Results 31 to 40 of about 37,262 (190)

Blocking the Bromodomains Function Contributes to Disturbances in Alga Chara vulgaris Spermatids Differentiation

Cells, 2020
Bromodomain containing (BRD) proteins play an essential role in many cellular processes. The aim of this study was to estimate activity of bromodomains during alga Chara vulgaris spermatids differentiation. The effect of a bromodomain inhibitor, JQ1 (100
Agnieszka Wojtczak
doaj   +1 more source

Bromodomain biology and drug discovery [PDF]

Nature Structural & Molecular Biology, 2019
The bromodomain (BrD) is a conserved structural module found in chromatin- and transcription-associated proteins that acts as the primary reader for acetylated lysine residues. This basic activity endows BrD proteins with versatile functions in the regulation of protein-protein interactions mediating chromatin-templated gene transcription, DNA ...
Nilesh Zaware, Ming-Ming Zhou
openaire   +2 more sources

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
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Selective inhibition of BET bromodomains [PDF]

Nature, 2010
Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts have been limited to chromatin modifying enzymes, or so-called epigenetic 'writers' and 'erasers'. Potent inhibitors of histone binding modules have not yet been described.
Filippakopoulos, P, Qi, J, Picaud, S, Shen, Y, Smith, W, Fedorov, O, Morse, E, Keates, T, Hickman, T, Felletar, I, Philpott, M, Munro, S, McKeown, M, Wang, Y, Christie, A, West, N, Cameron, M, Schwartz, B, Heightman, T, La Thangue, N, French, C, Wiest, O, Kung, A, Knapp, S, Bradner, J   +24 more
openaire   +4 more sources

Current Understanding of the Role of the Brd4 Protein in the Papillomavirus Lifecycle

Viruses, 2013
The Brd4 protein is an epigenetic reader that is central to regulation of cellular transcription and mitotic bookmarking. The transcription and replication proteins of many viruses interact with Brd4.
Moon Kyoo Jang, Alison A. McBride
doaj   +1 more source

An update on the potential for male contraception : emerging options [PDF]

, 2013
The human population continues to grow and is estimated to rise to 10.1 billion by the end of the century. Therefore, there is still an unmet need for safe and highly effective contraceptive options for both men and women.
Alsaadi, Manal, Ferro, Valerie, Garside, Deborah A, Gebril, Ayman M, Mullen, Alexander, Nimmo, Natalie   +5 more
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Methylpyrrole inhibitors of BET bromodomains [PDF]

Bioorganic & Medicinal Chemistry Letters, 2017
An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments guided by structure-based design provided lead molecules with significant activity in a mouse tumor model. Further modifications to the methylpyrrole core provided compounds with improved properties and enhanced ...
Lisa A, Hasvold, George S, Sheppard, Le, Wang, Steven D, Fidanze, Dachun, Liu, John K, Pratt, Robert A, Mantei, Carol K, Wada, Robbert, Hubbard, Yu, Shen, Xiaoyu, Lin, Xiaoli, Huang, Scott E, Warder, Denise, Wilcox, Leiming, Li, F Greg, Buchanan, Lauren, Smithee, Daniel H, Albert, Terrance J, Magoc, Chang H, Park, Andrew M, Petros, Sanjay C, Panchal, Chaohong, Sun, Peter, Kovar, Nirupama B, Soni, Steven W, Elmore, Warren M, Kati, Keith F, McDaniel   +27 more
openaire   +2 more sources

A Novel t(8;14)(q24;q11) Rearranged Human Cell Line as a Model for Mechanistic and Drug Discovery Studies of NOTCH1-Independent Human T-Cell Leukemia [PDF]

, 2018
MYC-translocated T-lineage acute lymphoblastic leukemia (T-ALL) is a rare subgroup of T-ALL associated with CDKN2A/B deletions, PTEN inactivation, and absence of NOTCH1 or FBXW7 mutations.
Amadori, Alberto, Bongiovanni, Deborah, Buldini, Barbara, Macri, Nadia, Martines, Annalisa, Matthijssens, Filip, Milani, Gloria, Minuzzo, Sonia, Piovan, Erich, Schumacher, Richard Fabian, Tosello, Valeria, Van Loocke, Wouder, Van Vlierberghe, Pieter   +12 more
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Application of Small Epigenetic Modulators in Pediatric Medulloblastoma [PDF]

, 2018
Medulloblastoma is one of the most frequent among pediatric brain tumors, and it has been classified in various subgroups. Some of them already benefit from quite good therapeutic options, whereas others urgently need novel therapeutic approaches ...
Annalisa Romanelli, Antonello Mai, Antonello Mai, Clemens Zwergel, Giulia Stazi, Giuseppina Catanzaro, Marco Tafani, Sergio Valente, Zein Mersini Besharat   +8 more
core   +2 more sources

Epigenetic roulette in blood stream plasmodium: gambling on sex [PDF]

, 2016
No abstract ...
Waters, Andrew
core   +7 more sources