Results 11 to 20 of about 27,094 (219)

Bromodomain Proteins in HIV Infection [PDF]

Viruses, 2013
Bromodomains are conserved protein modules of ~110 amino acids that bind acetylated lysine residues in histone and non-histone proteins. Bromodomains are present in many chromatin-associated transcriptional regulators and have been linked to diverse aspects of the HIV life cycle, including transcription and integration.
Ott, Melanie, Boehm, D, Conrad, RJ
openaire   +7 more sources

CBP/p300 bromodomain: new promising epigenetic target [PDF]

Visualized Cancer Medicine, 2022
CREB (cAMP responsive element binding protein) binding protein (CBP) and adenovirus E1A-associated 300 kDa protein (p300) are histone acetyltransferases, which are necessary for multiple cellular processes.
Xiang Qiuping, Zhou Yang, Zhang Yan, Xu Yong   +3 more
doaj   +3 more sources

Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N‑Terminal Bromodomain Chemical Probe [PDF]

, 2023
Small-molecule-mediated disruption of the protein–protein interactions between acetylated histone tails and the tandem bromodomains of the bromodomain and extra-terminal (BET) family of proteins is an important mechanism of action for the potential ...
Christopher R. Wellaway (7148462), Peter D. Craggs (7180412), Inmaculada Rioja (8539), Marc Reid (1695424), David S. Palmer (1328991), Ian D. Wall (2525425), Lucia Fusani (4578958), Emmanuel H. Demont (1399288), Rosa Cookson (2588734), Philip G. Humphreys (1357530), William J. Kerr (1267110), Erin Bradley (1436305), Alex Phillipou (8551068), Chun-wa Chung (1343454), Darren J. Mitchell (1343451), Rishi R. Shah (8232807), Rab K. Prinjha (449759)   +16 more
core   +6 more sources

Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition [PDF]

Journal for ImmunoTherapy of Cancer, 2019
Background Prostate cancer responds poorly to current immunotherapies. Epigenetic therapies such as BET Bromodomain inhibition can change the transcriptome of tumor cells, possibly making them more immunogenic and thus susceptible to immune targeting ...
Wendy Mao, Ali Ghasemzadeh, Zachary T. Freeman, Aleksandar Obradovic, Matthew G. Chaimowitz, Thomas R. Nirschl, Emily McKiernan, Srinivasan Yegnasubramanian, Charles G. Drake   +8 more
doaj   +2 more sources

Differential Water Networks Guide Selectivity Optimization of a Cell Active BPTF Inhibitor in Neuroblastoma. [PDF]

Angew Chem Int Ed Engl
BZ2 is a second‐generation Bromodomain PHD finger Transcription Factor (BPTF) inhibitor with improved selectivity over Class I and Class IV BRD off‐targets identified in our previously reported inhibitor, BZ1. Structural analyses reveal that water network engagement is key to this selectivity.
Babu K, Tsou CJ, Das S, Fan L, Pal A, Sneddon M, Stachowski TR, Samanta P, Nithianantham S, Buchholz C, Zhang S, Fu X, Kathayat RS, Lin W, Li Y, Yang L, Chen T, Fischer M, Shelat AA, Pomerantz WCK.   +19 more
europepmc   +3 more sources

A Minireview on BET Inhibitors: Beyond Bromodomain Targeting

Biomedicines
Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers that recognize the histone acetylation code and play a critical role in regulating gene transcription.
Mikhail S. Iudin, Yuri M. Khodarovich, Anna M. Varizhuk, Vladimir B. Tsvetkov, Vyacheslav V. Severov   +4 more
doaj   +2 more sources

Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader [PDF]

, 2021
Targeted protein degradation is a powerful induced-proximity tool to control cellular concentrations of native proteins using small molecules. However, the design of selectivity in protein degradation remains challenging.
Huda, Zahid, Dan, Harki, Anand, Divakaran, Taosheng, Chen, Wenwei , Lin, william, pomerantz   +5 more
core   +1 more source

Design of Class I/IV Bromodomain-Targeting Degraders for Chromatin Remodeling Complexes [PDF]

, 2022
Targeted protein degradation is an emerging technology that can be used for modulating the activity of epigenetic protein targets. Among bromodomain-containing proteins, a number of degraders for the BET family have been developed while non-BET ...
Marisa, Actis, Huda, Zahid, Jeff, Costello, William, Pomerantz, Jennifer, Kimbrough, Zoran, Rankovic   +5 more
core   +2 more sources

The BET inhibitor apabetalone decreases neuroendothelial proinflammatory activation in vitro and in a mouse model of systemic inflammation

Translational Neuroscience, 2023
Brain vascular inflammation is characterized by endothelial activation and immune cell recruitment to the blood vessel wall, potentially causing a breach in the blood – brain barrier, brain parenchyma inflammation, and a decline of cognitive function ...
Wasiak Sylwia, Fu Li, Daze Emily, Gilham Dean, Rakai Brooke D., Stotz Stephanie C., Tsujikawa Laura M., Sarsons Chris D., Studer Deborah, Rinker Kristina D., Jahagirdar Ravi, Wong Norman C. W., Sweeney Michael, Johansson Jan O., Kulikowski Ewelina   +14 more
doaj   +1 more source

Genome-wide analysis of bromodomain gene family in Arabidopsis and rice

Frontiers in Plant Science, 2023
The bromodomain-containing proteins (BRD-proteins) belongs to family of ‘epigenetic mark readers’, integral to epigenetic regulation. The BRD-members contain a conserved ‘bromodomain’ (BRD/BRD-fold: interacts with acetylated-lysine in histones), and ...
T. V. Abiraami, Ravi Prakash Sanyal, Hari Sharan Misra, Hari Sharan Misra, Ajay Saini, Ajay Saini   +5 more
doaj   +1 more source