Results 91 to 100 of about 37,262 (190)

Chemical probes targeting epigenetic proteins: Applications beyond oncology

Epigenetics, 2017
Epigenetic chemical probes are potent, cell-active, small molecule inhibitors or antagonists of specific domains in a protein; they have been indispensable for studying bromodomains and protein methyltransferases. The Structural Genomics Consortium (SGC),
Suzanne Ackloo, Peter J. Brown, Susanne Müller   +2 more
doaj   +1 more source

Epigenetic regulators as promising therapeutic targets in acute myeloid leukemia. [PDF]

, 2015
Acute myeloid leukemia (AML), the most prevalent acute leukemia in adults, is an aggressive hematological malignancy arising in hematopoietic stem and progenitor cells.
Gallipoli, Paolo, Giotopoulos, George, Huntly, Brian JP   +2 more
core   +2 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   +1 more source

Optimization of a “Bump-and-Hole” Approach to Allele-Selective BET Bromodomain Inhibition [PDF]

, 2018
Allele-specific chemical genetics enables selective inhibition within families of highly-conserved proteins. The four BET (bromodomain & extra-terminal domain) proteins – BRD2, BRD3, BRD4 and BRDT bind acetylated chromatin via their bromodomains and ...
Albrecht, Amorim, Anders, Andrieu, Arrowsmith, Bamborough, Bamborough, Baud, Baud, Bishop, Bolden, Bunnage, Cheung, Clackson, Conery, Dawson, Deeney, Delmore, Dubocovich, Filippakopoulos, Filippakopoulos, Gacias, Gadd, Galdeano, Gamsjaeger, Huang, Islam, Lamonica, Li, Lin, Lu, Miller, Mirguet, Muller, Nassar, Nguyen, Nicholls, Nicodeme, Philpott, Picaud, Raina, Raux, Runcie, Sander, Schroder, Shi, Shi, Smith, Stathis, Stonestrom, Tanaka, Theodoulou, Theodoulou, Wang, Winter, Yang, Zengerle, Zhou, Zou, Zuber   +59 more
core   +2 more sources

Structural Activity Relationship Analysis of New Diphenyl PFI-3 Analogues Targeting for the Treatment of Glioblastoma

Pharmaceuticals
Background/Objectives: Human glioblastoma (GBM) is the most aggressive brain cancer in adults and a highly treatment-refractory malignancy. The overall prognosis for the GBM is extremely poor, with a median survival of 12–14 months after initial ...
Dong-Jin Hwang, Chuanhe Yang, Yinan Wang, Hannah Kelso, Satyanarayana Pochampally, Lawrence M. Pfeffer, Duane D. Miller   +6 more
doaj   +1 more source

Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition

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   +1 more source

Predicting the outcomes of treatment to eradicate the latent reservoir for HIV-1 [PDF]

, 2014
Massive research efforts are now underway to develop a cure for HIV infection, allowing patients to discontinue lifelong combination antiretroviral therapy (ART). New latency-reversing agents (LRAs) may be able to purge the persistent reservoir of latent
Fu, Feng, Hill, Alison L., Nowak, Martin A., Rosenbloom, Daniel I. S., Siliciano, Robert F.   +4 more
core   +3 more sources

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design [PDF]

, 2019
Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera (PROTAC) degraders of the BAF ATPase subunits SMARCA2 and SMARCA4 using a ...
Arnhof, Heribert, Bader, Gerd, Boehmelt, Guido, Ciulli, Alessio, Dank, Christian, Diers, Emelyne, Ehrenhöfer-Wölfer, Katharina, Ettmayer, Peter, Farnaby, William, Galant, Michael, Gerstberger, Thomas, Gmaschitz, Teresa, Greb, Peter, Karolyi-Oezguer, Jale, Koegl, Manfred, McConnell, Darryl B., Owen-Hughes, Tom, Pearson, Mark, Petermann, Oliver, Riedmueller, Carina, Rinnenthal, Joerg, Roy, Michael J., Rumpel, Klaus, Schnitzer, Renate, Sharps, Bernadette, Steurer, Steffen, Trainor, Nicole, Traxler, Elisabeth, Wachter, Johannes, Weinstabl, Harald, Weiss-Puxbaum, Alexander, Whitworth, Claire, Wiechens, Nicola, Wu, Meng-Ying, Wöhrle, Simon, Zoephel, Andreas, Zollman, David   +36 more
core   +2 more sources

TgPRELID, a Mitochondrial Protein Linked to Multidrug Resistance in the Parasite Toxoplasma gondii [PDF]

, 2017
New drugs to control infection with the protozoan parasite Toxoplasma gondii are needed as current treatments exert toxic side effects on patients. Approaches to develop novel compounds for drug development include screening of compound libraries and ...
Ananth R. Srinivasan, Edwin T. Kamau, Jon P. Boyle, Jonathan Harper, Joseph M. Varberg, Margaret Phillips, Preethi Sankaran, Sarah E. Post, Victoria Jeffers, William J. Sullivan   +9 more
core   +3 more sources

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