Search Results - "CARLOMAGNO, Francesca"
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NCOA4-mediated ferritinophagy in macrophages is crucial to sustain erythropoiesis in mice
Published in Haematologica (Roma) (01-03-2021)“…Nuclear receptor coactivator 4 (NCOA4) promotes ferritin degradation and Ncoa4-ko mice in a C57BL/6 background show microcytosis and mild anemia, aggravated by…”
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NCOA4 Deficiency Impairs Systemic Iron Homeostasis
Published in Cell reports (Cambridge) (26-01-2016)“…The cargo receptor NCOA4 mediates autophagic ferritin degradation. Here we show that NCOA4 deficiency in a knockout mouse model causes iron accumulation in the…”
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Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases
Published in Scientific reports (09-08-2021)“…We have recently described Pz-1, a benzimidazole-based type-2 RET and VEGFR2 inhibitor. Based on a kinome scan, here we show that Pz-1 is also a potent (IC 50 …”
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Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology
Published in Journal of medicinal chemistry (14-05-2020)“…RET receptor tyrosine kinase is a driver oncogene in human cancer. We recently identified the clinical drug candidate Pz-1, which targets RET and VEGFR2. A key…”
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Tamoxifen erythroid toxicity revealed by studying the role of nuclear receptor co-activator 4 in erythropoiesis
Published in Haematologica (Roma) (01-08-2019)Get full text
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Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology
Published in Angewandte Chemie International Edition (20-07-2015)“…Oncogenic conversion of the RET (rearranged during transfection) tyrosine kinase is associated with several cancers. A fragment‐based chemical screen led to…”
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NCOA4 Transcriptional Coactivator Inhibits Activation of DNA Replication Origins
Published in Molecular cell (03-07-2014)“…NCOA4 is a transcriptional coactivator of nuclear hormone receptors that undergoes gene rearrangement in human cancer. By combining studies in Xenopus laevis…”
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Iron and Ferritin Modulate MHC Class I Expression and NK Cell Recognition
Published in Frontiers in immunology (2019)“…The ability of pathogens to sequester iron from their host cells and proteins affects their virulence. Moreover, iron is required for various innate host…”
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Disease associated mutations at valine 804 in the RET receptor tyrosine kinase confer resistance to selective kinase inhibitors
Published in Oncogene (12-08-2004)“…We have recently demonstrated that the pyrazolopyrimidines PP1 and PP2 and the 4-anilinoquinazoline ZD6474 display a strong inhibitory activity (IC(50)< or…”
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Antitumor Effects of ZD6474, a Small Molecule Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor, with Additional Activity against Epidermal Growth Factor Receptor Tyrosine Kinase
Published in Clinical cancer research (01-04-2003)“…Purpose: Vascular endothelial growth factor (VEGF) is a major mitogen for endothelial cells and enhances vascular permeability. Enhanced VEGF secretion is…”
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Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase
Published in PloS one (05-06-2015)“…Oncogenic mutation of the RET receptor tyrosine kinase is observed in several human malignancies. Here, we describe three novel type II RET tyrosine kinase…”
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BRAF Is a Therapeutic Target in Aggressive Thyroid Carcinoma
Published in Clinical cancer research (01-03-2006)“…Purpose: Oncogenic conversion of BRAF occurs in ∼44% of papillary thyroid carcinomas and 24% of anaplastic thyroid carcinomas. In papillary thyroid carcinomas,…”
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Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
Published in Cancer research (Chicago, Ill.) (01-03-2009)“…Anaplastic thyroid carcinoma (ATC) is one of the most aggressive and chemoresistant cancers. The serine/threonine kinase Polo-like kinase 1 (PLK1), a key…”
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Sorafenib Inhibits Imatinib-Resistant KIT and Platelet-Derived Growth Factor Receptor β Gatekeeper Mutants
Published in Clinical cancer research (01-06-2007)“…Purpose: Targeting of KIT and platelet-derived growth factor receptor (PDGFR) tyrosine kinases by imatinib is an effective anticancer strategy. However,…”
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Structure prediction and validation of the ERK8 kinase domain
Published in PloS one (11-01-2013)“…Extracellular signal-regulated kinase 8 (ERK8) has been already implicated in cell transformation and in the protection of genomic integrity and, therefore,…”
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Functional expression of the CXCR4 chemokine receptor is induced by RET PTC oncogenes and is a common event in human papillary thyroid carcinomas
Published in Oncogene (05-08-2004)“…To identify genes involved in the transformation of thyroid follicular cells, we explored, using DNA oligonucleotide microarrays, the transcriptional response…”
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The tyrosine kinase inhibitor ZD6474 blocks proliferation of RET mutant medullary thyroid carcinoma cells
Published in Endocrine-related cancer (01-02-2011)“…Oncogenic conversion of the RET tyrosine kinase is a frequent feature of medullary thyroid carcinoma (MTC). ZD6474 (vandetanib) is an ATP-competitive inhibitor…”
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Functional characterization of a novel FGFR1OP-RET rearrangement in hematopoietic malignancies
Published in Molecular oncology (01-03-2014)“…The RET (REarranged during Transfection) receptor tyrosine kinase is targeted by oncogenic rearrangements in thyroid and lung adenocarcinoma. Recently, a RET…”
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Molecular Mechanisms of RET Activation in Human Cancer
Published in Annals of the New York Academy of Sciences (01-06-2002)“…: Mutations that produce oncogenes with dominant gain of function target receptor protein tyrosine kinases (PTKs) in cancer and confer uncontrolled…”
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The receptor-type protein tyrosine phosphatase J antagonizes the biochemical and biological effects of RET-derived oncoproteins
Published in Cancer research (Chicago, Ill.) (15-06-2006)“…Thyroid cancer is frequently associated with the oncogenic conversion of the RET receptor tyrosine kinase. RET gene rearrangements, which lead to the…”
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