[HTML][HTML] Synergistic anticancer effect by targeting CDK2 and EGFR–ERK signaling

J Wu, Y Chen, R Li, Y Guan, M Chen, H Yin… - Journal of Cell …, 2024 - rupress.org
The EGFR-RAS-ERK pathway is one of the most important signaling cascades in cell
survival, growth, and proliferation. Aberrant activation of this pathway is a common …

EGCG sensitizes chemotherapeutic-induced cytotoxicity by targeting the ERK pathway in multiple cancer cell lines

R Wei, J Wirkus, Z Yang, J Machuca, Y Esparza… - Archives of biochemistry …, 2020 - Elsevier
Abstract Epigallocatechin-3-gallate (EGCG), a major polyphenol component of green tea,
presents anticancer efficacy. However, its exact mechanism of action is not known. In this …

[HTML][HTML] ERK pathway agonism for cancer therapy: evidence, insights, and a target discovery framework

O Timofeev, P Giron, S Lawo, M Pichler… - NPJ Precision …, 2024 - nature.com
At least 40% of human cancers are associated with aberrant ERK pathway activity (ERKp).
Inhibitors targeting various effectors within the ERKp have been developed and explored for …

Discovery of a novel dual-target inhibitor of ERK1 and ERK5 that induces regulated cell death to overcome compensatory mechanism in specific tumor types

G Wang, Y Zhao, Y Liu, D Sun, Y Zhen… - Journal of Medicinal …, 2020 - ACS Publications
ERK1 and ERK5 are proposed to have pivotal roles in several types of cancer. Under some
circumstance, ERK5 may provide a common bypass route, which rescues proliferation upon …

Efficacy of a covalent ERK1/2 inhibitor, CC-90003, in KRAS-mutant cancer models reveals novel mechanisms of response and resistance

I Aronchik, Y Dai, M Labenski, C Barnes, T Jones… - Molecular Cancer …, 2019 - AACR
As a critical signaling node, ERK1/2 are attractive drug targets, particularly in tumors driven
by activation of the MAPK pathway. Utility of targeting the MAPK pathway has been …

[HTML][HTML] FBXW7-mediated ERK3 degradation regulates the proliferation of lung cancer cells

HJ An, CJ Lee, GE Lee, Y Choi, D Jeung… - … & Molecular Medicine, 2022 - nature.com
Extracellular signal-regulated kinase 3 (ERK3) is an atypical member of the mitogen-
activated protein kinase (MAPK) family, members of which play essential roles in diverse …

Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways

W Xia, RJ Mullin, BR Keith, LH Liu, H Ma, DW Rusnak… - Oncogene, 2002 - nature.com
Dual EGFR/erbB2 inhibition is an attractive therapeutic strategy for epithelial tumors, as
ligand-induced erbB2/EGFR heterodimerization triggers potent proliferative and survival …

[HTML][HTML] Targeting ERK, an Achilles' Heel of the MAPK pathway, in cancer therapy

F Liu, X Yang, M Geng, M Huang - Acta pharmaceutica sinica B, 2018 - Elsevier
The mitogen-activated protein kinases (MAPK) pathway, often known as the RAS-RAF-MEK-
ERK signal cascade, functions to transmit upstream signals to its downstream effectors to …

Design of a dual ERK5 kinase activation and autophosphorylation inhibitor to block cancer stem cell activity

SR Kedika, SP Shukla, DG Udugamasooriya - Bioorganic & Medicinal …, 2020 - Elsevier
The importance of ERK5 kinase signaling in tumorigenicity, metastasis, and drug resistance
of cancer stem cells (CSCs) has been recognized recently, and we report a unique dual …

[HTML][HTML] SUV420H1 enhances the phosphorylation and transcription of ERK1 in cancer cells

T Vougiouklakis, K Sone, V Saloura, HS Cho… - Oncotarget, 2015 - ncbi.nlm.nih.gov
The oncogenic protein ERK, a member of the extracellular signal-regulated kinase (ERK)
cascade, is a well characterized signaling molecule involved in tumorigenesis. The ERK …