Results 101 to 110 of about 128,101 (191)

JQ1 affects BRD2-dependent and independent transcription regulation without disrupting H4-hyperacetylated chromatin states

Epigenetics, 2018
The bromodomain and extra-terminal domain (BET) proteins are promising drug targets for cancer and immune diseases. However, BET inhibition effects have been studied more in the context of bromodomain-containing protein 4 (BRD4) than BRD2, and the BET ...
Lusy Handoko, Bogumil Kaczkowski, Chung-Chau Hon, Marina Lizio, Masatoshi Wakamori, Takayoshi Matsuda, Takuhiro Ito, Prashanti Jeyamohan, Yuko Sato, Kensaku Sakamoto, Shigeyuki Yokoyama, Hiroshi Kimura, Aki Minoda, Takashi Umehara   +13 more
doaj   +1 more source

A Novel BD2-Selective Inhibitor of BRDs Mitigates ROS Production and OA Pathogenesis

Antioxidants
Bromodomain and extra-terminal domain (BET) family proteins regulate transcription and recognize lysine residues in histones. Selective BET inhibitors targeting one domain have attracted attention because they maintain normal physiological activities ...
Hyemi Lee, Jihye Choe, Min-Hee Son, In-Hyun Lee, Min Ju Lim, Jimin Jeon, Siyoung Yang   +6 more
doaj   +1 more source

BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability [PDF]

, 2018
Ligands for the bromodomain and extra-terminal domain (BET) family of bromodomains have shown promise as useful therapeutic agents for treating a range of cancers and inflammation.
Guzanov, Pavel, Stazi, G, Mapp, AK, Humphreys, PG, Filippakopoulos, P, Hicks, A, Laurin, CMC, Picaud, Sarah, Conway, Stuart J., Larissa See, Clayton, J, Moroglu, Mustafa, Reynolds, JK, Scorah, AR, Mustafa Moroglu, Ester M. Hammond, Laurin, Corentin M.C., See, L, Paul A. Bruno, Jessica K. Reynolds, Joseph P. Bluck, Amy R. Scorah, Scorah, Amy R., Philip C. Biggin, Moroglu, M, Hammond, EM, Laura E. Jennings, Evans, CNG, Giulia Stazi, Evans, Charles N.G., James Clayton, Amy Hicks, Sarah Picaud, Ishna N. Mistry, Anna K. Mapp, Corentine M.C. Laurin, Panagis Filippakopoulos, Bluck, Joseph P., Mistry, IN, Charles N.G. Evans, Biggin, PC, Matthias Schiedel, Pavel Guzanov, David S. Hewings, Hewings, DS, Bruno, PA, Philip G. Humphreys, Guzanov, P, Jennings, LE, Bluck, JP, Biggin, Philip C., Filippakopoulos, Panagiotis, Schiedel, M, Picaud, S, Stuart J. Conway, Conway, SJ, Reynolds, Jessica K.   +56 more
core   +1 more source

Selective BET bromodomain inhibition as an antifungal therapeutic strategy

Nature Communications, 2017
BET proteins bind chromatin through their bromodomains (BDs) to regulate transcription and chromatin remodelling. Here, the authors show that the BET protein Bdf1 is essential for the fungal pathogenCandida albicans, and report compounds that inhibit the
Flore Mietton, Elena Ferri, Morgane Champleboux, Ninon Zala, Danièle Maubon, Yingsheng Zhou, Mike Harbut, Didier Spittler, Cécile Garnaud, Marie Courçon, Murielle Chauvel, Christophe d’Enfert, Boris A. Kashemirov, Mitchell Hull, Muriel Cornet, Charles E. McKenna, Jérôme Govin, Carlo Petosa   +17 more
doaj   +1 more source

Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition

iScience
Summary: Combinatorial signaling by proinflammatory cytokines synergizes to exacerbate toxicity to cells and tissue injury during acute infections. To explore synergism at the gene-regulatory level, we investigated the dynamics of transcription and ...
Ronan C. Bracken, Lindsay M. Davison, Dennis P. Buehler, Maci E. Fulton, Emily E. Carson, Quanhu Sheng, Lindsey K. Stolze, Christelle Guillermier, Matthew L. Steinhauser, Jonathan D. Brown   +9 more
doaj   +1 more source

Targeting BET Bromodomains in Recalcitrant Cancers [PDF]

, 2017
Pancreatic and lung cancers have some of the worst five-year survival rates of all malignancies. These aggressive cancers are often diagnosed as metastatic disease and are refractory to therapeutic interventions. Driving mutations in these diseases are often therapeutic targets, but cancer cells evade death by circumventing the pathways targeted by ...
openaire   +1 more source

The Development and Evaluation of a Novel Highly Selective PET Radiotracer for Targeting BET BD1

Pharmaceuticals
Background/Objectives: Small molecules that interfere with the interaction between acetylated protein tails and the tandem bromodomains of BET (bromodomain and extra-terminal) family proteins are pivotal in modulating immune/inflammatory and neoplastic ...
Yanli Wang, Yongle Wang, Yulong Xu, Leyi Kang, Darcy Tocci, Changning Wang   +5 more
doaj   +1 more source

BET bromodomain proteins [PDF]

Science-Business eXchange, 2014
openaire   +3 more sources

Metabolic rewiring in MYC-driven medulloblastoma by BET-bromodomain inhibition. [PDF]

Sci Rep, 2023
Graziani V, Garcia AR, Alcolado LS, Le Guennec A, Henriksson MA, Conte MR.   +5 more
europepmc   +1 more source

Rationally designed chimeric PI3K-BET bromodomain inhibitors elicit curative responses in MYC-driven lymphoma. [PDF]

Proc Natl Acad Sci U S A, 2023
Oh DH, Ma X, Hogg SJ, He J, Kearney C, Brasacchio D, Susanto O, Maher B, Jennings IG, Newbold A, Fraser P, Gruber E, Kats LM, Gregory GP, Johnstone RW, Thompson PE, Shortt J.   +16 more
europepmc   +1 more source