Results 11 to 20 of about 128,101 (191)

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   +4 more sources

Advancements in the development of non-BET bromodomain chemical probes [PDF]

ChemMedChem, 2019
The bromodomain and extra terminal (BET) family of bromodomain‐containing proteins (BCPs) have been the subject of extensive research over the past decade, resulting in a plethora of high‐quality chemical probes for their tandem bromodomains.
Tomkinson, Nicholas C. O., Prinjhal, Rab K., Clegg, Michael A., Humphreys, Philip G.   +3 more
core   +9 more sources

Progress in the development of non-​BET bromodomain chemical probes [PDF]

ChemMedChem, 2016
The bromodomain and extra terminal (BET) family of bromodomains have been the focus of extensive research, leading to the development of many potent, selective chem. probes and recent clinical assets. The profound biol.
Tomkinson, Nicholas C. O., Theodoulou, Natalie H., Prinjha, Rab K., Humphreys, Philip G.   +3 more
core   +9 more sources

Targeting Cancer Cells with BET Bromodomain Inhibitors [PDF]

Cold Spring Harbor Perspectives in Medicine, 2017
Cancer cells are often hypersensitive to the targeting of transcriptional regulators, which may reflect the deregulated gene expression programs that underlie malignant transformation.
Xu, Y., Christopher R. Vakoc, Yali Xu, Vakoc, C. R.   +3 more
core   +3 more sources

Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition [PDF]

Cancer Discovery, 2013
Bromodomain inhibition comprises a promising therapeutic strategy in cancer, particularly for hematologic malignancies. To date, however, genomic biomarkers to direct clinical translation have been lacking. We conducted a cell-based screen of genetically
Bassil, Christopher F, Gustafson, William Clay, Nekritz, Erin A, Kung, Andrew L, Weiss, William A, Garnett, Matthew J, Puissant, Alexandre, Frumm, Stacey M, Chanthery, Yvan H, Benes, Cyril H, Zeid, Rhamy, Qi, Jun, Stegmaier, Kimberly, McDermott, Ultan, Bradner, James E, Greninger, Patricia, Alexe, Gabriela   +16 more
core   +6 more sources

BET Bromodomain Inhibition of MYC-Amplified Medulloblastoma [PDF]

Clinical Cancer Research, 2014
PurposeMYC-amplified medulloblastomas are highly lethal tumors. Bromodomain and extraterminal (BET) bromodomain inhibition has recently been shown to suppress MYC-associated transcriptional activity in other cancers.
Weiss, William A.,, Cho, Yoon-Jae, Swartling, Fredrik J, Bolin, Sara,, Cheshier, Samuel H., Paolella, Brenton R., Wechsler-Reya, Robert, Zeid, Rhamy, Gibson, William J, Bandopadhayay, Pratiti,, Kieran, Mark W., Bradner, James E, Bradner, James E.,, Gibson, William J., Bolin, Sara, Cheshier, Samuel H, Liu, Kun-Wei, Schumacher, Steven E., Bergthold, Guillaume,, Cho, Yoon-Jae,, Beroukhim, Rameen,, Mitra, Siddhartha S., Weiss, William A, Nguyen, Brian, Beroukhim, Rameen, Schubert, Simone, Bandopadhayay, Pratiti, Schumacher, Steven E, Mitra, Siddhartha S, Gholamin, Sharareh, Bergthold, Guillaume, Yu, Furong, Qi, Jun, Tang, Yujie, Paolella, Brenton R, Vue, Nujsaubnusi, Kieran, Mark W, Masoud, Sabran, Swartling, Fredrik J.,   +38 more
core   +8 more sources

Bromodomain and extra-terminal domain (BET) proteins regulate melanocyte differentiation

Epigenetics & Chromatin, 2020
Background Pharmacologic inhibition of bromodomain and extra-terminal (BET) proteins is currently being explored as a new therapeutic approach in cancer.
Archit Trivedi, Aanchal Mehrotra, Caitlin E. Baum, Brandon Lewis, Tupa Basuroy, Thomas Blomquist, Robert Trumbly, Fabian V. Filipp, Vijayasaradhi Setaluri, Ivana L. de la Serna   +9 more
doaj   +2 more sources

Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability. [PDF]

PLoS ONE, 2016
Lysine acetylation is an important epigenetic mark regulating gene transcription and chromatin structure. Acetylated lysine residues are specifically recognized by bromodomains, small protein interaction modules that read these modification in a sequence
Laura Lori, Alessandra Pasquo, Clorinda Lori, Maria Petrosino, Roberta Chiaraluce, Cynthia Tallant, Stefan Knapp, Valerio Consalvi   +7 more
doaj   +3 more sources

Inhibition of BET bromodomain targets genetically diverse glioblastoma. [PDF]

Clinical Cancer Research, 2013
PURPOSE: Glioblastoma is refractory to conventional therapies. The bromodomain and extraterminal domain (BET) proteins are epigenetic readers that selectively bind to acetylated lysine residues on histone tails.
Cheng, Z, Knapp, Stefan, Pierce, LA, Gong, Y, Muller, S, Knapp, S, Lu, K, Wang, J, Thompson, RC, Muller, Susanne, Ma, Y, Lu, Xin, Lu, X   +12 more
core   +6 more sources

Alternative Mechanisms for DNA Engagement by BET Bromodomain-Containing Proteins. [PDF]

Biochemistry, 2022
Epigenetic reader domains regulate chromatin structure and modulate gene expression through the recognition of post-translational modifications on histones. Recently, reader domains have also been found to harbor double-stranded (ds) DNA-binding activity,
Kalra P, Zahid H, Ayoub A, Dou Y, Pomerantz WCK.   +4 more
europepmc   +2 more sources