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Showing 1–13 of 13 results
Advanced filters: Author: Panagis Filippakopoulos Clear advanced filters

  • A new approach is used to target BET family bromodomains which are found in transcriptional regulators where they mediate the recognition of acetyl-lysine chromatin marks. Structural data reveal how the compound JQ1 binds to the bromodomain of BRD4. BRD4 has been implicated in a subtype of human squamous carcinomas, and JQ1 is found to inhibit the growth of BRD4 dependent tumours in mouse models.

    • Panagis Filippakopoulos
    • Jun Qi
    • James E. Bradner
    Research
    Nature
    Volume: 468, P: 1067-1073

  • Inhibiting bromodomains — which are small interaction modules on proteins that assemble acetylation-dependent transcriptional regulatory complexes — could be a way to alter the expression of disease-promoting genes. Here, the authors highlight recent developments in the discovery of small-molecule bromodomain inhibitors and discuss how they might be used in cancer, inflammation and viral infection.

    • Panagis Filippakopoulos
    • Stefan Knapp
    Reviews
    Nature Reviews Drug Discovery
    Volume: 13, P: 337-356

  • Bromodomains (BRDs) are domains found in diverse proteins that recognize acetylated Lys residues, primarily on histones. Hence, BRD-containing proteins serve as readers of protein acetylation and engage in the regulation of gene expression. Recent studies have provided new insights into the physiological roles of BRD-containing proteins and their deregulation in cancer.

    • Takao Fujisawa
    • Panagis Filippakopoulos
    Reviews
    Nature Reviews Molecular Cell Biology
    Volume: 18, P: 246-262

  • The microphthalmia-associated transcription factor MITF is a lineage-survival oncogene that plays a crucial role in melanocyte development and melanoma. Here, the authors reveal that MITF has a very long chromatin-bound half-life, and that MITF target selectivity is regulated by K206 acetylation, a residue linked to Waardenburg syndrome.

    • Pakavarin Louphrasitthiphol
    • Alessia Loffreda
    • Colin R. Goding
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-15

  • Bromodomains are conserved protein interaction modules that recognize acetyl-lysine modifications. Here the authors present a set of 25 selective small molecule inhibitors covering 29 human bromodomain targets and comprehensively evaluate the selectivity of this probe-set.

    • Qin Wu
    • David Heidenreich
    • Stefan Knapp
    ResearchOpen Access
    Nature Communications
    Volume: 10, P: 1-14

  • The role of BRD4 and Mediator in regulating enhancer-promoter interactions is poorly understood. Here the authors find that treatment with BET inhibitors or pharmacological degradation of BRD4 disrupts transcription while having very little effect on enhancer-promoter interactions.

    • Nicholas T. Crump
    • Erica Ballabio
    • Thomas A. Milne
    ResearchOpen Access
    Nature Communications
    Volume: 12, P: 1-15

  • Duchenne muscular dystrophy (DMD) is characterised by progressive muscle degeneration. Here, the authors show that the BET protein BRD4 is increased in the muscle of DMD mouse models, and that pharmacological inhibition of BRD4 leads to reduced muscle pathology in mice, by modulating NADPH oxidase expression.​

    • Marco Segatto
    • Roberta Szokoll
    • Giuseppina Caretti
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-13

  • On amino acid deprivation TFEB translocates from the cytoplasm to the nucleus. Here the authors identify a nuclear export signal in TFEB that requires dual phosphorylation at the S142 ERK/mTORC1 and S138 GSK3β sites, and further show glucose limitation drives nuclear accumulation of TFEB and inhibits GSK3β via an mTORC2-AKT dependent mechanism.

    • Linxin Li
    • Hans J. Friedrichsen
    • Colin R. Goding
    ResearchOpen Access
    Nature Communications
    Volume: 9, P: 1-15

  • Cachexia is a metabolic syndrome leading to muscle and adipose tissue loss in majority of cancer patients. Here the authors show that, in a mouse model, BET inhibitor JQ1 counteracts muscle and adipose tissue wasting tempering cachexia and prolonging survival through a mechanism unrelated to tumour growth.

    • Marco Segatto
    • Raffaella Fittipaldi
    • Giuseppina Caretti
    ResearchOpen Access
    Nature Communications
    Volume: 8, P: 1-16

  • Kinases are a widely targeted enzyme class in cancer chemotherapy. Several clinically used kinase inhibitors also inhibit bromodomains, epigenetic ‘readers’ of acetylated lysine residues, suggesting that kinase-bromodomain polypharmacology may offer benefits in therapeutic settings.

    • Pietro Ciceri
    • Susanne Müller
    • Stefan Knapp
    Research
    Nature Chemical Biology
    Volume: 10, P: 305-312