Results 21 to 30 of about 128,101 (191)

Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer [PDF]

Molecular Cell, 2020
Henry W Long, X Shirley Liu, Jun Qi
exaly   +2 more sources

Bromodomain Blockade for Intimal Hyperplasia — A Good BET?

EBioMedicine, 2015
Atherosclerosis contributes to heart attack, stroke, and peripheral vascular disease and remains the leading cause of death in the U.S. (Tabas et al., 2015). Atherosclerotic plaques can be treated by revascularization procedures, including angioplasty, stenting, or bypass surgery, but microtrauma to the blood vessel during these procedures can lead to ...
Allison C. Ostriker, Kathleen A. Martin
doaj   +3 more sources

Selective inhibition of BET bromodomains [PDF]

Nature, 2010
Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts have been limited to chromatin modifying enzymes, or so-called epigenetic 'writers' and 'erasers'. Potent inhibitors of histone binding modules have not yet been described.
Filippakopoulos, P, Qi, J, Picaud, S, Shen, Y, Smith, W, Fedorov, O, Morse, E, Keates, T, Hickman, T, Felletar, I, Philpott, M, Munro, S, McKeown, M, Wang, Y, Christie, A, West, N, Cameron, M, Schwartz, B, Heightman, T, La Thangue, N, French, C, Wiest, O, Kung, A, Knapp, S, Bradner, J   +24 more
openaire   +4 more sources

The Functions of BET Proteins in Gene Transcription of Biology and Diseases

Frontiers in Molecular Biosciences, 2021
The BET (bromodomain and extra-terminal domain) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT, are widely acknowledged as major transcriptional regulators in biology.
Ka Lung Cheung, Claudia Kim, Ming-Ming Zhou   +2 more
doaj   +1 more source

Methylpyrrole inhibitors of BET bromodomains [PDF]

Bioorganic & Medicinal Chemistry Letters, 2017
An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments guided by structure-based design provided lead molecules with significant activity in a mouse tumor model. Further modifications to the methylpyrrole core provided compounds with improved properties and enhanced ...
Lisa A, Hasvold, George S, Sheppard, Le, Wang, Steven D, Fidanze, Dachun, Liu, John K, Pratt, Robert A, Mantei, Carol K, Wada, Robbert, Hubbard, Yu, Shen, Xiaoyu, Lin, Xiaoli, Huang, Scott E, Warder, Denise, Wilcox, Leiming, Li, F Greg, Buchanan, Lauren, Smithee, Daniel H, Albert, Terrance J, Magoc, Chang H, Park, Andrew M, Petros, Sanjay C, Panchal, Chaohong, Sun, Peter, Kovar, Nirupama B, Soni, Steven W, Elmore, Warren M, Kati, Keith F, McDaniel   +27 more
openaire   +2 more sources

Small molecule ligands of the BET-like bromodomain, SmBRD3, affect Schistosoma mansoni survival, oviposition, and development [PDF]

, 2023
Schistosomiasis is a disease affecting over 200 million people worldwide, but its treatment relies on a single agent, praziquantel. To investigate new avenues for schistosomiasis control, we have conducted the first systematic analysis of bromodomain ...
Helen, Whiteland, Karl, Hoffmann, Josephine, Forde-Thomas, Manfred, Beckmann, Stuart, Conway, Anthony, Chan, Michael, McDonough, Rosa, Cookson, Darius, McArdle, Gilda, Padalino, Matthias, Schiedel   +10 more
core   +2 more sources

Two bromodomain proteins functionally interact to recapitulate an essential BRDT-like function in Drosophila spermatocytes [PDF]

Open Biology, 2015
In mammals, the testis-specific bromodomain and extra terminal (BET) protein BRDT is essential for spermatogenesis. In Drosophila, it was recently reported that the tBRD-1 protein is similarly required for male fertility.
Shuhei Kimura, Benjamin Loppin
doaj   +1 more source

Dihydropyridine Lactam Analogs Targeting BET Bromodomains

ChemMedChem, 2021
AbstractInhibitors of Bromodomain and Extra Terminal (BET) proteins are investigated for various therapeutic indications, but selectivity for BRD2, BRD3, BRD4, BRDT and their respective tandem bromodomains BD1 and BD2 remains suboptimal. Here we report selectivity‐focused structural modifications of previously reported dihydropyridine lactam 6 by ...
Jiewei Jiang, Logan H. Sigua, Alice Chan, Prakriti Kalra, William C.K. Pomerantz, Ernst Schönbrunn, Jun Qi, Gunda I. Georg   +7 more
openaire   +4 more sources

Binding hotspots of BAZ2B bromodomain:histone interaction revealed by solution NMR driven docking [PDF]

, 2014
Bromodomains are epigenetic reader domains, which have come under increasing scrutiny both from academic and pharmaceutical research groups. Effective targeting of the BAZ2B bromodomain by small molecule inhibitors has been recently reported, but no ...
Ferguson, Fleur M., Alexandre M. J. J. Bonvin (18079), Alexandre M. J. J. Bonvin, João P. G. L. M. Rodrigues (1312506), Wienk, Hans, Fleur M. Ferguson (1304613), Rolf Boelens (18078), Alessio Ciulli, Boelens, Rolf, NMR Spectroscopy, Chris Abell, Fleur M. Ferguson, Garcia Lopes Maia Rodrigues, João, Rodrigues, João P. G. L. M., David M. Dias, Bonvin, Alexandre M. J. J., Sub NMR Spectroscopy, Dias, David M., João P. G. L. M. Rodrigues, David M. Dias (1340694), Rolf Boelens, Abell, Chris, Hans Wienk (684663), Ciulli, Alessio, Hans Wienk, Chris Abell (197099), Alessio Ciulli (762789)   +26 more
core   +3 more sources

BET inhibitor suppresses migration of human hepatocellular carcinoma by inhibiting SMARCA4

Scientific Reports, 2021
Hepatocellular carcinoma (HCC) is one of the most prevalent and poorly responsive cancers worldwide. Bromodomain and extraterminal (BET) inhibitors, such as JQ1 and OTX-015, inhibit BET protein binding to acetylated residues in histones.
Hae In Choi, Ga Yeong An, Mina Baek, Eunyoung Yoo, Jin Choul Chai, Young Seek Lee, Kyoung Hwa Jung, Young Gyu Chai   +7 more
doaj   +1 more source