A comprehensive review on MAPK: a promising therapeutic target in cancer

C Braicu, M Buse, C Busuioc, R Drula, D Gulei… - Cancers, 2019 - mdpi.com
The mitogen-activated protein kinase (MAPK) pathway is an important bridge in the switch
from extracellular signals to intracellular responses. Alterations of signaling cascades are …

[HTML][HTML] Structural basis for the non-catalytic functions of protein kinases

JE Kung, N Jura - Structure, 2016 - cell.com
Protein kinases are known primarily for their ability to phosphorylate protein substrates,
which constitutes an essential biological process. Recently, compelling evidence has …

Small molecule inhibition of ERK dimerization prevents tumorigenesis by RAS-ERK pathway oncogenes

A Herrero, A Pinto, P Colón-Bolea, B Casar, M Jones… - Cancer cell, 2015 - cell.com
Nearly 50% of human malignancies exhibit unregulated RAS-ERK signaling; inhibiting it is a
valid strategy for antineoplastic intervention. Upon activation, ERK dimerize, which is …

Sulforaphane suppresses metastasis of triple-negative breast cancer cells by targeting the RAF/MEK/ERK pathway

Y Zhang, Q Lu, N Li, M Xu, T Miyamoto, J Liu - NPJ Breast Cancer, 2022 - nature.com
Breast cancer metastasis is the main cause of cancer death in women, so far, no effective
treatment has inhibited breast cancer metastasis. Sulforaphane (SFN), a natural compound …

RAF kinase dimerization: implications for drug discovery and clinical outcomes

T Brummer, C McInnes - Oncogene, 2020 - nature.com
The RAF kinases activated by RAS GTPases regulate cell growth and division by signal
transduction through the ERK cascade and mutations leading to constitutive activity are key …

Actionability classification of variants of unknown significance correlates with functional effect

A Johnson, PKS Ng, M Kahle, J Castillo… - npj Precision …, 2023 - nature.com
Genomically-informed therapy requires consideration of the functional impact of genomic
alterations on protein expression and/or function. However, a substantial number of variants …

Computational identification of novel stage-specific biomarkers in colorectal cancer progression

A Palaniappan, K Ramar, S Ramalingam - PloS one, 2016 - journals.plos.org
It is well-known that the conversion of normal colon epithelium to adenoma and then to
carcinoma stems from acquired molecular changes in the genome. The genetic basis of …

Analysis of RAS and drug induced homo-and heterodimerization of RAF and KSR1 proteins in living cells using split Nanoluc luciferase

L Rohrer, C Spohr, C Beha, R Griffin, S Braun… - Cell Communication and …, 2023 - Springer
The dimerization of RAF kinases represents a key event in their activation cycle and in
RAS/ERK pathway activation. Genetic, biochemical and structural approaches provided key …

The complexities and versatility of the RAS-to-ERK signalling system in normal and cancer cells

D Fey, D Matallanas, J Rauch, OS Rukhlenko… - Seminars in cell & …, 2016 - Elsevier
The intricate dynamic control and plasticity of RAS to ERK mitogenic, survival and apoptotic
signalling has mystified researches for more than 30 years. Therapeutics targeting the …

ARAF protein kinase activates RAS by antagonizing its binding to RASGAP NF1

W Su, R Mukherjee, R Yaeger, J Son, J Xu, N Na… - Molecular cell, 2022 - cell.com
RAF protein kinases are effectors of the GTP-bound form of small guanosine triphosphatase
RAS and function by phosphorylating MEK. We showed here that the expression of ARAF …