Results 11 to 20 of about 26,367 (213)

BRD4 sustains p63 transcriptional program in keratinocytes

Biology Direct
Here, we investigated the potential interaction between bromodomain-containing protein 4 (BRD4), an established epigenetic modulator and transcriptional coactivator, and p63, a member of the p53 transcription factor family, essential for epithelial ...
E. Foffi, A. Violante, R. Pecorari, A. M. Lena, F. Rugolo, G. Melino, E. Candi   +6 more
doaj   +3 more sources

Mechanistic role of GNE-987 targeting BRD4-HCP5 axis in pediatric T-cell acute lymphoblastic leukemia. [PDF]

J Cell Commun Signal
Abstract This study aims to explore the mechanism of action of the Bromodomain‐containing protein 4 (BRD4) inhibitor GNE‐987 in the treatment of pediatric T‐cell Acute Lymphoblastic Leukemia (T‐ALL), focusing on its effect in inhibiting T‐ALL cell proliferation by activating the HLA Complex P5 (HCP5) Super‐enhancer.
Sang X, Jiang M, Guan Y, Chen X, Zhang Z, Wu Y, Peng W.   +6 more
europepmc   +2 more sources

Molecular dynamics simulations data of six compounds F3J-BRD4/CBP, EX1-BRD4/CBP, and E2T-BRD4/CBP

Data in Brief, 2021
The data here described are related to the research article entitled "Molecular dynamics insights into binding selectivity of inhibitors toward BRD4 and CBP" [1]. Bromodomain-containing protein 4 (BRD4) and CREB binding protein (CBP) play important roles in tumorigenesis and development.
Shiliang Wu, Lifei Wang, Lulu Zhang, Xiaoyan Xu, Juan Zhao   +4 more
openaire   +3 more sources

BRD4 inhibitors block telomere elongation [PDF]

Nucleic Acids Research, 2017
Cancer cells maintain telomere length equilibrium to avoid senescence and apoptosis induced by short telomeres, which trigger the DNA damage response. Limiting the potential for telomere maintenance in cancer cells has been long been proposed as a therapeutic target.
Steven Wang, Alexandra M. Pike, Stella S. Lee, Margaret A. Strong, Carla J. Connelly, Carol W. Greider   +5 more
openaire   +3 more sources

P-TEFb et Brd4 [PDF]

médecine/sciences, 2018
La physiologie d’une cellule est dictée par l’intégration des signaux qu’elle reçoit et la mise en place de réponses adaptées par le biais, entre autres, de programmes transcriptionnels adéquats. Pour assurer un contrôle optimal de ces réponses, des mécanismes de régulation ont été sélectionnés, dont un processus de pause transcriptionnelle et de levée
Alessandro Furlan, Florence Agbazahou, Mélanie Henry, Mariano Gonzalez-Pisfil, Corentin Le Nézet, Dorian Champelovier, Marie Fournier, Bernard Vandenbunder, Gabriel Bidaux, Laurent Héliot   +9 more
openaire   +4 more sources

BRD4 Structure–Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536 [PDF]

ACS Medicinal Chemistry Letters, 2015
A focused library of analogues of the dual PLK1 kinase/BRD4 bromodomain inhibitor BI-2536 was prepared and then analyzed for BRD4 and PLK1 inhibitory activities. Particularly, replacement of the cyclopentyl group with a 3-bromobenzyl moiety afforded the most potent BRD4 inhibitor of the series (39j) with a K i = 8.7 nM, which was equipotent against ...
Lijia, Chen, Jeremy L, Yap, Makoto, Yoshioka, Maryanna E, Lanning, Rachel N, Fountain, Mithun, Raje, Jacob A, Scheenstra, Jeffrey W, Strovel, Steven, Fletcher   +8 more
openaire   +2 more sources

Increased expression of BRD4 isoforms long (BRD4-L) and short (BRD4-S) promotes chemotherapy resistance in high-grade serous ovarian carcinoma

Genes & Cancer, 2023
Chemoresistance in ovarian carcinoma is a puzzling issue that urges understanding of strategies used by cancer cells to survive DNA damage and to escape cell death. Expanding efforts to understand mechanisms driving chemoresistance and to develop alternative therapies targeting chemoresistant tumors are critical.
Drumond-Bock, Ana Luiza, Wang, Luyao, Wang, Lin, Cybula, Magdalena, Rostworowska, Maria, Kinter, Michael, Bieniasz, Magdalena   +6 more
openaire   +2 more sources

BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1 [PDF]

, 2013
The bromodomain and extra terminal (BET) family protein bromodomain containing protein 4 (BRD4) is an epigenetic regulator recently identified as a therapeutic target for several hematological cancers, notably mixed lineage leukemia-fusion acute myeloid ...
Bastow, Sarah, Chevassut, Timothy James Telfer, Horne, Gillian Abigail, Stewart, Helen Jayne Susan   +3 more
core   +1 more source

Effect of bet missense mutations on bromodomain function, inhibitor binding and stability [PDF]

, 2016
Lysine acetylation is an important epigenetic mark regulating gene transcription and chromatin structure. Acetylated lysine residues are specifically recognized by bromodomains, small protein interaction modules that read these modification in a ...
Alessandra, Pasquo, Chiaraluce, Roberta, Consalvi, Valerio, Cynthia, Tallant, Lori, Clorinda, Lori, Laura, Petrosino, Maria, Stefan, Knapp   +7 more
core   +2 more sources

ARV-825 Showed Antitumor Activity against BRD4-NUT Fusion Protein by Targeting the BRD4

Journal of Oncology, 2023
Objective. The bromodomain-containing 4 (BRD4) is a member of the bromodomain and extra terminal domain (BET) family, which is an important epigenetic reader. It is currently a promising oncology target. In some tumors, BET bromodomain inhibitors have demonstrated promising results.
Liu Yang, Yue Jing, Xia Xia, Xiushan Yin
openaire   +2 more sources