Results 111 to 120 of about 128,101 (191)

Cancer Differentiating Agent Hexamethylene Bisacetamide Inhibits BET Bromodomain Proteins

, 2016
Agents that trigger cell differentiation are highly efficacious in treating certain cancers, but such approaches are not generally effective in most malignancies.
Demir, Dagsu,, Welin, M., Walse, B., Nilsson, Lisa M,, Muralidharan, Somsundar Veppil,, Green, Lydia C.,, Logan, D. T., Nilsson, Jonas A,, Bhadury, Joydeep,   +8 more
core   +1 more source

BET Bromodomain Degradation Disrupts Function but Not 3D Formation of RNA Pol2 Clusters. [PDF]

Pharmaceuticals (Basel), 2023
Chin DH, Osman I, Porch J, Kim H, Buck KK, Rodriguez J, Carapia B, Yan D, Moura SB, Sperry J, Nakashima J, Altman K, Altman D, Gryder BE.   +13 more
europepmc   +1 more source

Bromodomain-containing protein 4 in inflammatory diseases: molecular mechanisms and therapeutic potential

Journal of Inflammation
Bromodomain-containing protein 4 (BRD4), a key member of the bromodomain and extra-terminal (BET) family, plays a critical role in regulating gene expression as an epigenetic reader.
Rachele Frascatani, Irene Marafini, Marco Colella, Giovanni Monteleone   +3 more
doaj   +1 more source

Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment In Vitro and In Vivo. [PDF]

Mol Cancer Ther, 2023
Jonchere B, Williams J, Zindy F, Liu J, Robinson S, Farmer DM, Min J, Yang L, Stripay JL, Wang Y, Freeman BB, Yu J, Shelat AA, Rankovic Z, Roussel MF.   +14 more
europepmc   +1 more source

BET bromodomain [PDF]

Science-Business eXchange, 2013
openaire   +1 more source

Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. [PDF]

J Med Chem, 2021
Karim RM, Bikowitz MJ, Chan A, Zhu JY, Grassie D, Becker A, Berndt N, Gunawan S, Lawrence NJ, Schönbrunn E.   +9 more
europepmc   +1 more source

Sensitization of Resistant Cells with a BET Bromodomain Inhibitor in a Cell Culture Model of Deep Intrinsic Resistance in Breast Cancer. [PDF]

Cancers (Basel), 2023
Singh B, Sarli VN, Milligan RD, Kinne HE, Shamsnia A, Washburn LJ, Addanki S, Lucci A.   +7 more
europepmc   +1 more source

Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity. [PDF]

J Med Chem, 2022
Guan X, Cheryala N, Karim RM, Chan A, Berndt N, Qi J, Georg GI, Schönbrunn E.   +7 more
europepmc   +1 more source

Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor

, 2018
We report the structure-based discovery of CF53 (28) as a highly potent and orally active inhibitor of bromodomain and extra-terminal (BET) proteins. By the incorporation of a NH-pyrazole group into the 9H-pyrimido­[4,5-b]­indole core, we identified a ...
Jeanne A. Stuckey (632892), Donna McEachern (573068), Xiaoqin Li (1399105), Bing Zhou (168418), Angelo Aguilar (573070), Chao-Yie Yang (695092), Yang Hu (315392), Xu Ran (382624), Jeff W. Kampf (1537393), Ting Zhao (434093), Bo Wen (207648), Longchuan Bai (387425), Liu Liu (512237), Shaomeng Wang (88290), Jennifer L. Meagher (1669465), Yujun Zhao (216850), Sally Przybranowski (3860143), Siwei Li (144874), Duxin Sun (501117), Mi Wang (2476957)   +19 more
core   +1 more source

Distinct modulation of IFNγ-induced transcription by BET bromodomain and catalytic P300/CBP inhibition in breast cancer. [PDF]

Clin Epigenetics, 2022
Hogg SJ, Motorna O, Kearney CJ, Derrick EB, House IG, Todorovski I, Kelly MJ, Zethoven M, Bromberg KD, Lai A, Beavis PA, Shortt J, Johnstone RW, Vervoort SJ.   +13 more
europepmc   +1 more source