Results 51 to 60 of about 43,525 (155)

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
openaire   +7 more sources

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

BET‐ting on Nrf2: How Nrf2 Signaling can Influence the Therapeutic Activities of BET Protein Inhibitors [PDF]

BioEssays, 2018
BET proteins such as Brd3 and Brd4 are chromatin‐associated factors, which control gene expression programs that promote inflammation and cancer. The Nrf2 transcription factor is a master regulator of genes that protect the organism against xenobiotic attack and oxidative stress.
Nirmalya, Chatterjee, Dirk, Bohmann
openaire   +2 more sources

BET Proteins Exhibit Transcriptional and Functional Opposition in the Epithelial-to-Mesenchymal Transition. [PDF]

Mol Cancer Res, 2018
Transcriptional programs in embryogenesis and cancer, such as the epithelial-to-mesenchymal transition (EMT), ensure cellular plasticity, an essential feature of carcinoma progression.
Andrieu GP, Denis GV.
europepmc   +2 more sources

The Bet v 1 fold: an ancient, versatile scaffold for binding of large, hydrophobic ligands

BMC Evolutionary Biology, 2008
Background The major birch pollen allergen, Bet v 1, is a member of the ubiquitous PR-10 family of plant pathogenesis-related proteins. In recent years, a number of diverse plant proteins with low sequence similarity to Bet v 1 was identified.
Breiteneder Heimo, Lackner Peter, Radauer Christian   +2 more
doaj   +1 more source

BET bromodomain protein inhibition is a therapeutic option for medulloblastoma [PDF]

Oncotarget, 2013
Medulloblastoma is the most common malignant brain tumor of childhood, and represents a significant clinical challenge in pediatric oncology, since overall survival currently remains under 70%. Patients with tumors overexpressing MYC or harboring a MYC oncogene amplification have an extremely poor prognosis.
Henssen, Anton, Thor, Theresa, Odersky, Andrea, Heukamp, Lukas, El-Hindy, Nicolai, Beckers, Anneleen, Speleman, Frank, Althoff, Kristina, Schäfers, Simon, Schramm, Alexander, Sure, Ulrich, Fleischhack, Gudrun, Eggert, Angelika, Schulte, Johannes   +13 more
openaire   +5 more sources

Selective BH3 mimetics synergize with BET inhibition to induce mitochondrial apoptosis in rhabdomyosarcoma cells

Neoplasia: An International Journal for Oncology Research, 2022
BH3 mimetics are promising novel anticancer therapeutics. By selectively inhibiting BCL-2, BCL-xL, or MCL-1 (i.e. ABT-199, A-1331852, S63845) they shift the balance of pro- and anti-apoptotic proteins in favor of apoptosis.
Ufuk Erdogdu, Nadezda Dolgikh, Stephanie Laszig, Vinzenz Särchen, Michael T. Meister, Marek Wanior, Stefan Knapp, Cathinka Boedicker   +7 more
doaj   +1 more source

BRD4 bimodal binding at promoters and drug-induced displacement at Pol II pause sites associates with I-BET sensitivity

Epigenetics & Chromatin, 2019
Background Deregulated transcription is a major driver of diseases such as cancer. Bromodomain and extra-terminal (BET) proteins (BRD2, BRD3, BRD4 and BRDT) are chromatin readers essential for maintaining proper gene transcription by specifically binding
P. Khoueiry, A. Ward Gahlawat, M. Petretich, A. M. Michon, D. Simola, E. Lam, E. E. Furlong, V. Benes, M. A. Dawson, R. K. Prinjha, G. Drewes, P. Grandi   +11 more
doaj   +1 more source

Targetable BET proteins- and E2F1-dependent transcriptional program maintains the malignancy of glioblastoma [PDF]

, 2018
Significance Glioblastoma (GBM) cells develop intrinsic or acquired insensitiveness to BET bromodomain inhibitors (BBIs) yet develop persistent BET protein dependency. Selective degradation of BET proteins by a next-generation chemical compound
Carol Tang, Huang, Mo-Li, Liang Xu, Koeffler, H Phillip, Mo-Li Huang, Anand Mayakonda, H. Phillip Koeffler, Wendi Sun, Xu, Liang, Benjamin P. Berman, Sandanaraj, Edwin, Beng Ti Ang, Edwin Sandanaraj, Lynnette Koh, Ke, Xin-Yu, Ling-Wen Ding, Bradner, James E, Dennis L. Buckley, Sun, Wendi, Goh, Boon Cher, Lin, Ruby Yu-Tong, See Wee Lim, Kappei, Dennis, Jianxiang Chen, Winter, Georg E, Ye Chen, Ang, Beng Ti, Berman, Benjamin P, Buckley, Dennis L, Lim, See Wee, Chen, Jianxiang, Ding, Ling-Wen, Dennis Kappei, Dinh, Huy Q, Yuk Kien Chong, Huy Q. Dinh, Wang, Ling-Zhi, Chong, Yuk Kien, James E. Bradner, Koh, Lynnette, Ling-Zhi Wang, Xin-Yu Ke, Georg E. Winter, Ruby Yu-Tong Lin, Boon Cher Goh, Chen, Ye, Mayakonda, Anand, Tang, Carol   +47 more
core   +1 more source

The bromodomain and extra-terminal domain degrader MZ1 exhibits preclinical anti-tumoral activity in diffuse large B-cell lymphoma of the activated B cell-like type

Exploration of Targeted Anti-tumor Therapy, 2021
Aim: Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers that play a fundamental role in transcription regulation. Preclinical and early clinical evidence sustain BET targeting as an anti-cancer approach.
Chiara Tarantelli, Eleonora Cannas, Hillarie Ekeh, Carmelo Moscatello, Eugenio Gaudio, Luciano Cascione, Sara Napoli, Cesare Rech, Andrea Testa, Chiara Maniaci, Andrea Rinaldi, Emanuele Zucca, Anastasios Stathis, Alessio Ciulli, Francesco Bertoni   +14 more
doaj   +1 more source