–MEK–ERK signalling pathway for
their growth,,. We found that ATP-competitive RAF inhibitors inhibit ERK signalling in cells …