Results 121 to 130 of about 24,956 (275)

Opposing effects of cancer-type-specific SPOP mutants on BET protein degradation and sensitivity to BET inhibitors

, 2017
It is generally assumed that recurrent mutations within a given cancer driver gene elicit similar drug responses. Cancer genome studies have identified recurrent but divergent missense mutations affecting the substrate-recognition domain of the ubiquitin
Bellini, Elisa, Losa, Marco, Carr, Steven A, Gregory V Kryukov, Mutch, D.G., Steven A Carr, Craig M Bielski, Peter, Matthias, Ulbricht, A., Jean-Philippe P Theurillat, Wild, P.J., Carney, Michael E, Bellini, E., Kryukov, Gregory V, Boris J N Winterhoff, El Tekle, G., Peter Schraml, Udeshi, Namrata D, Janouskova, H., Anna Ulbricht, Cascione, Luciano; https://orcid.org/, Peter, M., Cascione, L., Theurillat, Jean-Philippe P, Carlo V Catapano, Wild, Peter J, Anna Rinaldi, Civenni, Gianluca, Udeshi, N.D., Broaddus, Russell R, Tiziano Bernasocchi, Garraway, Levi A, Tanya Svinkina, Enchev, R.I., Schraml, P., Sara Napoli, Marco Losa, Hana Janouskova, Namrata D Udeshi, Berchuck, A., Catapano, C.V., Carney, M.E., Carr, S.A., Winterhoff, Boris J N, Moch, H., Rinaldi, A., Civenni, G., Garraway, L.A., Russell R Broaddus, Bertoni, F., Moch, Holger, Geniver El Tekle, Gianluca Civenni, David G Mutch, Enchev, Radoslav I, Winterhoff, BJN, Bielski, C.M., Kryukov, G.V., Matthias Peter, Theurillat, J.P., Napoli, Sara, Schraml, Peter, Catapano, Carlo V, Svinkina, Tanya, Luciano Cascione, Levi A Garraway, Bertoni, Francesco, Michael E Carney, Mutch, David G; https://orcid.org/, Elisa Bellini, Radoslav I Enchev, Bernasocchi, T., Peter J Wild, Svinkina, T., Janouskova, Hana, Losa, M., Napoli, S., El Tekle, Geniver, Andrew Berchuck, Francesco Bertoni, Bielski, Craig M, Broaddus, R.R., Berchuck, Andrew, Rinaldi, Anna, Bernasocchi, Tiziano, Ulbricht, Anna, Holger Moch   +86 more
core   +1 more source

BET inhibitors synergize with sunitinib in melanoma through GDF15 suppression. [PDF]

Exp Mol Med, 2023
Zeng F, Li Y, Meng Y, Sun H, He Y, Yin M, Chen X, Deng G.   +7 more
europepmc   +1 more source

Acute caffeine treatment protects the developing retina from ischemia‐induced cell death

FEBS Open Bio, EarlyView.
Caffeine reduces cell death in the developing retina under ischemia (OGD). This effect does not involve BDNF upregulation or antioxidant pathways (NRF2/VEGF). Neuroprotection occurs mainly through adenosine A2A receptor antagonism, decreasing glutamate release and excitotoxicity, highlighting caffeine's potential as an acute neuroprotective agent in ...
Amanda Alves Nascimento, Danniel Pereira‐Figueiredo, Gabriella Grossi de Lima Dias, Gabriel Ferreira dos Santos, Mariana Rodrigues Pereira, Rafael Brito, Karin C Calaza   +6 more
wiley   +1 more source

MEK inhibitors overcome resistance to BET inhibition across a number of solid and hematologic cancers

, 2018
BET inhibitors exhibit broad activity in cancer models, making predictive biomarkers challenging to define. Here we investigate the biomarkers of activity of the clinical BET inhibitor GSK525762 (I-BET; I-BET762) across cancer cell lines and demonstrate ...
Melissa C. Musso, Anastasia Wyce, Shawn W. Foley, Lijoy K. Mathew, Michael T. McCabe, Satyajit R. Rajapurkar, Olena Barbash, Melissa Stern, Kathryn M. Keenan, Charles F. McHugh, Daniel J. Felitsky, Xi-Ping Zhang, Susan Korenchuk, Natalie O. Karpinich, Peter J. Tummino, Christopher Carpenter, Jeanne J. Matteo, Ryan G. Kruger   +17 more
core   +1 more source

Sudden anaerobization in Amphibacillus xylanus increases intracellular labile ferrous iron and inhibits cell growth

FEBS Open Bio, EarlyView.
Abruptly changing from aerobic to anaerobic conditions (sudden anaerobization) induced growth inhibition and a significant increase in intracellular labile ferrous iron in the aerotolerant anaerobe Amphibacillus xylanus. We found that free flavins mediate efficient electron transfer from NADH to ferric iron under anaerobic conditions, suggesting that ...
Shinya Kimata, Yoichi Sakai, Keisuke Tanaka, Etsuro Yoshimura, Ken Kitano, Morio Ishikawa, Tadahiro Nakamoto, Tsutomu Takayama, Hirofumi Inoue, Kaho Nomura, Tomonori Suzuki, Masataka Uchino, Akira Abe, Youichi Niimura   +13 more
wiley   +1 more source

Simultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells. [PDF]

J Enzyme Inhib Med Chem, 2023
Negri A, Marozzi M, Trisciuoglio D, Rotili D, Mai A, Rizzi F.   +5 more
europepmc   +1 more source

UiO‐66 metal–organic frameworks in biomedicine: From structural tunability to bioimaging, photodiagnostics, and photodynamic cancer therapy

FEBS Open Bio, EarlyView.
UiO‐66(Zr) metal–organic frameworks are chemically stable, biocompatible, and highly tunable nanomaterials. Their modular structure enables controlled drug delivery, multimodal bioimaging, and light‐activated photodynamic therapy, supporting integrated diagnostic and therapeutic (theranostic) applications in cancer and biomedical research.
Veronika Huntošová, Grigorii Rakhalskii, Miroslav Almáši   +2 more
wiley   +1 more source

Potential Applications of BET Inhibitors in Combination with other Anti-Cancer Agents

Bromodomain and Extra-Terminal Domain (BET) proteins are a family of epigenetic readers which bind to specific acetylated lysine residues located on histone tails.
Gray, Araminta
core   +1 more source

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain

, 2018
The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomainsBRD2, BRD3, BRD4, and BRDTeach contain two bromodomain modules.
Chun-wa Chung (1343454), David J. Hirst (1399282), Paul Bamborough (1343466), Emmanuel H. Demont (1399288), Matthew Lindon (1355946), Robert P. Law (2613493), Rab K. Prinjha (449759), Allan J. B. Watson (1369614), Stephen J. Atkinson (1297362), Laurie J. Gordon (1343442)   +9 more
core   +1 more source

From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors. [PDF]

Eur J Med Chem, 2023
Koravovic M, Mayasundari A, Tasic G, Keramatnia F, Stachowski TR, Cui H, Chai SC, Jonchere B, Yang L, Li Y, Fu X, Hiltenbrand R, Paul L, Mishra V, Klco JM, Roussel MF, Pomerantz WC, Fischer M, Rankovic Z, Savic V.   +19 more
europepmc   +1 more source