Results 51 to 60 of about 3,510,874 (207)

Gene regulation and tumor suppression by the bromodomain-containing protein BRD7 [PDF]

Cell Cycle, 2010
Oncogene-induced senescence (OIS) is a cellular defense mechanism against excessive mitogenic signaling and tumorigenesis. One of the major pathways required for OIS is the p53 tumor suppressor pathway. Consequently, many human tumors harbor p53 mutations while others show a dysfunctional p53 pathway, frequently by unknown mechanisms.
MANTOVANI, FIAMMA, Drost J., Voorhoeve P. M., DEL SAL, GIANNINO, Agami R.   +4 more
openaire   +3 more sources

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

Bromodomain inhibitors and cancer therapy: From structures to applications

Epigenetics, 2017
Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes that are “writers,” “erasers,” or “readers” of histone modification marks are common. Bromodomains are “readers” that bind acetylated lysines in histone tails. Their
Montserrat Pérez-Salvia, Manel Esteller
doaj   +1 more source

BRD4 Inhibitor GNE-987 Exerts Anticancer Effects by Targeting Super-Enhancer-Related Gene LYL1 in Acute Myeloid Leukemia

Journal of Immunology Research, 2022
Background. AML (acute myeloid leukemia) is a common hematological malignancy in children with poor treatment effects and poor prognosis. Recent studies have shown that as a novel BRD4 (bromodomain containing 4) PROTACs (proteolysis targeting chimeras ...
Xu Sang, Yongping Zhang, Fang Fang, Li Gao, Yanfang Tao, Xiaolu Li, Zimu Zhang, Jianwei Wang, Yuanyuan Tian, Zhiheng Li, Di Yao, Yumeng Wu, Xinran Chu, Kunlong Zhang, Li Ma, Lihui Lu, Yanling Chen, Juanjuan Yu, Ran Zhuo, Shuiyan Wu, Zhen Zhang, Jian Pan, Shaoyan Hu   +22 more
doaj   +1 more source

Solution structure of the extraterminal domain of the bromodomain‐containing protein BRD4 [PDF]

Protein Science, 2008
AbstractBRD4, which is a member of the BET (bromodomains and extraterminal) protein family, interacts preferentially with acetylated chromatin and possesses multiple cellular functions in meiosis, embryonic development, the cell cycle, and transcription.
Yi-Jan, Lin, Takashi, Umehara, Makoto, Inoue, Kohei, Saito, Takanori, Kigawa, Moon-Kyoo, Jang, Keiko, Ozato, Shigeyuki, Yokoyama, Balasundaram, Padmanabhan, Peter, Güntert   +9 more
openaire   +2 more sources

The discovery of I-BRD9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition [PDF]

, 2015
Acetylation of histone lysine residues is one of the most well-studied post-translational modifications of chromatin, selectively recognized by bromodomain “reader” modules.
Ka Hing Che (1357551), Andrew J. Bannister (231506), Gerard Drewes (1290381), Drewy, David H., Prinjha, Rab K., Matthew Lindon (1355946), Laurie Gordon (1357524), Tony Kouzarides, Kouzarides, Tony, Drewry, David H., Paola Grandi (1343472), Rino A. Bit, Dittmann, Antje, Molnar, Judit, Humphreys, Philip G., Nicholas C. O. Tomkinson (1357533), Rab K. Prinjha, Leveridge, Melanie, Samuel C. Robson (1357527), Melanie Leveridge (1357542), Gordon, Laurie, Philip G. Humphreys (1357530), Becher, Isabelle, Che, Ka Hing, Anne-Marie Michon (1343457), Chun-wa Chung (1343454), Judit Molnar (1357521), Isabelle Becher, Samuel C. Robson, Matthew Lindon, David H. Drewry, Bamborough, Paul, Lindon, Matthew, Antje Dittmann, Michon, Anne-Marie, Nicholas C. O. Tomkinson, Rino A. Bit (1357536), Tomkinson, Nicholas C. O., Paul Bamborough (1343466), Anne-Marie Michon, Paola Grandi, David H. Drewry (386307), Paul Bamborough, Gerard Drewes, Bit, Rino A., Philip G. Humphreys, Grandi, Paola, Theodoulou, Natalie H., Isabelle Becher (1357539), Drewes, Gerard, Melanie Leveridge, Bannister, Andrew J., Tony Kouzarides (17431), Andrew J. Bannister, Chung, Chun-wa, Natalie H. Theodoulou (1357545), Ka Hing Che, Laurie Gordon, Chun-wa Chung, Judit Molnar, Robson, Samuel C., Rab K. Prinjha (449759), Natalie H. Theodoulou, Antje Dittmann (1357548)   +63 more
core   +1 more source

Bromodomain-containing protein 4 knockdown promotes neuronal ferroptosis in a mouse model of subarachnoid hemorrhage

Neural Regeneration Research
Neuronal cell death is a common outcome of multiple pathophysiological processes and a key factor in neurological dysfunction after subarachnoid hemorrhage. Neuronal ferroptosis in particular plays an important role in early brain injury.
Peng Lu, Fan Zhang, Lei Yang, Yijing He, Xi Kong, Kecheng Guo, Yuke Xie, Huangfan Xie, Bingqing Xie, Yong Jiang, Jianhua Peng   +10 more
doaj   +1 more source

A Nutrient-Based Cellular Model to Characterize Acetylation-Dependent Protein-Protein Interactions

Frontiers in Molecular Biosciences, 2022
Cellular homeostasis requires the orderly expression of thousands of transcripts. Gene expression is regulated by numerous proteins that recognize post-translational modifications—in particular, the acetylation of lysine residues (Kac) on histones.
Jérémy Loehr, Jérémy Loehr, Pata-Eting Kougnassoukou Tchara, Pata-Eting Kougnassoukou Tchara, Pata-Eting Kougnassoukou Tchara, Kevin Gonthier, Kevin Gonthier, Chahinez Noufi, Chahinez Noufi, Naomie Linteau, Naomie Linteau, Étienne Audet-Walsh, Étienne Audet-Walsh, Jean-Philippe Lambert, Jean-Philippe Lambert, Jean-Philippe Lambert   +15 more
doaj   +1 more source

Drug Discovery Targeting Bromodomain-Containing Protein 4

Journal of Medicinal Chemistry, 2017
BRD4, the most extensively studied member of the BET family, is an epigenetic regulator that localizes to DNA via binding to acetylated histones and controls the expression of therapeutically important gene regulatory networks through the recruitment of transcription factors to form mediator complexes, phosphorylating RNA polymerase II, and by its ...
Zhiqing Liu, Pingyuan Wang, Haiying Chen, Eric A. Wold, Bing Tian, Allan R. Brasier, Jia Zhou   +6 more
openaire   +2 more sources

The Putative Bromodomain Protein PfBDP7 of the Human Malaria Parasite Plasmodium Falciparum Cooperates With PfBDP1 in the Silencing of Variant Surface Antigen Expression

Frontiers in Cell and Developmental Biology, 2022
Epigenetic regulation is a critical mechanism in controlling virulence, differentiation, and survival of the human malaria parasite Plasmodium (P.) falciparum.
Jennifer E. Quinn, Myriam D. Jeninga, Katharina Limm, Kapil Pareek, Tina Meißgeier, Anna Bachmann, Anna Bachmann, Anna Bachmann, Michael F. Duffy, Michaela Petter, Michaela Petter   +10 more
doaj   +1 more source