Targeting chromosomal instability in patients with cancer

DH Al-Rawi, E Lettera, J Li, M DiBona… - Nature Reviews Clinical …, 2024 - nature.com
Chromosomal instability (CIN) is a hallmark of cancer and a driver of metastatic
dissemination, therapeutic resistance, and immune evasion. CIN is present in 60–80% of …

[HTML][HTML] Non-cell-autonomous cancer progression from chromosomal instability

J Li, MJ Hubisz, EM Earlie, MA Duran, C Hong… - Nature, 2023 - nature.com
Chromosomal instability (CIN) is a driver of cancer metastasis,,–, yet the extent to which this
effect depends on the immune system remains unknown. Using ContactTracing—a newly …

Phytochemical‐mediated modulation of autophagy and endoplasmic reticulum stress as a cancer therapeutic approach

M Al Azzani, ZN Nizami, R Magramane… - Phytotherapy …, 2024 - Wiley Online Library
Autophagy and endoplasmic reticulum (ER) stress are conserved processes that generally
promote survival, but can induce cell death when physiological thresholds are crossed. The …

PERK inhibition by HC-5404 sensitizes renal cell carcinoma tumor models to antiangiogenic tyrosine kinase inhibitors

ME Stokes, V Calvo, S Fujisawa, C Dudgeon… - Clinical Cancer …, 2023 - AACR
Purpose: Tumors activate protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK,
also called EIF2AK3) in response to hypoxia and nutrient deprivation as a stress-mitigation …

A PERK-Specific Inhibitor Blocks Metastatic Progression by Limiting Integrated Stress Response–Dependent Survival of Quiescent Cancer Cells

V Calvo, W Zheng, A Adam-Artigues, KA Staschke… - Clinical Cancer …, 2023 - AACR
Purpose: The integrated stress response (ISR) kinase PERK serves as a survival factor for
both proliferative and dormant cancer cells. We aim to validate PERK inhibition as a new …

[HTML][HTML] Unfolded protein response at the cross roads of tumourigenesis, oxygen sensing and drug resistance in clear cell renal cell carcinoma

YH Chee, A Samali, CM Robinson - … et Biophysica Acta (BBA)-Reviews on …, 2022 - Elsevier
Clear cell renal cell carcinoma (ccRCC) is the most common form of kidney cancer. Despite
therapeutic advances, long term survival in patients diagnosed with advanced disease is …

[HTML][HTML] Novel small molecule inhibitors targeting renal cell carcinoma: Status, challenges, future directions

L Xiong, Y Zhang, J Wang, M Yu, L Huang… - European Journal of …, 2024 - Elsevier
Renal cell carcinoma (RCC) is the most common renal malignancy with a rapidly increasing
morbidity and mortality rate gradually. RCC has a high mortality rate and an extremely poor …

Targeting apoptosis and unfolded protein response: the impact of β-hydroxybutyrate in clear cell renal cell carcinoma under glucose-deprived conditions

F Roohy, M Siri, K Kohansal, A Ghalandari… - Molecular Biology …, 2024 - Springer
Background Clear cell renal cell carcinoma (ccRCC) plays a significant role in the mortality
associated with kidney cancer. Targeting biological processes that inhibit cancer growth …

Optimization of a novel mandelamide-derived pyrrolopyrimidine series of PERK inhibitors

ME Stokes, MD Surman, V Calvo, D Surguladze, AH Li… - Pharmaceutics, 2022 - mdpi.com
The protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is one of three
endoplasmic reticulum (ER) transmembrane sensors of the unfolded protein response …

Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator

CG Thomson, TD Aicher, W Cheng, H Du… - Journal of Medicinal …, 2024 - ACS Publications
A series of activators of GCN2 (general control nonderepressible 2) kinase have been
developed, leading to HC-7366, which has entered the clinic as an antitumor therapy …