Results 31 to 40 of about 15,581 (231)

New synthetic routes to Triazolo-benzodiazepine analogues:expanding the scope of the bump-and-hole approach for selective Bromo and Extra-Terminal (BET) bromodomain inhibition [PDF]

, 2015
We describe new synthetic routes developed toward a range of substituted analogues of bromo and extra-terminal (BET) bromodomain inhibitors I-BET762/JQ1 based on the triazolo-benzodiazepine scaffold.
Alessio Ciulli, Cynthia Tallant, Enrique Lin-Shiao, Matthias G. J. Baud, Michael Zengerle, Sternbach L. H.   +5 more
core   +4 more sources

BET Bromodomain Proteins as Cancer Therapeutic Targets [PDF]

Cold Spring Harbor Symposia on Quantitative Biology, 2016
Epigenetic regulators are emerging therapeutic targets in a wide variety of human cancers. BET bromodomain proteins have been identified as key regulators of oncogenic transcription factors including MYC; therefore, their inhibition might provide a way to block these "undruggable" targets.
Shaokun, Shu, Kornelia, Polyak
openaire   +2 more sources

BET Bromodomain Inhibition of MYC -Amplified Medulloblastoma [PDF]

Clinical Cancer Research, 2014
Abstract Purpose: MYC-amplified medulloblastomas are highly lethal tumors. Bromodomain and extraterminal (BET) bromodomain inhibition has recently been shown to suppress MYC-associated transcriptional activity in other cancers. The compound JQ1 inhibits BET bromodomain-containing proteins, including BRD4.
Bandopadhayay, Pratiti, Bergthold, Guillaume, Nguyen, Brian, Schubert, Simone, Gholamin, Sharareh, Tang, Yujie, Bolin, Sara, Schumacher, Steven E, Zeid, Rhamy, Masoud, Sabran, Yu, Furong, Vue, Nujsaubnusi, Gibson, William J, Paolella, Brenton R, Mitra, Siddhartha S, Cheshier, Samuel H, Qi, Jun, Liu, Kun-Wei, Wechsler-Reya, Robert, Weiss, William A, Swartling, Fredrik J, Kieran, Mark W, Bradner, James E, Beroukhim, Rameen, Cho, Yoon-Jae   +24 more
openaire   +6 more sources

The Drug Vehicle and Solvent N-Methylpyrrolidone Is an Immunomodulator and Antimyeloma Compound

Cell Reports, 2014
N-methyl-2-pyrrolidone (NMP) is a common solvent and drug vehicle. We discovered unexpected antineoplastic and immunomodulatory activity of NMP in a cMYC-driven myeloma model.
Jake Shortt, Andy K. Hsu, Benjamin P. Martin, Karen Doggett, Geoffrey M. Matthews, Maria A. Doyle, Jason Ellul, Tina E. Jockel, Daniel M. Andrews, Simon J. Hogg, Andrea Reitsma, David Faulkner, P. Leif Bergsagel, Marta Chesi, Joan K. Heath, William A. Denny, Philip E. Thompson, Paul J. Neeson, David S. Ritchie, Grant A. McArthur, Ricky W. Johnstone   +20 more
doaj   +1 more source

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

, 2016
Acetylation of histone lysine residues is one of the most well-studied post-translational modifications of chromatin, selectively recognized by bromodomain “reader” modules.
Andrew J. Bannister, Anne-Marie Michon, Antje Dittmann, Arrowsmith C. H., Bagnyukova T. V., Bamborough P., Baud M. G. J., Borah J. C., Brand M., Bunnage M. E., Chun-wa Chung, Chung C. W., Chung C. W., Chung C. W., Chung C. W., David H. Drewry, Dawson M. A., Demont E. H., Fedorov O., Ferguson F. M., Filippakopoulos P., Filippakopoulos P., Filippalopoulos P., Fish P. V., Furdas S. D., Gardner K. E., Garnier J. M., Gentile G., Gerard Drewes, Gosmini R., Guetzoyan L., Harner M. J., Hay D. A., Hewings D. S., Hewings D. S., Hewings D. S., Hohmann A. F., Hongbin S., Isabelle Becher, Jennings L. E., Judit Molnar, Ka Hing Che, Kadoch C., Knapp S., Laurie Gordon, Mathews T. P., Matthew Lindon, McKeown M. R., McLure K. G., Melanie Leveridge, Middeljans E., Mirguet O., Mirguet O., Morinière J., Mujtaba S., Müller S., Natalie H. Theodoulou, Nicholas C. O. Tomkinson, Nicodeme E., Paola Grandi, Paul Bamborough, Philip G. Humphreys, Picaud S., Prinjha R. K., Rab K. Prinjha, Rino A. Bit, Rooney T. P. C., Samuel C. Robson, Sanchez R., Sattler S., Scotto L., Seal J., Sweis R. F., Tony Kouzarides, Vollmuth F., Yan Y., Young R. J., Zeng L., Zhang G., Zhang S.   +79 more
core   +2 more sources

An RNAi-based dimorphic genetic screen identified the double bromodomain protein BET-1 as a sumo-dependent attenuator of RAS-mediated signalling. [PDF]

PLoS ONE, 2013
Attenuation of RAS/RAF/MAPK signalling is essential to prevent hyperactivation of this oncogenic pathway. In C. elegans, the sumoylation pathway and a combination of histone tail modifications regulate gene expression to attenuate the LET-60 (RAS ...
Fiona Gee, Kate Fisher, Ulrike Klemstein, Gino B Poulin   +3 more
doaj   +1 more source

Benefit of Apabetalone on Plasma Proteins in Renal Disease. [PDF]

, 2018
Introduction:Apabetalone, a small molecule inhibitor, targets epigenetic readers termed BET proteins that contribute to gene dysregulation in human disorders. Apabetalone has in vitro and in vivo anti-inflammatory and antiatherosclerotic properties.
Gilham, Dean, Halliday, Christopher, Jahagirdar, Ravi, Johansson, Jan O, Kalantar-Zadeh, Kamyar, Kulikowski, Ewelina, Robson, Richard, Stotz, Stephanie C, Sweeney, Michael, Tsujikawa, Laura M, Wasiak, Sylwia, Wong, Norman C   +11 more
core   +2 more sources

Targeting BET Bromodomains in Cancer

Annual Review of Cancer Biology, 2022
Cancer is frequently dependent on aberrant gene expression programs that might be vulnerable to targeting with novel therapeutics. Bromodomain and extraterminal domain (BET) proteins are powerful transcriptional coregulators often found as part of oncogenic transcriptional programs. The bromodomain functionality of BET proteins is highly druggable, and
openaire   +1 more source

Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains [PDF]

Molecular Cell, 2019
Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers opportunities for therapeutic intervention in cancer and other diseases. Here, we profile the interactomes of BRD2, BRD3, BRD4, and BRDT following treatment with the pan-BET BRD inhibitor JQ1, revealing broad rewiring of the interaction landscape, with three distinct ...
Lambert, Jean-Philippe, Picaud, Sarah, Fujisawa, Takao, Hou, Huayun, Savitsky, Pavel, Uusküla-Reimand, Liis, Gupta, Gagan D, Abdouni, Hala, Lin, Zhen-Yuan, Tucholska, Monika, Knight, James D R, Gonzalez-Badillo, Beatriz, St-Denis, Nicole, Newman, Joseph A, Stucki, Manuel, Pelletier, Laurence, Bandeira, Nuno, Wilson, Michael D, Filippakopoulos, Panagis, Gingras, Anne-Claude   +19 more
openaire   +3 more sources

Bromodomain and extra-terminal domain inhibition modulates the expression of pathologically relevant microRNAs in diffuse large B-cell lymphoma

Haematologica, 2018
Aberrant changes in microRNA expression contribute to lymphomagenesis. Bromodomain and extra-terminal domain inhibitors such as OTX015 (MK-8628, birabresib) have demonstrated preclinical and clinical activity in hematologic tumors.
Afua A. Mensah, Luciano Cascione, Eugenio Gaudio, Chiara Tarantelli, Riccardo Bomben, Elena Bernasconi, Domenico Zito, Andrea Lampis, Jens C. Hahne, Andrea Rinaldi, Anastasios Stathis, Emanuele Zucca, Ivo Kwee, Valter Gattei, Nicola Valeri, Maria E Riveiro, Francesco Bertoni   +16 more
doaj   +1 more source