Results 41 to 50 of about 33,428 (239)

Identification of a BAZ2A-Bromodomain Hit Compound by Fragment Growing [PDF]

, 2022
BAZ2A is an epigenetic regulator affecting transcription of ribosomal RNA. It is overexpressed in aggressive and recurrent prostate cancer, promoting cellular migration. Its bromodomain is characterized by a shallow and difficult-to-drug pocket. Here, we
Spiliotopoulos, Dimitrios, Corsi, Jessica, Cazzanelli, Giulia, Caflisch, Amedeo; https://orcid.org/, Batiste, Laurent, Dalle Vedove, Andrea, Marchand, Jean-Rémy; https://orcid.org/, D'Agostino, Vito Giuseppe, Lolli, Graziano; https://orcid.org/   +8 more
core   +1 more source

Rational design and development of selective BRD7 bromodomain inhibitors and their activity in prostate cancer

, 2023
Bromodomain-containing proteins are readers of acetylated lysine and play important roles in cancer. Bromo-domain-containing protein 7 (BRD7) has been implicated in multiple malignancies; however, there are no selective chemical probes to study its ...
Sandra, Ordonez, Surbhi, Sood, Alexander, McQuade, Brian , Smith, Sijie, Wang, Emily, Dykhuizen, Brayden, Strohmier, Chad, Maschinot   +7 more
core   +1 more source

Bromodomain dimers: A case study of BRD4 and family-wide AlphaFold predictions [PDF]

Structural Dynamics
Bromodomains are conserved acetyl-lysine reader domains that play a central role in the assembly of transcriptional regulatory complexes. While generally presumed to function as monomers, bromodomain homo-dimers have been identified, and several ...
Alisa S. Dengler, Lara Lunglmeir, Matthias J. Brandl, T. Reid Alderson   +3 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

Discovery and characterization of bromodomain 2–specific inhibitors of BRDT

Proceedings of the National Academy of Sciences of the United States of America, 2021
Significance There is no nonhormonal contraceptive pill for men, although hundreds of genes have been identified to play roles during spermatogenesis and fertilization in the male reproductive tract. To address the absence of contraceptive drugs for men,
Zhifeng Yu, A. Ku, J. Anglin, Rajesh Sharma, M. N. Ucisik, J. Faver, Feng Li, Pranavanand Nyshadham, Nicholas Simmons, K. Sharma, Sureshbabu Nagarajan, Kevin P. Riehle, Gundeep Kaur, B. Sankaran, Marta R. Storl-Desmond, S. Palmer, D. Young, Choel Kim, M. Matzuk   +18 more
semanticscholar   +1 more source

A Chemical Probe for the ATAD2 Bromodomain [PDF]

Angewandte Chemie, 2016
AbstractATAD2 is a cancer‐associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio‐isostere to exploit the unique properties of fluorine, and 2) using 1,3‐interactions to ...
Paul Bamborough, Chun‐wa Chung, Emmanuel H. Demont, Rebecca C. Furze, Andrew J. Bannister, Ka Hing Che, Hawa Diallo, Clement Douault, Paola Grandi, Tony Kouzarides, Anne‐Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Christina Rau, Samuel Robson, Robert J. Sheppard, Richard Upton, Robert J. Watson   +17 more
openaire   +3 more sources

Reading More than Histones: The Prevalence of Nucleic Acid Binding among Reader Domains

Molecules, 2018
The eukaryotic genome is packaged into the cell nucleus in the form of chromatin, a complex of genomic DNA and histone proteins. Chromatin structure regulation is critical for all DNA templated processes and involves, among many things, extensive post ...
Tyler M. Weaver, Emma A. Morrison, Catherine A. Musselman   +2 more
doaj   +1 more source

A phase 1 study of the pan‐bromodomain and extraterminal inhibitor mivebresib (ABBV‐075) alone or in combination with venetoclax in patients with relapsed/refractory acute myeloid leukemia

Cancer, 2021
Acute myeloid leukemia (AML) is a heterogenous malignancy driven by genetic and epigenetic factors. Inhibition of bromodomain and extraterminal (BET) proteins, epigenetic readers that play pivotal roles in the regulation of genes relevant to cancer ...
G. Borthakur, O. Odenike, Ibrahim Aldoss, D. Rizzieri, T. Prebet, Chris Chen, R. Popovic, Dimple A. Modi, Rujuta H Joshi, J. Wolff, B. Jonas   +10 more
semanticscholar   +1 more source

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

, 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   +1 more source

Chemical synthesis of the ATAD2 bromodomain [PDF]

Proceedings of the National Academy of Sciences, 2014
Significance The bromodomain–histone binding motif has been shown to read epigenetic marks on chromatin, and proteins with a bromodomain can have powerful effects on gene expression and transcriptional regulation. ATAD2 is one such protein and has been linked to a wide variety of cancers with expression of ATAD2 correlating strongly with a ...
Gardner S, Creech, Chelsea, Paresi, Yue-Ming, Li, Samuel J, Danishefsky   +3 more
openaire   +2 more sources