Results 121 to 130 of about 33,428 (239)

Disulfide bridge formation influences ligand recognition by the ATAD2 bromodomain

, 2019
The ATPase family, AAA domain-containing protein 2 (ATAD2) has a C-terminal bromodomain, which functions as a chromatin reader domain recognizing acetylated lysine on the histone tails within the nucleosome. ATAD2 is overexpressed in many cancers and its
Eckenroth, Brian E, Evans, Chiara M, Lloyd, Jonathan T, Gay, Jamie C, Langini, Cassiano, Glass, Karen C; https://orcid.org/, Caflisch, Amedeo, Carlson, Samuel   +7 more
core   +1 more source

BET bromodomain inhibition suppresses innate inflammatory and profibrotic transcriptional networks in heart failure

Science Translational Medicine, 2017
BET bromodomain inhibition treats heart failure by blocking innate inflammatory and profibrotic gene networks. BETting on a new heart failure treatment Heart failure remains a common and difficult-to-treat medical condition with a high mortality, and ...
Qiming Duan, Sarah McMahon, Priti Anand, Hirsh Shah, Sean Thomas, Hazel T. Salunga, Yu Huang, Rongli Zhang, A. Sahadevan, M. Lemieux, Jonathan D. Brown, D. Srivastava, J. Bradner, T. McKinsey, Saptarsi M. Haldar   +14 more
semanticscholar   +1 more source

Targeting STAT5 in Hematologic Malignancies through Inhibition of the Bromodomain and Extra-Terminal (BET) Bromodomain Protein BRD2

, 2014
The transcription factor signal STAT5 is constitutively activated in a wide range of leukemias and lymphomas, and drives the expression of genes necessary for proliferation, survival, and self-renewal.
Wadleigh, Martha, Frank, David, Toniolo, P. A., Walker, Sarah, Qi, Jun, Stone, Richard, Bradner, James E, Cerulli, R., Nelson, Erik, Liu, Suhu, Xiang, Michael   +10 more
core   +1 more source

Biased Multicomponent Reactions to Develop Novel Bromodomain Inhibitors [PDF]

, 2015
BET bromodomain inhibition has contributed new insights into gene regulation and emerged as a promising therapeutic strategy in cancer. Structural analogy of early methyl-triazolo BET inhibitors has prompted a need for structurally dissimilar ligands as ...
Zhang, Zijuan, Wei Zhang (405), Jun Qi (128861), Huang, Yibo, Stephen C Blacklow (1343160), Fu, Harry, Asha Kadam (1343175), Zijuan Zhang (1343181), Marineau, Jason J, Xiang Xu (141229), James E Bradner (1343172), Bradner, James E, Xiaofeng Zhang (172446), Xu, Xiang, Yibo Huang (1343157), Liu, Shuai, Harry Fu (1343163), Zhang, Wei, Zhang, Xiaofeng, Shuai Liu (145969), Jason J Marineau (1343154), Dennis L Buckley (1343178), Shaw, Daniel L, Buckley, Dennis L, Michael R McKeown (1343166), Daniel L Shaw (1343169), Qi, Jun, Kadam, Asha, McKeown, Michael R, Blacklow, Stephen   +29 more
core   +1 more source

Bromodomain Proteins Contribute to Maintenance of Bloodstream Form Stage Identity in the African Trypanosome.

PLoS Biology, 2015
Trypanosoma brucei, the causative agent of African sleeping sickness, is transmitted to its mammalian host by the tsetse. In the fly, the parasite's surface is covered with invariant procyclin, while in the mammal it resides extracellularly in its ...
Danae Schulz, Monica R Mugnier, Eda-Margaret Paulsen, Hee-Sook Kim, Chun-wa W Chung, David F Tough, Inmaculada Rioja, Rab K Prinjha, F Nina Papavasiliou, Erik W Debler   +9 more
doaj   +1 more source

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

Nature Chemical Biology, 2018
The addressable pocket of a protein is often not functionally relevant in disease. This is true for the multidomain, bromodomain-containing transcriptional regulator TRIM24.
Lara N. Gechijian, Dennis L. Buckley, Matthew A. Lawlor, Jaime M. Reyes, Joshiawa Paulk, Christopher J. Ott, Georg E. Winter, Michael A. Erb, Thomas G. Scott, Mousheng Xu, H. Seo, S. Dhe-Paganon, Nicholas Kwiatkowski, J. Perry, J. Qi, N. Gray, J. Bradner   +16 more
semanticscholar   +1 more source

New home for bromodomains [PDF]

Science-Business eXchange, 2012
Researchers at Dana-Farber and the Baylor College of Medicine have shown that Tensha's bromodomain inhibitors could prevent sperm production and be developed as a male contraceptive. The biotech, which is focused on developing the molecules for cancer, has exclusive rights to the findings and is interested in pursuing bromodomain inhibitors in the ...
openaire   +1 more source

A novel carboxamide bromodomain inhibitor attenuates osteoarthritis via epigenetic repression of NF-κB and MAPK signaling

Frontiers in Immunology
Bromodomains are epigenetic readers that modulate gene expression linked to inflammation and cartilage degeneration. Emerging evidence suggests their dysregulation plays a pivotal role in osteoarthritis (OA) pathogenesis, making them promising ...
Hyemi Lee, Seong Jae Han, Subin Ok, Kwang Min Lee, Seungseok Choi, Injoo Yoon, Somang Choi, Jina Kim, Serim Ryu, Min-Hee Son, In-Hyun Lee, Chanmi Cho, Siyoung Yang   +12 more
doaj   +1 more source

Identification of Novel Bromodomain-Containing Protein 4 (BRD4) Binders through 3D Pharmacophore-Based Repositioning Screening Campaign

Molecules
A 3D structure-based pharmacophore model built for bromodomain-containing protein 4 (BRD4) is reported here, specifically developed for investigating and identifying the key structural features of the (+)-JQ1 known inhibitor within the BRD4 binding site.
Ester Colarusso, Erica Gazzillo, Eleonora Boccia, Stefania Terracciano, Ines Bruno, Giuseppe Bifulco, Maria Giovanna Chini, Gianluigi Lauro   +7 more
doaj   +1 more source

Structural insights into the recognition of mono- and di-acetylated histones by the ATAD2B bromodomain

, 2018
Bromodomains are chromatin reader modules that recognize acetylated lysine. Different bromodomains exhibit a preference for specific patterns of lysine acetylation marks on core and variant histone proteins, however, the functional relationships that ...
Samuel Carlson, Margaret Phillips, Michael-Christopher Keogh, Cong Gao, Kyle McLaughlin, Andrea Dest, Jonathan T. Lloyd, Chiara M. Evans, John L. Markley, Gabriel Cornilescu, Samuel P. Boyson, Karen C. Glass, Mulu Y. Lubula, Jamie C. Gay, Marco Tonelli, Seth Frietze, Matthew R. Marunde   +16 more
core   +1 more source