Results 81 to 90 of about 20,657 (229)

BET bromodomain inhibitor JQ1 modulates microRNA expression in thyroid cancer cells

Oncology Reports, 2017
Anaplastic thyroid carcinoma (ATC) represents the most lethal thyroid cancer sub-type, currently unresponsive to standard treatments. Recently, bromodomain and extra-terminal (BET) proteins have emerged as attractive therapeutic targets in several diseases, including cancer.
Mio, Catia, Conzatti, Ketty, Baldan, Federica, Allegri, Lorenzo, Sponziello, Marialuisa, Rosignolo, Francesca, Russo, Diego, Filetti, Sebastiano, Damante, Giuseppe   +8 more
openaire   +5 more sources

AI‐Powered Framework for Evaluating Drug Efficacy for Three‐Dimensional In Vitro Cancer Models in Robot‐Assisted Production

Advanced Robotics Research, EarlyView.
An AI‐powered, robot‐assisted framework automatically produces, images, and analyzes 3D tumor spheroids to evaluate drug efficacy. Integrated modules handle spheroid formation, live/dead staining, brightfield imaging, and automated image analysis, including spheroid segmentation, viability and metrics to assess the drug treatment efficacy. The workflow
Dalia Mahdy, Jesus Nieves, Lukas Königer, Matthias Peindl, Fabio Erhard, Marc Möllmann, Anke Klingner, Markus Münig, Bibin Babu, Thomas Schwarz, Marco Metzger, Gudrun Dandekar, Maximiliane Wußmann, Jan Hansmann   +13 more
wiley   +1 more source

Chemical Catalysis Guides Structural Identification for the Major In Vivo Metabolite of the BET Inhibitor JQ1

ACS Medicinal Chemistry Letters
The bromodomain inhibitor (+)-JQ1 is a highly validated chemical probe; however, it exhibits poor in vivo pharmacokinetics. To guide efforts toward improving its pharmacological properties, we identified the (+)-JQ1 primary metabolite using chemical ...
Secondra L. Holmes, Prashi Jain, Kenneth G. Rodriguez, Jade C. Williams, Zhifeng Yu, Christian G Cerda-Smith, Errol L. G. Samuel, James B. Campbell, John M. Hakenjos, D. Monsivais, Feng Li, S. Chamakuri, M. Matzuk, C. Santini, Kevin Mackenzie, D. Young   +15 more
semanticscholar   +1 more source

Small molecule JQ1 promotes prostate cancer invasion via BET-independent inactivation of FOXA1 [PDF]

Journal of Clinical Investigation, 2020
Recent findings have shown that inhibitors targeting bromodomain and extraterminal domain (BET) proteins, such as the small molecule JQ1, are potent growth inhibitors of many cancers and hold promise for cancer therapy. However, some reports have also revealed that JQ1 can activate additional oncogenic pathways and may affect epithelial-to-mesenchymal ...
Leiming, Wang, Mafei, Xu, Chung-Yang, Kao, Sophia Y, Tsai, Ming-Jer, Tsai   +4 more
openaire   +2 more sources

Discovery of SKP2‐Recruiting PROTACs for Target Protein Degradation

Advanced Science, EarlyView.
Based on the SKP2‐targeting ligand SL1, we designed non‐covalent PROTACs by linking it with the BRD4 inhibitor JQ1 and the AR antagonist AL through a linker. These PROTACs successfully induced the ubiquitination of BRD4 and AR, followed by proteasome‐mediated degradation.
Guanjun Dong, Aima Huang, Ziqing Zhao, Bikai Lai, Xin Pan, Huiyu Yang, Xiaohan Xu, Tianwei Wang, Fangchen Zhao, Zhimin Zhang, Yongbo Xue, Guanjun Deng, Wenbin Deng, Jianwei Chen   +13 more
wiley   +1 more source

Protective effect of the BET protein inhibitor JQ1 in cisplatin-induced nephrotoxicity [PDF]

American Journal of Physiology-Renal Physiology, 2018
As a potent chemotherapy drug, cisplatin is also notorious for its side-effects including nephrotoxicity in kidneys, presenting a pressing need to identify renoprotective agents. Cisplatin nephrotoxicity involves epigenetic regulations, including changes in histone acetylation.
Liping, Sun, Jing, Liu, Yanggang, Yuan, Xinzhou, Zhang, Zheng, Dong   +4 more
openaire   +2 more sources

Targeting PRKCN, an Essential Driver Orchestrating mTOR‐IRF4 Axis Independently of Kinase Activity, in Multiple Myeloma

Advanced Science, EarlyView.
Constitutive PRKCN expression is driven by super‐enhancers and modulated by NF‐κB signaling in multiple myeloma (MM). PRKCN activates mTORC1/2‐IRF4 signaling axis and favors tumor cell growth independently of its kinase activity. IRF4 reciprocally promotes PRKCN transcription, creating a feed‐forward loop.
Koukou Tang, Dongpeng Jiang, Peng Ke, Xiaosen Bian, Lili Zhang, Ying Zhang, Tingting Zhu, Weiwei Qu, Wenhui Qi, Yang Xu, Chengcheng Fu, Depei Wu, Jianhong Chu   +12 more
wiley   +1 more source

Theoretical Studies of Several Small-Ring Precursors to (+)-JQ1 [PDF]

, 2013
We present the results of DFT(B3LYP) calculations on several precursors to (+)-JQ1 using an accurate basis set, including a report of conformational analysis, thermochemistry, optimized geometries and electrostatic potentials, and calculated IR and Raman
Atkinson, Elizabeth J. O., Diamond, James J, Romero, Kevin J   +2 more
core   +1 more source

Uniqueness thresholds on trees versus graphs

, 2008
Counter to the general notion that the regular tree is the worst case for decay of correlation between sets and nodes, we produce an example of a multi-spin interacting system which has uniqueness on the $d$-regular tree but does not have uniqueness on ...
Sly, Allan
core   +1 more source

Ising model for distribution networks [PDF]

, 2011
An elementary Ising spin model is proposed for demonstrating cascading failures (break-downs, blackouts, collapses, avalanches, ...) that can occur in realistic networks for distribution and delivery by suppliers to consumers. A ferromagnetic Hamiltonian
Aleksiejuk A, B. Van Schaeybroeck, Barabási AL, Barabási AL, Buldyrev SV, C. Giuraniuc, Catanzaro M, Cohen R, Crucitti P, Dorogovtsev SN, Gellings CW, Giuraniuc CV, Giuraniuc CV, Giuraniuc CV, Goh K-I, H. Hooyberghs, Indekeu JO, J.O. Indekeu, Malarz K, Motter AE, Newman MEJ, S. Van Lombeek, Sachtjen ML, Simonsen I, Strogatz SH, Van Lombeek S, Watts DJ   +26 more
core   +1 more source