Results 81 to 90 of about 15,581 (231)

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

Systemic aging fuels heart failure: Molecular mechanisms and therapeutic avenues

ESC Heart Failure, Volume 12, Issue 2, Page 1059-1080, April 2025.
Abstract Systemic aging influences various physiological processes and contributes to structural and functional decline in cardiac tissue. These alterations include an increased incidence of left ventricular hypertrophy, a decline in left ventricular diastolic function, left atrial dilation, atrial fibrillation, myocardial fibrosis and cardiac ...
Zhuyubing Fang, Umar Raza, Jia Song, Junyan Lu, Shun Yao, Xiaohong Liu, Wei Zhang, Shujuan Li   +7 more
wiley   +1 more source

BET Bromodomain Inhibition Synergizes with PARP Inhibitor in Epithelial Ovarian Cancer

Cell Reports, 2017
Summary: PARP inhibition is known to be an effective clinical strategy in BRCA mutant cancers, but PARP inhibition has not been applied to BRCA-proficient tumors.
Sergey Karakashev, Hengrui Zhu, Yuhki Yokoyama, Bo Zhao, Nail Fatkhutdinov, Andrew V. Kossenkov, Andrew J. Wilson, Fiona Simpkins, David Speicher, Dineo Khabele, Benjamin G. Bitler, Rugang Zhang   +11 more
doaj   +1 more source

Loci specific epigenetic drug sensitivity. [PDF]

, 2020
Therapeutic targeting of epigenetic modulators offers a novel approach to the treatment of multiple diseases. The cellular consequences of chemical compounds that target epigenetic regulators (epi-drugs) are complex.
Pilko, Anna, Wollman, Roy, Zhang, Thanutra   +2 more
core   +1 more source

Epigenetic regulators as promising therapeutic targets in acute myeloid leukemia. [PDF]

, 2015
Acute myeloid leukemia (AML), the most prevalent acute leukemia in adults, is an aggressive hematological malignancy arising in hematopoietic stem and progenitor cells.
Gallipoli, Paolo, Giotopoulos, George, Huntly, Brian JP   +2 more
core   +2 more sources

Dietary Compound Resveratrol Is a Pan-BET Bromodomain Inhibitor [PDF]

Nutrients, 2017
The chemopreventive and anticancer effects of resveratrol (RSV) are widely reported in the literature. Specifically, mechanisms involving epigenetic regulation are promising targets to regulate tumor development. Bromodomains act as epigenetic readers by recognizing lysine acetylation on histone tails and boosting gene expression in order to regulate ...
Luiz Dutra, David Heidenreich, Gabriel Silva, Chung Man Chin, Stefan Knapp, Jean Santos   +5 more
openaire   +5 more sources

Molecular and genomic advances in breast cancer: A comprehensive review of predictive and therapeutic innovations

Precision Medical Sciences, EarlyView.
Breast cancer subtypes, estrogen receptor‐positive (ER+), HER2‐enriched, and TNBC, are defined by genomic and epigenetic signatures. Multi‐omics profiling, immunotherapy, liquid biopsy, and AI‐driven radiogenomics enable precision medicine. Tools like Oncotype DX and PAM50 support personalized care.
Samina Malik, Arif Malik, Shahzad Ahmad, Hassan Mohsin, Shazia Iqbal   +4 more
wiley   +1 more source

Bromodomain and Extraterminal Proteins as Novel Epigenetic Targets for Renal Diseases

Frontiers in Pharmacology, 2019
Epigenetic mechanisms, especially DNA methylation and histone modifications, are dynamic processes that regulate the gene expression transcriptional program in normal and diseased states. The bromodomain and extraterminal (BET) protein family (BRD2, BRD3,
Jose Luis Morgado-Pascual, Jose Luis Morgado-Pascual, Sandra Rayego-Mateos, Sandra Rayego-Mateos, Lucia Tejedor, Lucia Tejedor, Beatriz Suarez-Alvarez, Beatriz Suarez-Alvarez, Marta Ruiz-Ortega, Marta Ruiz-Ortega   +9 more
doaj   +1 more source

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  

AlphaFold2‐Guided Cyclic Peptide Stabilizer Design to Target Protein–Protein Interactions

Proteins: Structure, Function, and Bioinformatics, EarlyView.
ABSTRACT The control and modulation of protein–protein interactions (PPIs) is of central importance for the majority of biological processes and most biomedical applications. Stabilization of PPIs, besides inhibition, is of growing pharmaceutical interest.
Niklas Halbwedl, Martin Zacharias
wiley   +1 more source