Results 21 to 30 of about 34,214 (293)

A New Recruitable E3 Ligase UHRF1 Supporting Targeted Protein Degradation: A Minimal Azide as a Recruitment Ligand. [PDF]

Adv Sci (Weinh)
Targeted protein degradation is often limited by the scarcity of usable E3 ligases. Herein, we report the first small‐molecule GPX4 degraders that incorporate either electrophilic warheads or a minimal azide group as an E3 recruitment ligand. The azide‐based degrader DK‐5070 effectively drives potent GPX4 degradation; mechanistic studies reveal that ...
Lin Z, Duan K, Wan R, Jiang T, Wei J, Sun M, Skryl'nikova MA, Gureev MA, Zhang ZM, Zhang Z, Ding K, Ma N, Liu T, Tan Y, Li Z.   +14 more
europepmc   +2 more sources

GPX4 protein in brain tissues.

, 2023
(A) Representative immunofluorescence images of GPX4 (red), NeuN (green) and DAPI (blue) (bar = 50 μm). (B) Bar graph of GPX4 fluorescence intensity in the whole field of view (n = 3). (C) Western blot analysis of GPX4 (n = 3). * P < 0.05.
Deng-Hai Zhang (16954832), Feng-Ying Guo (16954835), Yan-Mei Ma (8767593), Meng Wang (124646), Li Jing (445177), Jian-Zhong Zhang (10920444), Lan Yang (457660), Lu Li (14069)   +7 more
core   +1 more source

The Modulatory Effect of Liraglutide on the Expression of GPX4, HO-1 and SLC7A11 Signaling Pathway in Obese Rats [PDF]

Pharmaceutical Sciences
Background: Obesity, a multifaceted metabolic condition, is associated with oxidative stress and disrupted redox homeostasis, leading to ferroptosis and metabolic dysfunction. Liraglutide, a well-known glucagon-like peptide-1 (GLP-1) receptor agonist, is
Mahmood Jameel Saeed, Inam Sameh Arif
doaj   +1 more source

Hypermethylation of the Nrf2 Promoter Induces Ferroptosis by Inhibiting the Nrf2-GPX4 Axis in COPD

International Journal of COPD, 2021
Zixiao Zhang,1,* Congli Fu,1,2,* Jiaxin Liu,1 Xiaoyan Sai,1 Chu Qin,1 Tingting Di,1 Yue Yang,1 Yan Wu,1 Tao Bian1 1Department of Respiratory Medicine, Wuxi People’s Hospital Affiliated to Nanjing, Medical University, Wuxi, Jiangsu, 214023, People’
Zhang Z, Fu C, Liu J, Sai X, Qin C, Di T, Yang Y, Wu Y, Bian T   +8 more
doaj  

A mTORC1-mediated cyst(e)ine sensing mechanism governing GPX4 synthesis and ferroptosis

Molecular & Cellular Oncology, 2021
Ferroptosis is a cell death mechanism triggered by lipid peroxidation. Our recent study linked cyst(e)ine availability with glutathione peroxidase 4 (GPX4) protein synthesis and ferroptosis mitigation via a Rag-mechanistic target of rapamycin complex 1 ...
Yuelong Yan, Guang Lei, Boyi Gan
doaj   +1 more source

Selenium and GPX4, a vital symbiosis

Free Radical Biology and Medicine, 2018
Selenium has transitioned from an environmental poison and carcinogen to an essential micronutrient associated with a broad array of health promoting effects. These beneficial effects are now accepted to be linked to its incorporation into selenoproteins, a family of rare proteins utilizing a specialized translation machinery to integrate selenium in ...
Friedmann Angeli, J.P.F., Conrad, M.
openaire   +4 more sources

Degrading GPX4 via Biomimetic Nanoparticle-Mediated In Situ Synthesis of Deep-Learning-Designed Binder-Degron Chimeras for Prostate Cancer Therapy. [PDF]

Adv Sci (Weinh)
A deep‐learning‐designed binder is fused to a combinatorial degron to create a binder‐degron chimera (bdC) that recruits the CUL2‐RING ubiquitin ligase complex. Encapsulation in a prostate‐cancer‐targeted, CD47‐camouflaged nanocarrier enables tumor‐specific in situ bdC expression, triggering GPX4 degradation and ferroptosis, thereby establishing a ...
Zhang SH, An Y, Zeng N, Liu MC, Sun JX, Gong X, Xu JZ, Wang SG, Xia QD.   +8 more
europepmc   +2 more sources

Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles

, 2023
We recently described glutathione peroxidase 4 (GPX4) as a promising target for killing therapy-resistant cancer cells via ferroptosis. The onset of therapy resistance by multiple types of treatment results in a stable cell state marked by high levels of
Cai, Luke L., Eaton, John K., Niehues, Michael, Viswanathan, Vasanthi S, Neuhaus, Roland, Badock, Volker, Lazarski, Kiel E., Ryan, Matthew J., Montagnon, Claire, Hillig, Roman C., Christian, Sven, Furst, Laura, Eheim, Ashley L., Clemons, Paul, Schreiber, Stuart L, Gradl, Stefan, Ruberto, Richard, Kramm, Anneke, Chen, Sixun, Zimmermann, Katja, Moosmayer, Dieter, Hilpmann, André, Bajrami, Besnik   +22 more
core   +1 more source

A masked zinger to block GPX4

Nature Chemical Biology, 2020
Ferroptosis induced by GPX4 inhibition offers promise for killing drug-resistant cancer cells, yet current GPX4 inhibitors lack selectivity. The discovery of masked nitrile oxide electrophiles as selective prodrug inhibitors of GPX4 points to an attractive path for chemically inducing ferroptosis.
Stefan G. Kathman, Benjamin F. Cravatt
openaire   +2 more sources

Mechanistische und evolutionäre Aspekte der Glutathionperoxidase 4 (Gpx4) [PDF]

, 2022
Die Glutathionperoxidase 4 (Gpx4) zählt zur Enzymfamilie der Glutathionperoxidasen (Gpx). Diese Proteine reduzieren organische und anorganische Hydroperoxide zu deren jeweiligen Hydroxiden. Charakteristischerweise verfügen die Enzyme der Gpx-Familie über
Roth, Sophia
core   +1 more source