Results 41 to 50 of about 104,722 (190)

Opposing effects of cancer-type-specific SPOP mutants on BET protein degradation and sensitivity to BET inhibitors [PDF]

Nature Medicine, 2017
It is generally assumed that recurrent mutations within a given cancer driver gene elicit similar drug responses. Cancer genome studies have identified recurrent but divergent missense mutations affecting the substrate-recognition domain of the ubiquitin ligase adaptor SPOP in endometrial and prostate cancers.
Janouskova, Hana, El Tekle, Geniver, Bellini, Elisa, Udeshi, Namrata D, Rinaldi, Anna, Ulbricht, Anna, Bernasocchi, Tiziano, Civenni, Gianluca, Losa, Marco, Svinkina, Tanya, Bielski, Craig M, Kryukov, Gregory V, Cascione, Luciano, Napoli, Sara, Enchev, Radoslav I, Mutch, David G, Carney, Michael E, Berchuck, Andrew, Winterhoff, Boris J N, Broaddus, Russell R, Schraml, Peter, Moch, Holger, Bertoni, Francesco, Catapano, Carlo V, Peter, Matthias, Carr, Steven A, Garraway, Levi A, Wild, Peter J, Theurillat, Jean-Philippe P   +28 more
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Crystal structure of the DNA binding domain of the transcription factor T-bet suggests simultaneous recognition of distant genome sites [PDF]

, 2014
The transcription factor T-bet (Tbox protein expressed in T cells) is one of the master regulators of both the innate and adaptive immune responses. It plays a central role in T-cell lineage commitment, where it controls the T[subscript H]1 response, and
Brandt, Gabriel S., Dekker, Job, Glimcher, Laurie H, Hoang, Quyen Q., Hwang, Eun Sook, Lazarevic, Vanja, Liu, Ce Feng, Naumova, Natalia, Petsko, Gregory A., Ringe, Dagmar   +9 more
core   +1 more source

The Bromodomain and Extra-Terminal Domain (BET) Family: Functional Anatomy of BET Paralogous Proteins [PDF]

International Journal of Molecular Sciences, 2016
The Bromodomain and Extra-Terminal Domain (BET) family of proteins is characterized by the presence of two tandem bromodomains and an extra-terminal domain. The mammalian BET family of proteins comprises BRD2, BRD3, BRD4, and BRDT, which are encoded by paralogous genes that may have been generated by repeated duplication of an ancestral gene during ...
openaire   +2 more sources

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
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BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell. [PDF]

PLoS ONE, 2016
Displacement of Bromodomain and Extra-Terminal (BET) proteins from chromatin has promise for cancer and inflammatory disease treatments, but roles of BET proteins in metabolic disease remain unexplored.
Jude T Deeney, Anna C Belkina, Orian S Shirihai, Barbara E Corkey, Gerald V Denis   +4 more
doaj   +1 more source

BET acetyl-lysine binding proteins control pathological cardiac hypertrophy [PDF]

Journal of Molecular and Cellular Cardiology, 2013
Cardiac hypertrophy is an independent predictor of adverse outcomes in patients with heart failure, and thus represents an attractive target for novel therapeutic intervention. JQ1, a small molecule inhibitor of bromodomain and extraterminal (BET) acetyl-lysine reader proteins, was identified in a high throughput screen designed to discover novel small
Jessica I, Spiltoir, Matthew S, Stratton, Maria A, Cavasin, Kim, Demos-Davies, Brian G, Reid, Jun, Qi, James E, Bradner, Timothy A, McKinsey   +7 more
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Selective small molecule induced degradation of the BET bromodomain protein BRD4 [PDF]

, 2015
The Bromo- and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET selective bromodomain inhibitor JQ1.
Alessio Ciulli, Anders L., Baratta M. G., Baud M. G. J., Belkina A. C., Boi M., Brand M., Bretones G., Cheng Z., Chung C.-W., Corson T. W., Cyrus K., Delmore J. E., Filippakopoulos P., Filippakopoulos P., Filippakopoulos P., Galdeano C., Gallenkamp D., Gosmini R., Hnilicová J., Hon W.-C., Khan Y. M., Kwok-Ho Chan, Lamoureux F., Lee H., Li Z., McLure K. G., Mertz J. A., Michael Zengerle, Mirguet O., Nicodeme E., Prinjha R. K., Raina K., Sakamoto K. M., Sakamoto K. M., Schneekloth J. S., Seoane J., Shi J., Strasser A., Zuber J.   +39 more
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Progress in the development of non-​BET bromodomain chemical probes [PDF]

, 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.
Arrowsmith, Bamborough, Bantscheff, Borah, Brand, Bunnage, Caron, Chaikuad, Chung, Chung, Chung, Chung, Clark, Coudé, Dawson, Demont, Demont, Drouin, Fedorov, Fedorov, Ferguson, Filippakopoulos, Filippakopoulos, Filippakopoulos, Fish, Furdas, Gallenkamp, Garnier, Gerona-Navarro, Gu, Guetzoyan, Harner, Hay, Hay, Hewings, Hewings, Hewings, Hohmann, Jennings, Knapp, Machleidt, McKeown, McLure, Medina, Mirguet, Mirguet, Mujtaba, Mujtaba, Mujtaba, Müller, Nicodeme, Philpott, Piatnitski Chekler, Picaud, Picaud, Prinjha, Rooney, Sachchidanand, Sanchez, Seal, Sweis, Sweis, Ullah, Vangamudi, Vidler, Werner, Zeng, Zhang   +67 more
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Nejire/dCBP-mediated control of H3 acetylation and transcriptional regulation by testis-specific Plus3 domain proteins during Drosophila spermatogenesis [PDF]

, 2018
Spermatogenesis describes the development from germ line stem cells to highly specialized sperm. Drosophila melanogaster spermatogenesis is a good model system for chromatin remodelling processes as many of these processes are similar in mammals and in ...
Hundertmark, Tim
core   +1 more source

BETTING ON ALTERNATIVES: TARGETING TELOMERIC DILNCRNA AND BET PROTEINS IN ALT CANCER

, 2023
The Alternative Lengthening of Telomeres (ALT) pathway is a homology-driven, damage-induced mechanism of telomere maintenance (TMM) that sustains the proliferation of 10-15% of human cancers. We have recently discovered that damaged DNA, including deprotected telomeres, triggers de novo transcription of damage-induced long non-coding RNA (dilncRNA ...
openaire   +1 more source