Results 111 to 120 of about 15,581 (231)

Improving PARP inhibitor efficacy in bladder cancer without genetic BRCAness by combination with PLX51107

Molecular Oncology, Volume 20, Issue 3, Page 779-803, March 2026.
Clinical trials on PARP inhibitors in urothelial carcinoma (UC) showed limited efficacy and a lack of predictive biomarkers. We propose SLFN5, SLFN11, and OAS1 as UC‐specific response predictors. We suggest Talazoparib as the better PARP inhibitor for UC than Olaparib.
Jutta Schmitz, Anna L. Bartkowiak, Michael Rose, Nora Kolks, Patrick Petzsch, Vandana Solanki, Anne Stoffel, Bianca Faßbender, Leandra Lepping, Julka Volkamer, Karl Köhrer, Marc Seifert, Tokameh Mahmoudi, Tahlita C. M. Zuiverloon, Günter Niegisch, Michèle J. Hoffmann   +15 more
wiley   +1 more source

Development of a PET Probe Targeting Bromodomain and Extra-Terminal Proteins for In Vitro and In Vivo Visualization

Pharmaceuticals
Background: Bromodomain and extra-terminal (BET) proteins are critical regulators of gene transcription, as they recognize acetylated lysine residues. The BD1 bromodomain of BRD4, a member of the BET family, has emerged as a promising therapeutic target ...
Yongle Wang, Yanli Wang, Yulong Xu, Hua Cheng, Tewodros Mulugeta Dagnew, Leyi Kang, Darcy Tocci, Iris Z. Shen, Can Zhang, Changning Wang   +9 more
doaj   +1 more source

Binding hotspots of BAZ2B bromodomain: Histone interaction revealed by solution NMR driven docking. [PDF]

, 2014
Bromodomains are epigenetic reader domains, which have come under increasing scrutiny both from academic and pharmaceutical research groups. Effective targeting of the BAZ2B bromodomain by small molecule inhibitors has been recently reported, but no ...
Alessio Ciulli, Alexandre M. J. J. Bonvin, Artimo P., Best R. B., Charlop-Powers Z., Chris Abell, Cole R., Corrêa D. H., David M. Dias, de Vries S. J., Dominguez C., Fedorov O., Ferguson F. M., Filippakopoulos P., Filippakopoulos P., Filippakopoulos P., Fleur M. Ferguson, García de la Torre J., Guetg C., Hans Wienk, Hess B., Huang D., Hwang T.-L., Jones M. H., João P. G. L. M. Rodrigues, Liu Y., Magno A., Marley J., Morris K. F., Muller S., Nicodeme E., Olsson M. H. M., Philpott M., Poplawski A., Rolf Boelens, Sun H., Trellet M., Wienk H.   +37 more
core   +6 more sources

Scalable syntheses of the BET bromodomain inhibitor JQ1

Tetrahedron Letters, 2015
We have developed methods involving the use of alternate, safer reagents for the scalable syntheses of the potent BET bromodomain inhibitor JQ1. A one-pot three step method, involving the conversion of a benzodiazepine to a thioamde using Lawesson's reagent, followed by amidrazone formation and installation of the triazole moiety furnished JQ1.
Syeda, Shameem Sultana, Jakkaraj, Sudhakar, Georg, Gunda I.   +2 more
openaire   +2 more sources

PBRM1 Deficiency Reshapes an Immune Suppressive Microenvironment Through Epigenetic Tuning of PBRM1‐KDM5C‐IL6 Axis in ccRCC

Advanced Science, Volume 13, Issue 16, 18 March 2026.
PBRM1 ranks as the second most commonly mutated gene in ccRCC. This study reveals that PBRM1 loss promotes an immunosuppressive microenvironment by elevating M2 TAMs via the KDM5C–IL‐6 axis. These M2 TAMs, along with CAFs, form a barrier that excludes CD8+ T cells. Targeting IL‐6 synergizes with anti‐PD1 therapy, offering a promising strategy for PBRM1‐
Wenjiao Xia, Hongru Wang, Yu Dong, Zitong Yang, Yiyang Zhou, Zhinan Xia, Qinchen Li, Liangliang Ren, Yichun Zheng, Junliang Yan, Dongmei Ma, Zhi Chen, Xingang Cui, Guixin Zhu, Cheng Zhang   +14 more
wiley   +1 more source

The BET protein FSH functionally interacts with ASH1 to orchestrate global gene activity in Drosophila [PDF]

, 2013
BACKGROUND: The question of how cells re-establish gene expression states after cell division is still poorly understood. Genetic and molecular analyses have indicated that Trithorax group (TrxG) proteins are critical for the long-term maintenance of ...
Christian Beisel, Daniel Hess, Moritz Gerstung, Niko Beerenwinkel, Renato Paro, Tobias Kockmann, Tommy Schlumpf, Zhu Xhinzhou   +7 more
core   +2 more sources

Cytokine‐Engineered Chimeric Antigen Receptor‐T Cell Therapy: How to Balance the Efficacy and Toxicity

Advanced Science, Volume 13, Issue 14, 9 March 2026.
Cytokine‐engineered CAR‐T cells represent a promising immunotherapy against malignancies due to direct tumor killing and potent immunity response. However, significant toxicities, including CRS and ICANS, have restricted clinical applications. How to keep the risk‐benefit balance of the advanced therapy is of great importance for maximizing the benefit
Xinru Zhang, Gulizeba Aimaiti, Yuanye Guan, Yuzhe Sha, Wei Zhou, Jiefeng Shen, Bo Zhao, Wei‐En Yuan   +7 more
wiley   +1 more source

A Review of the Bromodomain and Extraterminal Domain Epigenetic Reader Proteins: Function on Virus Infection and Cancer

Viruses
The BET (bromodomain and extraterminal domain) family of proteins, particularly BRD4 (bromodomain-containing protein 4), plays a crucial role in transcription regulation and epigenetic mechanisms, impacting key cellular processes such as proliferation ...
Mengli Wu, Guiquan Guan, Hong Yin, Qingli Niu   +3 more
doaj   +1 more source

tBRD-1 selectively controls gene activity in the Drosophila testis and interacts with two new members of the bromodomain and extra-terminal (BET) family.

PLoS ONE, 2014
Multicellular organisms have evolved specialized mechanisms to control transcription in a spatial and temporal manner. Gene activation is tightly linked to histone acetylation on lysine residues that can be recognized by bromodomains.
Ina Theofel, Marek Bartkuhn, Tim Hundertmark, Thomas Boettger, Stefanie M K Gärtner, Katja Leser, Stephan Awe, Michael Schipper, Renate Renkawitz-Pohl, Christina Rathke   +9 more
doaj   +1 more source

Central role of Yes-associated protein and WW-domain-containing transcriptional co-activator with PDZ-binding motif in pancreatic cancer development. [PDF]

, 2019
Pancreatic ductal adenocarcinoma (PDAC) remains a deadly disease with no efficacious treatment options. PDAC incidence is projected to increase, which may be caused at least partially by the obesity epidemic.
Eibl, Guido, Rozengurt, Enrique
core