María E. Riveiro
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Evaluating the Role of the Tyrosine Phosphatase SHP-2 in Mediating Adrenomedullin Proangiogenic Activity in Solid Tumors Open
International audience
Exploring the Role of Adrenomedullin in Overcoming Resistance to Anti-VEGF Therapy in Oncology Open
International audience
View article: A first-in-class Wiskott-Aldrich syndrome protein activator with anti-tumor activity in hematologic cancers
A first-in-class Wiskott-Aldrich syndrome protein activator with anti-tumor activity in hematologic cancers Open
Hematological cancers are among the most common cancers in adults and children. Despite significant improvements in therapies, many patients still succumb to the disease. Therefore, novel therapies are needed. The Wiskott-Aldrich syndrome …
Supplemental Figures S7 from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Supplemental Figures S7. Supplemental Figures S7. Effects of JQ1 and OTX015 on BRD4 binding to MYD88 promoter region in DLBCL cell lines.
Supplementary Figure 3. from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
Mechanisms of reduced cell viability induced by OTX015 are cell line dependent. OTX015 reduces cell proliferation over time and induces cell cycle changes as well as apoptosis. (a) Representative photomicrographs of neuroblastoma cell line…
IMR5_H3K27ac_AllnonPromoterPeaks from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
All H3K27Ac peaks called in non-promoter regions in IMR5
Data from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
Purpose: Targeting BET proteins was previously shown to have specific antitumoral efficacy against MYCN-amplified neuroblastoma. We here assess the therapeutic efficacy of the BET inhibitor, OTX015, in preclinical neuroblastoma models and …
Supplemental Table S1 from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Supplemental Table S1: Cell lines and growth medium.
MYCN targets OTX015_BRD4 and gene expression from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
Westermann et al. as well as Valentijn et al. MYCN target gene list and expression changes after OTX015 treatment as well as BRD4 binding
Data from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Purpose: In cancer cells, the epigenome is often deregulated, and inhibition of the bromodomain and extra-terminal (BET) family of bromodomain-containing proteins is a novel epigenetic therapeutic approach. Preliminary results of an ongoin…
Supplementary Figure 6. from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
BET inhibition preferentially disrupts expression of genes associated with super-enhancers. (a) ChIP-seq profiles for H3K27Ac binding at representative super-enhancer-associated gene loci, including MYCN, NCOR2, BCOR and GLI2, in MYCN-ampl…
Supplementary Figure 1. from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
OTX015 has no significant effect on non-malignant human fibroblasts. (a) Representative pictures of human fibroblasts treated for 72 h with 500 nM OTX015 or DMSO control. Scale bar=100 µm. (b) Growth of fibroblasts treated with 500 nM OTX0…
Supplementary Figure 5. from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
BET bromodomain inhibition leads to disruption of MYCN driven gene-expression programs even at high levels of MYCN. (a) Enrichment of the published gene expression signature for JQ1-treated human MYCN-amplified neuroblastoma cell lines (11…
Differentially expressed genes OTX015 JQ1 from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
Differentially expressed genes in IMR5 cells after OTX015 and JQ1 treatment respectively
Supplemental Table S2-3 from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Supplemental Table S2-3. Supplemental Table S2: List of genes affected by OTX015 in DLBCL cell lines exposed to OTX015. Supplemental Table S3: gene-sets affected by OTX015 in DLBCL cell lines exposed to OTX015.
GSEA cancer gene sets OTX015 and JQ1 from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
GSEA of cancer gene sets after treatment with OTX015 and/or JQ1(GSEA, Broad institute)
Supplemental Figures S6 from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Supplemental Figures S6. Supplemental Figures S6: OTX015 effects on the production of IL-4 and IL-10 in DLBCL cell lines.
Supplementary Figure 6. from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
BET inhibition preferentially disrupts expression of genes associated with super-enhancers. (a) ChIP-seq profiles for H3K27Ac binding at representative super-enhancer-associated gene loci, including MYCN, NCOR2, BCOR and GLI2, in MYCN-ampl…
IMR5_H3K27ac_AllnonPromoterPeaks from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
All H3K27Ac peaks called in non-promoter regions in IMR5
All genes Hg19_BRD4_OTX from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
List of all genes from hg19 with changes in BRD4 binding using BRD4- ChIP-seq in IMR5 cells with changes after treatment with OTX015
Supplementary Figure 2. from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
OTX015 effect on cell viability positively correlates with MYCN status. (a) IC50 of the IMR 5, Chp 134, Chp 212, SK N-BE(2), IMR-32, SK-N-BE, NB69, SK N AS and GI-M-EN neuroblastoma cell lines measured using MTT assays. (b) Maximum reducti…
Supplemental Figures S3-5 from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Supplemental Figures S3-5. Supplemental Figures S3: the gene expression changes induced by OTX015 in DLBCL cell lines. Supplemental Figures S4: network of genes affected by OTX015. Supplemental Figures S5: similar biologic effects of OTX01…
Supplemental Table S4 from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Supplemental Table S4: List of gene-sets associated with the sensitivity to OTX015.
Supplementary Figure 2. from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
OTX015 effect on cell viability positively correlates with MYCN status. (a) IC50 of the IMR 5, Chp 134, Chp 212, SK N-BE(2), IMR-32, SK-N-BE, NB69, SK N AS and GI-M-EN neuroblastoma cell lines measured using MTT assays. (b) Maximum reducti…
Data from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Purpose: In cancer cells, the epigenome is often deregulated, and inhibition of the bromodomain and extra-terminal (BET) family of bromodomain-containing proteins is a novel epigenetic therapeutic approach. Preliminary results of an ongoin…
All genes Hg19_BRD4_OTX from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
List of all genes from hg19 with changes in BRD4 binding using BRD4- ChIP-seq in IMR5 cells with changes after treatment with OTX015
GSEA general cell biology gene sets from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
GSEA of gene sets describing general cellular processes after treatment with OTX015 and/or JQ1(GSEA, Broad institute)
Supplemental Figures S6 from The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs Open
Supplemental Figures S6. Supplemental Figures S6: OTX015 effects on the production of IL-4 and IL-10 in DLBCL cell lines.
Supplementary Figure 4. from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
OTX015 reduces cell proliferation and induces apoptosis in MYCN amplified human xenografts. (a) Representative pictures of IMR5 xenograft tumor sections stained with hematoxylin/eosin, and immunohistochemical staining for apoptotic cells (…
Data from Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition Open
Purpose: Targeting BET proteins was previously shown to have specific antitumoral efficacy against MYCN-amplified neuroblastoma. We here assess the therapeutic efficacy of the BET inhibitor, OTX015, in preclinical neuroblastoma models and …