Dual degradation mechanism of GPX4 degrader in induction of ferroptosis exerting anti-resistant tumor effect

C Wang, C Zheng, H Wang, S Shui, H Jin, G Liu… - European Journal of …, 2023 - Elsevier
Abstract Targeting Glutathione peroxidase 4 (GPX4) has become a promising strategy for
drug-resistant cancer therapy via ferroptosis induction. It was found that the GPX4 inhibitors …

[HTML][HTML] Prospects for anti-tumor mechanism and potential clinical application based on glutathione peroxidase 4 mediated ferroptosis

M Chen, Z Shi, Y Sun, H Ning, X Gu… - International Journal of …, 2023 - mdpi.com
Ferroptosis, characterized by excessive iron accumulation and lipid peroxidation, is a novel
form of iron-dependent cell death, which is morphologically, genetically, and biochemically …

A potent GPX4 degrader to induce ferroptosis in HT1080 cells

H Song, J Liang, Y Guo, Y Liu, K Sa, G Yan… - European Journal of …, 2024 - Elsevier
Abstract Glutathione peroxidase 4 (GPX4) is the most promising target for inducing
ferroptosis. GPX4-targeting strategies primarily focus on inhibiting its activity or adjusting its …

Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells

H Wang, C Wang, B Li, C Zheng, G Liu, Z Liu… - European Journal of …, 2023 - Elsevier
Ferroptosis is an iron-dependent cell death caused by the accumulation of lipid
peroxidation. The glutathione peroxidase 4 (GPX4) is an antioxidative enzyme and a major …

Structure-activity relationship study of RSL3-based GPX4 degraders and its potential noncovalent optimization

C Zheng, C Wang, D Sun, H Wang, B Li, G Liu… - European Journal of …, 2023 - Elsevier
Ferroptosis is an iron-dependent, non-apoptotic form of cell death involving in various
disease processes. Mechanistically, glutathione peroxidase 4 (GPX4) which belongs to the …

[HTML][HTML] Identification of a small molecule as inducer of ferroptosis and apoptosis through ubiquitination of GPX4 in triple negative breast cancer cells

Y Ding, X Chen, C Liu, W Ge, Q Wang, X Hao… - Journal of hematology & …, 2021 - Springer
Background TNBC is the most aggressive breast cancer with higher recurrence and
mortality rate than other types of breast cancer. There is an urgent need for identification of …

[HTML][HTML] Post-translational modification of GPX4 is a promising target for treating ferroptosis-related diseases

C Cui, F Yang, Q Li - Frontiers in Molecular Biosciences, 2022 - frontiersin.org
Glutathione peroxidase 4 (GPX4) is one of the most important antioxidant enzymes. As the
key regulator of ferroptosis, GPX4 has attracted considerable attention in the fields of cancer …

Directly targeting glutathione peroxidase 4 may be more effective than disrupting glutathione on ferroptosis-based cancer therapy

Y Wei, H Lv, AB Shaikh, W Han, H Hou, Z Zhang… - … et Biophysica Acta (BBA …, 2020 - Elsevier
Background Cancer is one of the major threats to human health and current cancer
therapies have been unsuccessful in eradicating it. Ferroptosis is characterized by iron …

Identification of a small molecule that enhances ferroptosis via inhibition of ferroptosis suppressor protein 1 (FSP1)

H Yoshioka, T Kawamura, M Muroi… - ACS Chemical …, 2022 - ACS Publications
Glutathione peroxidase 4 (GPX4) is an intracellular enzyme that oxidizes glutathione while
reducing lipid peroxides and is a promising target for cancer therapy. To date, several GPX4 …

PDTAC: targeted photodegradation of GPX4 triggers ferroptosis and potent antitumor immunity

S Liu, X Zhao, S Shui, B Wang, Y Cui… - Journal of Medicinal …, 2022 - ACS Publications
Targeted degradation of proteins, especially those regarded as undruggable or difficult to
drug, attracts wide attention to develop novel therapeutic strategies. Glutathione peroxidase …