A Novel ERK2 Degrader Z734 Induces Apoptosis of MCF–7 Cells via the HERC3/p53 Signaling Pathway

S Xu, Y Xiong, R Yao, R Tian, Z Meng, MY Zaky, B Fu… - Molecules, 2022 - mdpi.com
Breast cancer is one of the leading causes of death worldwide, and synthetic chemicals
targeting specific proteins or various molecular pathways for tumor suppression, such as …

[HTML][HTML] Computational design, chemical synthesis, and biological evaluation of a novel ERK inhibitor (BL-EI001) with apoptosis-inducing mechanisms in breast …

B Liu, L Fu, C Zhang, L Zhang, Y Zhang, L Ouyang… - Oncotarget, 2015 - ncbi.nlm.nih.gov
Abstract Extracellular signal-regulated kinase1/2 (ERK1/2) plays a crucial role in the
resistance of apoptosis in carcinogenesis; however, its targeted small-molecule inhibitors …

A novel dual EGFR/HER2 inhibitor KU004 induces cell cycle arrest and apoptosis in HER2-overexpressing cancer cells

C Tian, P Ding, Z Yuan, H Li, Y Zhao, L Sun, Q Guo… - Apoptosis, 2015 - Springer
Human epidermal growth factor receptor 2 (HER2) is a validated therapeutic target in cancer
therapy, and HER2 protein-tyrosine kinase inhibitors have attracted considerable attention …

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 …

BAY-885, a mitogen-activated protein kinase kinase 5 inhibitor, induces apoptosis by regulating the endoplasmic reticulum stress/Mcl-1/Bim pathway in breast cancer …

L Wang, X Ji, C Mao, R Yu - Bioengineered, 2022 - Taylor & Francis
The mitogen-activated protein kinase kinase 5 (MEK5)/extracellular signal-regulated kinase
5 (ERK5) axis has been reported to promote tumorigenesis in breast cancer (BC). Therefore …

Structure-Guided Discovery and Preclinical Assessment of Novel (Thiophen-3-yl) aminopyrimidine Derivatives as Potent ERK1/2 Inhibitors

W Shuai, H Xiao, P Yang, Y Zhang, F Bu… - Journal of Medicinal …, 2024 - ACS Publications
The RAS-RAF-MEK-ERK signaling cascade is abnormally activated in various tumors,
playing a crucial role in mediating tumor progression. As the key component at the terminal …

Inhibiting ERK5 Overcomes Breast Cancer Resistance to Anti-HER2 Therapy By Targeting the G1–S Cell-Cycle Transition

J Zhang, AJ Pearson, N Sabherwal, BA Telfer… - Cancer research …, 2022 - AACR
Targeting HER2 has become a landmark in the treatment of HER2-driven breast cancer.
Nonetheless, the clinical efficacy of anti-HER2 therapies can be short-lived and a significant …

Novel small molecule decreases cell proliferation, migration, clone formation, and gene expression through ERK inhibition in MCF-7 and MDA-MB-231 breast cancer …

E Hatzidaki, P Parsonidis, P Apostolou… - Anti-cancer …, 2019 - journals.lww.com
Abstract The Ras–Raf–MEK1/2–ERK1/2 pathway is an attractive target for the development
of anticancer agents because of the high prevalence of ERK activation in human cancers …

ERK: a double-edged sword in cancer. ERK-dependent apoptosis as a potential therapeutic strategy for cancer

R Sugiura, R Satoh, T Takasaki - Cells, 2021 - mdpi.com
The RAF/MEK/ERK signaling pathway regulates diverse cellular processes as exemplified
by cell proliferation, differentiation, motility, and survival. Activation of ERK1/2 generally …

[HTML][HTML] Therapeutic potential of ERK5 targeting in triple negative breast cancer

MJ Ortiz-Ruiz, S Álvarez-Fernández, T Parrott… - Oncotarget, 2014 - ncbi.nlm.nih.gov
Triple negative breast cancers (TNBCs) account for 15% of all breast cancers, and represent
one of the most aggressive forms of the disease, exhibiting short relapse-free survival. In …