1. Modulation of Retinoic Acid Receptor Subtypes by 5- and 8-Substituted (Naphthalen-2-yl)-based Arotinoids.

    Chemmedchem 10(8):1378 (2015) PMID 26012882

    Retinoid receptors (RARs and RXRs) transduce the signals of their natural and synthetic ligands (retinoids and rexinoids) to cellular transcriptional machinery to induce gene programs that control diverse biological and physiological effects on organisms. All-trans-retinoic acid, the natural lig...
  2. The inactive X chromosome is epigenetically unstable and transcriptionally labile in breast cancer.

    Genome Research 25(4):488 (2015) PMID 25653311 PMCID PMC4381521

    Disappearance of the Barr body is considered a hallmark of cancer, although whether this corresponds to genetic loss or to epigenetic instability and transcriptional reactivation is unclear. Here we show that breast tumors and cell lines frequently display major epigenetic instability of the ina...
  3. Thioether analogues of disulfide-bridged cyclic peptides targeting death receptor 5: conformational analysis, dimerisation and consequences for receptor activation.

    ChemBioChem 16(2):293 (2015) PMID 25487639

    Cyclic peptides containing redox-stable thioether bridges might provide a useful alternative to disulfide-bridged bioactive peptides. We report the effect of replacing the disulfide bridge with a lanthionine linkage in a 16-mer cyclic peptide that binds to death receptor 5 (DR5, TRAIL-R2). Upon ...
  4. Thioether analogues of disulfide-bridged cyclic peptides targeting death receptor 5: conformational analysis, dimerisation and consequences for receptor activation.

    ChemBioChem 16(2):293 (2015) PMID 25487639

    Cyclic peptides containing redox-stable thioether bridges might provide a useful alternative to disulfide-bridged bioactive peptides. We report the effect of replacing the disulfide bridge with a lanthionine linkage in a 16-mer cyclic peptide that binds to death receptor 5 (DR5, TRAIL-R2). Upon ...
  5. Thioether analogues of disulfide-bridged cyclic peptides targeting death receptor 5: conformational analysis, dimerisation and consequences for receptor activation.

    ChemBioChem 16(2):293 (2015) PMID 25487639

    Cyclic peptides containing redox-stable thioether bridges might provide a useful alternative to disulfide-bridged bioactive peptides. We report the effect of replacing the disulfide bridge with a lanthionine linkage in a 16-mer cyclic peptide that binds to death receptor 5 (DR5, TRAIL-R2). Upon ...
  6. Human cells contain natural double-stranded RNAs with potential regulatory functions.

    Nature Structural & Molecular Biology 22(1):89 (2015) PMID 25504323

    Recent evidence has suggested the existence of sense-antisense transcription in mammals, but the existence of double-stranded RNAs endowed with biological function has remained elusive. Herein we show that hundreds of putative natural double-stranded RNAs (ndsRNAs) are expressed from intersperse...
  7. Human cells contain natural double-stranded RNAs with potential regulatory functions.

    Nature Structural & Molecular Biology 22(1):89 (2015) PMID 25504323

    Recent evidence has suggested the existence of sense-antisense transcription in mammals, but the existence of double-stranded RNAs endowed with biological function has remained elusive. Herein we show that hundreds of putative natural double-stranded RNAs (ndsRNAs) are expressed from intersperse...
  8. An Unexpected Mode Of Binding Defines BMS948 as A Full Retinoic Acid Receptor β (RARβ, NR1B2) Selective Agonist.

    PLoS ONE 10(5):e0123195 (2015) PMID 25933005 PMCID PMC4416907

    Retinoic acid is an important regulator of cell differentiation which plays major roles in embryonic development and tissue remodeling. The biological action of retinoic acid is mediated by three nuclear receptors denoted RARα, β and γ. Multiple studies support that RARβ possesses functional cha...
  9. Assessing quality standards for ChIP-seq and related massive parallel sequencing-generated datasets: When rating goes beyond avoiding the crisis

    Genomics Data 2:268 (2014)

    Massive parallel DNA sequencing combined with chromatin immunoprecipitation and a large variety of DNA/RNA-enrichment methodologies is at the origin of data resources of major importance. Indeed these resources, available for multiple genomes, represent the most comprehensive catalogue...
  10. Senescence-secreted factors activate Myc and sensitize pretransformed cells to TRAIL-induced apoptosis.

    Aging Cell 13(3):487 (2014) PMID 24589226 PMCID PMC4326894

    Senescent cells secrete a plethora of factors with potent paracrine signaling capacity. Strikingly, senescence, which acts as defense against cell transformation, exerts pro-tumorigenic activities through its secretome by promoting tumor-specific features, such as cellular proliferation, epithel...
  11. Senescence-secreted factors activate Myc and sensitize pretransformed cells to TRAIL-induced apoptosis.

    Aging Cell 13(3):487 (2014) PMID 24589226

    Senescent cells secrete a plethora of factors with potent paracrine signaling capacity. Strikingly, senescence, which acts as defense against cell transformation, exerts pro-tumorigenic activities through its secretome by promoting tumor-specific features, such as cellular proliferation, epithel...
  12. Senescence-secreted factors activate Myc and sensitize pretransformed cells to TRAIL-induced apoptosis.

    Aging Cell 13(3):487 (2014) PMID 24589226 PMCID PMC4326894

    Senescent cells secrete a plethora of factors with potent paracrine signaling capacity. Strikingly, senescence, which acts as defense against cell transformation, exerts pro-tumorigenic activities through its secretome by promoting tumor-specific features, such as cellular proliferation, epithel...
  13. Senescence-secreted factors activate Myc and sensitize pretransformed cells to TRAIL-induced apoptosis.

    Aging Cell 13(3):487 (2014) PMID 24589226 PMCID PMC4326894

    Senescent cells secrete a plethora of factors with potent paracrine signaling capacity. Strikingly, senescence, which acts as defense against cell transformation, exerts pro-tumorigenic activities through its secretome by promoting tumor-specific features, such as cellular proliferation, epithel...
  14. Dual RXR Agonists and RAR Antagonists Based on the Stilbene Retinoid Scaffold.

    ACS Medicinal Chemistry Letters 5(5):533 (2014) PMID 24900875 PMCID PMC4027779

    Arotinoids containing a C5,C8-diphenylnaphthalene-2-yl ring linked to a (C3-halogenated) benzoic acid via an ethenyl connector (but not the corresponding naphthamides), which are prepared by Horner-Wadsworth-Emmons reaction of naphthaldehydes and benzylphosphonates, display the rather unusual pr...
  15. Dual RXR Agonists and RAR Antagonists Based on the Stilbene Retinoid Scaffold.

    ACS Medicinal Chemistry Letters 5(5):533 (2014) PMID 24900875 PMCID PMC4027779

    Arotinoids containing a C5,C8-diphenylnaphthalene-2-yl ring linked to a (C3-halogenated) benzoic acid via an ethenyl connector (but not the corresponding naphthamides), which are prepared by Horner-Wadsworth-Emmons reaction of naphthaldehydes and benzylphosphonates, display the rather unusual pr...
  16. Functions, therapeutic applications, and synthesis of retinoids and carotenoids.

    Chemical Reviews 114(1):1 (2014) PMID 24266866

  17. Functions, therapeutic applications, and synthesis of retinoids and carotenoids.

    Chemical Reviews 114(1):1 (2014) PMID 24266866

  18. Integrative genomics to dissect retinoid functions.

    Sub-Cellular Biochemistry 70:181 (2014) PMID 24962886

    Retinoids and rexinoids, as all other ligands of the nuclear receptor (NR) family, act as ligand-regulated trans-acting transcription factors that bind to cis-acting DNA regulatory elements in the promoter regions of target genes (for reviews see [12, 22, 23, 26, 36]). Ligand binding modulates t...
  19. Integrative genomics to dissect retinoid functions.

    Sub-Cellular Biochemistry 70:181 (2014) PMID 24962886

    Retinoids and rexinoids, as all other ligands of the nuclear receptor (NR) family, act as ligand-regulated trans-acting transcription factors that bind to cis-acting DNA regulatory elements in the promoter regions of target genes (for reviews see [12, 22, 23, 26, 36]). Ligand binding modulates t...
  20. Genome-wide studies of nuclear receptors in cell fate decisions

    Seminars in Cell & Developmental Biology 24(10-12):706 (2013)

    • Emphasis on the retinoic acid receptor system. • Gene expression signatures of NRs. • Historical st...