Results 11 to 20 of about 56,924 (160)

A Comprehensive Review of BET Protein Biochemistry, Physiology, and Pathological Roles

Frontiers in Pharmacology, 2022
Epigenetic modifications, specifically acetylation of histone plays a decisive role in gene regulation and transcription of normal cellular mechanisms and pathological conditions.
Hafiz Akbar Ali, Hafiz Akbar Ali, Yalan Li, Akram Hafiz Muhammad Bilal, Tingting Qin, Ziqiao Yuan, Wen Zhao, Wen Zhao   +7 more
doaj   +1 more source

BET Inhibitors Synergize with Carfilzomib to Induce Cell Death in Cancer Cells via Impairing Nrf1 Transcriptional Activity and Exacerbating the Unfolded Protein Response

Biomolecules, 2020
Currently, proteasome inhibitors bortezomib, carfilzomib, and ixazomib are successfully used in clinics to treat multiple myeloma. However, these agents show limited efficacy against solid tumors. Identification of drugs that can potentiate the action of
Janakiram R. Vangala, Ajay Potluri, Senthil K. Radhakrishnan   +2 more
doaj   +1 more source

Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection

Microbiology Spectrum, 2022
African swine fever (ASF), an acute, severe, highly contagious disease caused by African swine fever virus (ASFV) infection in domestic pigs and boars, has a mortality rate of up to 100%.
Yaru Zhao, Qingli Niu, Saixia Yang, Jifei Yang, Zhonghui Zhang, Shuxian Geng, Jie Fan, Zhijie Liu, Guiquan Guan, Zhiqing Liu, Jia Zhou, Haitao Hu, Jianxun Luo, Hong Yin   +13 more
doaj   +1 more source

Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases

Pharmaceuticals, 2022
BET proteins, which recognize and bind to acetylated histones, play a key role in transcriptional regulation. The development of chemical BET inhibitors in 2010 greatly facilitated the study of these proteins.
Dayu Wu, Qiong Duan
doaj   +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

BET bromodomain protein inhibition is a therapeutic option for medulloblastoma [PDF]

, 2013
Medulloblastoma is the most common malignant brain tumor of childhood, and represents a significant clinical challenge in pediatric oncology, since overall survival currently remains under 70%.
Althof, Kristina, Beckers, Anneleen, Eggert, Angelika, El-Hindy, Nicolai, Fleischhack, Gudrun, Henssen, Anton, Heukamp, Lukas, Odersky, Andrea, Schramm, Alexander, Schulte, Johannes H, Schäfers, Simon, Speleman, Franki, Sure, Ulrich, Thor, Theresa   +13 more
core   +4 more sources

Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer [PDF]

, 2014
Triple-negative breast cancer (TNBC) is a heterogeneous and clinically aggressive disease for which there is no targeted therapy. BET bromodomain inhibitors, which have shown efficacy in several models of cancer have not been evaluated in TNBC.
Anders, Lars, Barry, William T., Bradner, James, Brown, Jonathan, Brown, Myles, Carroll, Jason S., Chiang, Cheng-Ming, Dillon, Deborah, Doherty, Ernest, Duarte, Melissa, D’Santos, Clive, Ekram, Muhammad B., Guo, Hao, He, Housheng Hansen, Janiszewska, Michalina, Jin Huh, Sung, Krop, Ian E., Letai, Antony, Liang, Yi, Lin, Charles Y., Liu, X. Shirley, Long, Henry W., McKeown, Michael, Meyer, Clifford A., Mohammed, Hisham, Ni, Min, Ott, Christopher, Peluffo, Guillermo, Polyak, Kornelia, Qi, Jun, Rao, Prakash K., Roberts, Justin M., Ryan, Jeremy, Shu, Shaokun, Stover, Daniel G., Tabassum, Doris P., Winer, Eric P., Witwicki, Robert M., Wu, Shwu-Yuan, Young, Richard A.   +39 more
core   +1 more source

Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells. role of cMYC-IRF4-miR-125b interplay [PDF]

, 2016
Background: Anticancer immune responses may contribute to the control of tumors after conventional chemotherapy and different observations have indicated that chemotherapeutic agents can induce immune responses resulting in cancer cell death and immune ...
Abruzzese, MARIA PIA, Bilotta, MARIA TERESA, Borrelli, Cristiana, Cippitelli, Marco, Fionda, Cinzia, Molfetta, Rosa, Paolini, Rossella, Petrucci, MARIA TERESA, Ricciardi, Maria Rosaria, Santoni, Angela, Soriani, Alessandra, Vulpis, Elisabetta, Zingoni, Alessandra, Zitti, Beatrice   +13 more
core   +13 more sources

Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction

Nature Communications, 2020
Inhibitors of the BET family proteins are limited by their potency and oral bio-availability. Here, the authors report a new BET inhibitor, NHWD-870, with improved potency compared to previous BET inhibitors, and show that it suppresses BRD4 and targets ...
Mingzhu Yin, Ying Guo, Rui Hu, Wesley L. Cai, Yao Li, Shiyao Pei, Hongyin Sun, Cong Peng, Jiali Li, Rui Ye, Qiaohong Yang, Nenghui Wang, Yongguang Tao, Xiang Chen, Qin Yan   +14 more
doaj   +1 more source

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