Results 11 to 20 of about 20,494 (185)

Methylation of BRD4 by PRMT1 regulates BRD4 phosphorylation and promotes ovarian cancer invasion

Cell Death and Disease, 2023
Bromodomain-containing protein 4 (BRD4), the major component of bromodomain and extra-terminal domain (BET) protein family, has important functions in early embryonic development and cancer development. However, the posttranslational modification of BRD4
Yi Liu, Hejing Liu, Miaomiao Ye, Mengying Jiang, Xin Chen, Gendi Song, Huihui Ji, Zhi-wei Wang, Xueqiong Zhu   +8 more
doaj   +2 more sources

Transcriptome analysis of dominant-negative Brd4 mutants identifies Brd4-specific target genes of small molecule inhibitor JQ1 [PDF]

Scientific Reports, 2017
The bromodomain protein Brd4 is an epigenetic reader and plays a critical role in the development and maintenance of leukemia. Brd4 binds to acetylated histone tails and activates transcription by recruiting the positive elongation factor P-TEFb.
Tim-Michael Decker, Michael Kluge, Stefan Krebs, Nilay Shah, Helmut Blum, Caroline C. Friedel, Dirk Eick   +6 more
doaj   +2 more sources

BRD4-mediated repression of p53 is a target for combination therapy in AML [PDF]

, 2021
Acute myeloid leukemia (AML) is a typically lethal molecularly heterogeneous disease, with few broad-spectrum therapeutic targets. Unusually, most AML retain wild-type TP53, encoding the pro-apoptotic tumor suppressor p53.
McGarry, Lynn, Lopez, Jonathan, Sha Li (145229), Xue Lei (4092547), Adams, Peter D., Claire Reid (16283252), Huang, Xu, Copland, Mhairi, Tait, Stephen W.G., Abraham, Sheela A., Higgins, Brian, Rishi, Loveena, Stewart, Helen J.S., Cole, John, others (6644544), Lei, Xue, Campos, Joana, Latif, Anne-Louise, Helen Stewart (4461571), Maria Terradas Terradas (16283243), Li, Sha, Keeshan, Karen, John Cole (392281), Robertson, Neil A., Loveena Rishi (16283246), William Clark (775696), Morton, Jennifer P., Timothy Chevassut (4462168), Neil A Robertson (9356086), Terradas Terradas, Maria, Kathryn Gilroy (8103383), Sakamaki, Jun-ichi, Lynn McGarry (3418214), Reid, Claire, Claire McKeeve (16283249), Davison, Andrew, Newcombe, Ashley, Ryan, Kevin M., Holyoake, Tessa, Ashley Newcombe (16283240), Blyth, Karen, Anne-Louise Latif (16283237), Clark, William, Kirschner, Kristina, Chevassut, Timothy J.T., McKeeve, Claire, Gilroy, Kathryn   +46 more
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Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader [PDF]

, 2021
Targeted protein degradation is a powerful induced-proximity tool to control cellular concentrations of native proteins using small molecules. However, the design of selectivity in protein degradation remains challenging.
Huda, Zahid, Dan, Harki, Anand, Divakaran, Taosheng, Chen, Wenwei , Lin, william, pomerantz   +5 more
core   +1 more source

Discovery of the natural product 3',4',7,8-tetrahydroxyflavone as a novel and potent selective BRD4 bromodomain 2 inhibitor

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Bromodomain-containing protein 4 (BRD4) binds acetylated lysine residues on the N-terminal tails of histones through two bromodomains (BD1 and BD2) to regulate gene transcription.
Jiao Li, Wei Zou, Koukou Yu, Bing Liu, Weifeng Liang, Lisha Wang, Yin Lu, Zequn Jiang, Aiyun Wang, Jiapeng Zhu   +9 more
doaj   +1 more source

Bromodomain protein BRD4 is an epigenetic activator of B7-H6 expression in acute myeloid leukemia

OncoImmunology, 2021
B7-H6, a ligand for the NK activating receptor NKp30, has been identified as a biomarker of poor prognosis in several solid cancers. However, little is known about the role of B7-H6 and the mechanisms that control its expression in acute myeloid leukemia
Aroa Baragaño Raneros, Ramon M Rodriguez, Aida Bernardo Flórez, Pilar Palomo, Enrique Colado, Alfredo Minguela, Beatriz Suarez-Alvarez, Carlos López-Larrea   +7 more
doaj   +1 more source

Structural variation of protein-ligand complexes of the first bromodomain of BRD4 [PDF]

, 2021
The bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal domain (BET) family, plays a key role in several diseases, especially cancers.
Ellen, Guest, Guest, Ellen E., Stephen, Pickett, Pickett, Stephen D., Jonathan, Hirst, Hirst, Jonathan D.   +5 more
core   +5 more sources

Molecular Insight into Function of the Evolutionarily Conserved Brd4 Extraterminal Domain (ET) and Mechanism of Brd4 Functions in Human Diseases

, 2012
Bromodomain protein 4 (Brd4) plays critical roles in development, cancer progression and virus-host pathogenesis. Papillomaviruses (PV) E2 protein associates with Brd4 and this interaction is important for transcriptional regulation of the viral ...
Rahman, Shaila
core   +6 more sources

Inducing DNA damage through R-loops to kill cancer cells

Molecular & Cellular Oncology, 2021
R-loops are intermediate structures of transcription that can accumulate when transcriptional elongation is blocked by inhibiting BRD4. In normal cells, R-loop persistence suppresses firing of adjacent replication origins.
Fred C. Lam, Yi Wen Kong, Michael B. Yaffe   +2 more
doaj   +1 more source

Diverse Amine-Acid Coupling Reactions Modulate the Potency of BRD4 PROTACs [PDF]

, 2023
Protein degradation with proteolysis targeting chimeras (PROTACs) has emerged as a powerful therapeutic strate-gy. PROTACs are heterobifunctional molecules consisting of a target-binding moiety, a linker and an E3 ligase-binding moiety that are commonly ...
Andrew, McGrath, Nadeem A., Vellore, Jennifer D., Venable, Haiyan, Huang, Tim, Cernak, Jean-Francois, Brazeau, Lu, Zhu, Zhicai, Shi, Zirong, Zhang, Christine, Gelin   +9 more
core   +1 more source