Results 201 to 210 of about 33,428 (239)

Cancer and the bromodomains of BAF180

Biochemical Society Transactions, 2012
Chromatin remodelling complexes alter the structure of chromatin and have central roles in all DNA-templated activities, including regulation of gene expression and DNA repair. Mutations in subunits of the PBAF (polybromo/Brg1-associated factor) or SWI/SNF-B remodelling complex, including BAF180, are frequently associated with cancer.
Brownlee, Peter M, Chambers, Anna L, Oliver, Antony W, Downs, Jessica A   +3 more
openaire   +3 more sources

The TRIM33 bromodomain recognizes histone lysine lactylation

ACS Chemical Biology
Histone lysine lactylation (Kla) regulates inflammatory gene expression in activated macrophages and mediates the polarization of inflammatory (M1) to reparative (M2) macrophages.
Raymundo Nuñez, P. Sidlowski, Erica A. Steen, Sarah L. Wynia-Smith, Daniel J. Sprague, Robert F. Keyes, Brian C. Smith   +6 more
semanticscholar   +1 more source

Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer.

Journal of Medicinal Chemistry, 2021
CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential target for prostate cancer treatment. Herein, we report the structural optimization of a series of 1-(indolizin-3-yl)ethan-1-one compounds as new selective CBP ...
Qiuping Xiang, Chao Wang, Tian Wu, Cheng Zhang, Qing-Hua Hu, Guolong Luo, Jiankang Hu, Xiaoxi Zhuang, Ling-jiao Zou, Hui Shen, Xi-shan Wu, Yan Zhang, X. Kong, Jinsong Liu, Yong Xu   +14 more
semanticscholar   +1 more source

Bromodomain motifs and scaffolding

Frontiers in Bioscience, 2001
Bromodomain-containing multiprotein complexes share some of the properties of signal transduction scaffolds. Insights from MAP kinase signaling scaffolds, for example, may provide useful perspectives for future studies of bromodomain proteins. The regulatory processes of modification (phosphorylation, acetylation, ubiquitination), turnover, nuclear ...
openaire   +2 more sources

Phase Ib Trial With Birabresib, a Small-Molecule Inhibitor of Bromodomain and Extraterminal Proteins, in Patients With Selected Advanced Solid Tumors.

Journal of Clinical Oncology, 2018
PURPOSE Birabresib (MK-8628/OTX015) is a first-in-class bromodomain inhibitor with activity in select hematologic tumors. Safety, efficacy, and pharmacokinetics of birabresib were evaluated in patients with castrate-resistant prostate cancer, nuclear ...
J. Lewin, J. Soria, A. Stathis, J. Delord, S. Peters, A. Awada, P. Aftimos, M. Békradda, K. Rezai, Z. Zeng, Azher Hussain, S. Perez, L. Siu, C. Massard   +13 more
semanticscholar   +1 more source

Bromodomain Histone Readers and Cancer

Journal of Molecular Biology, 2017
Lysine acetylation of histone proteins is a fundamental post-translational modification that regulates chromatin structure and plays an important role in gene transcription. Aberrant levels of histone lysine acetylation are associated with the development of several diseases.
Abhinav K, Jain, Michelle C, Barton
openaire   +2 more sources

BET bromodomain inhibitors in leukemia

Experimental Hematology, 2015
The last few years have seen the identification of bromodomain and extraterminal (BET) proteins as critical mediators of transcription with effects on its direct control and cisregulation. This discovery is important in furthering our understanding of the mechanisms of normal transcriptional control. Subsequent work has shed light on the multiple roles
Faisal, Basheer, Brian J P, Huntly
openaire   +2 more sources

The exploitation of FRET probes to track bromodomain/histone interactions in cells for bromodomain inhibitors

Drug Discovery Today: Technologies, 2016
Bromodomain-containing proteins are epigenetic readers of histone codes, which recognize acetylated histones and are involved in transcription, nucleosome remodeling and DNA repair. Chromosomal translocations of bromodomain-containing proteins have been implicated in many diseases. In this regard, small molecules that inhibit bromodomains are promising
Kazuki, Sasaki, Minoru, Yoshida
openaire   +2 more sources

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Nature, 2020
Emily J. Faivre, K. McDaniel, D. Albert, Srinivasa R. Mantena, J. Plotnik, Denise M. Wilcox, Lu Zhang, M. Bui, G. Sheppard, Le Wang, Vasudha Sehgal, Xiaoyu Lin, Xiaoli Huang, Xin Lu, Tamar Uziel, P. Hessler, L. Lam, Richard J. Bellin, G. Mehta, S. Fidanze, J. Pratt, Dachun Liu, Lisa A. Hasvold, Chaohong Sun, S. Panchal, J. Nicolette, S. Fossey, Chang H. Park, K. Longenecker, L. Bigelow, M. Torrent, S. Rosenberg, W. Kati, Yu Shen   +33 more
semanticscholar   +1 more source

Bromodomain inhibitors revisited

Science, 2020
Drug Discovery Bromodomain and extraterminal domain (BET) proteins contribute to the pathogenesis of cancer and immune diseases through their effects on transcriptional regulation. BET proteins contain two nearly identical bromodomains, BD1 and BD2, structural modules that have attracted great interest as targets for drug development.
openaire   +1 more source