Results 41 to 50 of about 56,924 (160)

The novel BET inhibitor UM-002 reduces glioblastoma cell proliferation and invasion

Scientific Reports, 2021
Bromodomain and extraterminal domain (BET) proteins have emerged as therapeutic targets in multiple cancers, including the most common primary adult brain tumor glioblastoma (GBM).
Anna M. Jermakowicz, Matthew J. Rybin, Robert K. Suter, Jann N. Sarkaria, Zane Zeier, Yangbo Feng, Nagi G. Ayad   +6 more
doaj   +1 more source

BET degraders reveal BRD4 disruption of 7SK and P-TEFb is critical for effective reactivation of latent HIV in CD4+ T-cells

Journal of Virology
HIV cure strategies that aim to induce viral reactivation for immune clearance leverage latency reversal agents to modulate host pathways which directly or indirectly facilitate viral reactivation.
Anne-Marie W. Turner, Frances M. Bashore, Shane D. Falcinelli, Joshua A. Fox, Alana L. Keller, Anthony D. Fenton, Renee F. Geyer, Brigitte Allard, Jennifer L. Kirchherr, Nancie M. Archin, Lindsey I. James, David M. Margolis   +11 more
doaj   +1 more source

The Functions of BET Proteins in Gene Transcription of Biology and Diseases

Frontiers in Molecular Biosciences, 2021
The BET (bromodomain and extra-terminal domain) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT, are widely acknowledged as major transcriptional regulators in biology.
Ka Lung Cheung, Claudia Kim, Ming-Ming Zhou   +2 more
doaj   +1 more source

Epigenetic dysregulation in chronic myeloid leukaemia: A myriad of mechanisms and therapeutic options [PDF]

, 2018
The onset of global epigenetic changes in chromatin that drive tumor proliferation and heterogeneity is a hallmark of many forms cancer. Identifying the epigenetic mechanisms that govern these changes and developing therapeutic approaches to modulate ...
Koschmieder, Steffen, Vetrie, David
core   +1 more source

Siah2 control of T-regulatory cells limits anti-tumor immunity. [PDF]

, 2020
Understanding the mechanisms underlying anti-tumor immunity is pivotal for improving immune-based cancer therapies. Here, we report that growth of BRAF-mutant melanoma cells is inhibited, up to complete rejection, in Siah2-/- mice.
Aifantis, Ioannis, Bosenberg, Marcus, Bradley, Linda M, Brown, Kevin, Dolgalev, Igor, Feng, Yongmei, Hockemeyer, Kathryn, Li, Yan, Marine, Jean-Christophe, Otero, Dennis C, Poźniak, Joanna, Rambow, Florian, Ronai, Ze'ev A, Scortegagna, Marzia, Tinoco, Roberto, Zhang, Tongwu   +15 more
core   +2 more sources

Application of Small Epigenetic Modulators in Pediatric Medulloblastoma [PDF]

, 2018
Medulloblastoma is one of the most frequent among pediatric brain tumors, and it has been classified in various subgroups. Some of them already benefit from quite good therapeutic options, whereas others urgently need novel therapeutic approaches ...
Annalisa Romanelli, Antonello Mai, Antonello Mai, Clemens Zwergel, Giulia Stazi, Giuseppina Catanzaro, Marco Tafani, Sergio Valente, Zein Mersini Besharat   +8 more
core   +2 more sources

N-terminal BET bromodomain inhibitors disrupt a BRD4-p65 interaction and reduce inducible nitric oxide synthase transcription in pancreatic β-cells

Frontiers in Endocrinology, 2022
Chronic inflammation of pancreatic islets is a key driver of β-cell damage that can lead to autoreactivity and the eventual onset of autoimmune diabetes (T1D).
Joshua A. Nord, Sarah L. Wynia-Smith, Alyssa L. Gehant, Rachel A. Jones Lipinski, Aaron Naatz, Inmaculada Rioja, Rab K. Prinjha, John A. Corbett, Brian C. Smith   +8 more
doaj   +1 more source

Selective small molecule induced degradation of the BET bromodomain protein BRD4 [PDF]

, 2015
The Bromo- and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET selective bromodomain inhibitor JQ1.
Alessio Ciulli, Anders L., Baratta M. G., Baud M. G. J., Belkina A. C., Boi M., Brand M., Bretones G., Cheng Z., Chung C.-W., Corson T. W., Cyrus K., Delmore J. E., Filippakopoulos P., Filippakopoulos P., Filippakopoulos P., Galdeano C., Gallenkamp D., Gosmini R., Hnilicová J., Hon W.-C., Khan Y. M., Kwok-Ho Chan, Lamoureux F., Lee H., Li Z., McLure K. G., Mertz J. A., Michael Zengerle, Mirguet O., Nicodeme E., Prinjha R. K., Raina K., Sakamoto K. M., Sakamoto K. M., Schneekloth J. S., Seoane J., Shi J., Strasser A., Zuber J.   +39 more
core   +5 more sources

Epigenomic regulation of heart failure: integrating histone marks, long noncoding RNAs, and chromatin architecture. [PDF]

, 2018
Epigenetic processes are known to have powerful roles in organ development across biology. It has recently been found that some of the chromatin modulatory machinery essential for proper development plays a previously unappreciated role in the ...
McKinsey, Timothy A, Vondriska, Thomas M, Wang, Yibin   +2 more
core  

Is now the time for molecular driven therapy for diffuse large B-cell lymphoma? [PDF]

, 2017
INTRODUCTION: Recent genetic and molecular discoveries regarding alterations in diffuse large B-cell lymphoma (DLBCL) deeply changed the approach to this lymphoproliferative disorder.
Ansuinelli, Michela, DE ANGELIS, Federico, DI ROCCO, Alice, Foa, Roberto, Martelli, Maurizio   +4 more
core   +1 more source