Francesca Carlomagno

Francesca Carlomagno

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Francesca Carlomagno

Francesca Carlomagno

Publications by authors named "Francesca Carlomagno"

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Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology.

J Med Chem 2020 May 28;63(9):4506-4516. Epub 2020 Apr 28.

Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli "Federico II", 80131 Napoli, Italy.

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http://dx.doi.org/10.1021/acs.jmedchem.9b01336DOI Listing
May 2020

RET Gene Fusions in Malignancies of the Thyroid and Other Tissues.

Genes (Basel) 2020 Apr 15;11(4). Epub 2020 Apr 15.

Department of Molecular Medicine and Medical Biotechnology, University of Naples "Federico II", 80131 Naples, Italy.

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http://dx.doi.org/10.3390/genes11040424DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7230609PMC
April 2020

Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.

J Med Chem 2019 02 19;62(4):1731-1760. Epub 2018 Sep 19.

Department of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.

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http://dx.doi.org/10.1021/acs.jmedchem.8b01092DOI Listing
February 2019

The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer.

Best Pract Res Clin Endocrinol Metab 2017 06 10;31(3):307-318. Epub 2017 May 10.

Istituto di Endocrinologia e Oncologia Sperimentale, CNR, Via S Pansini 5, 80131 Naples, Italy; Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università Federico II, Via S Pansini 5, 80131 Naples, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.beem.2017.04.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5624797PMC
June 2017

Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase.

PLoS One 2015 5;10(6):e0128364. Epub 2015 Jun 5.

Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli "Federico II", Naples, Italy; Istituto di Endocrinologia ed Oncologia Sperimentale del CNR, Naples, Italy.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0128364PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4457528PMC
March 2016

NCOA4 Deficiency Impairs Systemic Iron Homeostasis.

Cell Rep 2016 Jan 14;14(3):411-421. Epub 2016 Jan 14.

Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università degli Studi di Napoli Federico II, and Istituto di Endocrinologia ed Oncologia Sperimentale del Consiglio Nazionale delle Ricerche, 80131 Napoli, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2015.12.065DOI Listing
January 2016

Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology.

Angew Chem Int Ed Engl 2015 Jul 30;54(30):8717-21. Epub 2015 Jun 30.

Medicinal Chemistry Division, Pharmacology and Toxicology, College of Pharmacy, The University of Arizona, 1703 E. Mabel, Tucson, AZ 85721 (USA).

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http://doi.wiley.com/10.1002/anie.201501104
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http://dx.doi.org/10.1002/anie.201501104DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4535927PMC
July 2015

Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation.

Eur J Med Chem 2014 Oct 8;86:714-23. Epub 2014 Sep 8.

College of Pharmacy, Department of Pharmacology and Toxicology, The University of Arizona, Tucson, AZ 85721, USA; The University of Arizona Cancer Center, 1515 N Campbell Ave, Tucson, AZ 85724, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.09.023DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4666024PMC
October 2014

Growth factor transduction pathways: paradigm of anti-neoplastic targeted therapy.

J Mol Med (Berl) 2014 Jul 8;92(7):723-33. Epub 2014 Jun 8.

Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università degli Studi di Napoli Federico II, via Pansini 5, 80131, Naples, Italy,

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http://dx.doi.org/10.1007/s00109-014-1177-7DOI Listing
July 2014

NCOA4 transcriptional coactivator inhibits activation of DNA replication origins.

Mol Cell 2014 Jul 5;55(1):123-37. Epub 2014 Jun 5.

Istituto di Endocrinologia ed Oncologia Sperimentale del CNR/Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli "Federico II," 80131 Naples, Italy. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S10972765140036
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http://dx.doi.org/10.1016/j.molcel.2014.04.031DOI Listing
July 2014

Central role of RET in thyroid cancer.

Cold Spring Harb Perspect Biol 2013 Dec 1;5(12):a009233. Epub 2013 Dec 1.

Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Universita' degli Studi di Napoli Federico II, 80131 Napoli, Italy.

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http://dx.doi.org/10.1101/cshperspect.a009233DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3839608PMC
December 2013

Attacking cancer with molecularly targeted agents.

Curr Opin Pharmacol 2013 Aug 16;13(4):483-5. Epub 2013 Jul 16.

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http://dx.doi.org/10.1016/j.coph.2013.06.011DOI Listing
August 2013

Structure prediction and validation of the ERK8 kinase domain.

PLoS One 2013 11;8(1):e52011. Epub 2013 Jan 11.

Istituto Toscano Tumori-Core Research Laboratory, Signal Transduction Unit, AOU Senese, Siena, Italy.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0052011PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3543423PMC
July 2013

Molecular mechanism of 17-allylamino-17-demethoxygeldanamycin (17-AAG)-induced AXL receptor tyrosine kinase degradation.

J Biol Chem 2013 Jun 29;288(24):17481-94. Epub 2013 Apr 29.

Dipartimento di Medicina Molecolare e Biotecnologie Mediche, University of Naples Federico II, Naples, Italy.

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http://dx.doi.org/10.1074/jbc.M112.439422DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3682548PMC
June 2013

Ponatinib (AP24534) is a novel potent inhibitor of oncogenic RET mutants associated with thyroid cancer.

J Clin Endocrinol Metab 2013 May 22;98(5):E811-9. Epub 2013 Mar 22.

Istituto di Endocrinologia ed Oncologia Sperimentale del Consiglio Nazionale delle Ricerche, Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli Federico II, 80131 Naples, Italy.

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http://dx.doi.org/10.1210/jc.2012-2672DOI Listing
May 2013

Thyroid Cancer: Role of RET and Beyond.

Eur Thyroid J 2012 Apr 28;1(1):15-23. Epub 2012 Mar 28.

Dipartimento di Biologia e Patologia Cellulare e Molecolare L. Califano, Università degli Studi di Napoli Federico II, Napoli, Italia.

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http://dx.doi.org/10.1159/000336975DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3821455PMC
April 2012

Thyroid cancer in 2010: a roadmap for targeted therapies.

Nat Rev Endocrinol 2011 Feb;7(2):65-7

Dipartimento di Biologia e Patologia Cellulare e Molecolare L Califano, Universita' degli studi di Napoli, Via Pansini 5, 80131 Naples, Italy.

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http://dx.doi.org/10.1038/nrendo.2010.232DOI Listing
February 2011

RET is a heat shock protein 90 (HSP90) client protein and is knocked down upon HSP90 pharmacological block.

J Clin Endocrinol Metab 2010 Jul 5;95(7):3552-7. Epub 2010 May 5.

Istituto di Endocrinologia ed Oncologia Sperimentale del Consiglio Nazionale delle Ricerche, Dipartimento di Biologia e Patologia Cellulare e Molecolare, Universitá Federico II, 80131 Naples, Italy.

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https://academic.oup.com/jcem/article-lookup/doi/10.1210/jc.
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http://dx.doi.org/10.1210/jc.2009-2315DOI Listing
July 2010

Identification of tyrosine 806 as a molecular determinant of RET kinase sensitivity to ZD6474.

Endocr Relat Cancer 2009 Mar 24;16(1):233-41. Epub 2008 Nov 24.

Dipartimento di Biologia e Patologia Cellulare e Molecolare, Università di Napoli Federico II, via S. Pansini 5, 80131 Naples, Italy.

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http://dx.doi.org/10.1677/ERC-08-0213DOI Listing
March 2009

Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma.

Cancer Res 2009 Mar 17;69(5):1916-23. Epub 2009 Feb 17.

Dipartimento di Biologia e Patologia Cellulare e Molecolare L. Califano c/o Istituto di Endocrinologia ed Oncologia Sperimentale del CNR, Universita' Federico II, Naples, Italy.

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http://dx.doi.org/10.1158/0008-5472.CAN-08-1693DOI Listing
March 2009

Receptor tyrosine kinase inhibitors in thyroid cancer.

Best Pract Res Clin Endocrinol Metab 2008 Dec;22(6):1023-38

Istituto di Endocrinologia ed Oncologia Sperimentale CNR, 80131 Naples, Italy c/o Dipartimento di Biologia e Patologia Cellulare e Molecolare, Universita' Federico II, 80131 Naples, Italy.

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http://dx.doi.org/10.1016/j.beem.2008.09.012DOI Listing
December 2008

New therapeutic approaches to treat medullary thyroid carcinoma.

Nat Clin Pract Endocrinol Metab 2008 Jan;4(1):22-32

University Paris-Sud 11, Paris, France.

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http://dx.doi.org/10.1038/ncpendmet0717DOI Listing
January 2008

Constitutive and AP20187-induced Ret activation in photoreceptors does not protect from light-induced damage.

Invest Ophthalmol Vis Sci 2007 Nov;48(11):5199-206

Telethon Institute of Genetics and Medicine (TIGEM), Naples, Italy.

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http://dx.doi.org/10.1167/iovs.07-0140DOI Listing
November 2007

Receptor- and non-receptor tyrosine kinases induce processing of the amyloid precursor protein: role of the low-density lipoprotein receptor-related protein.

Neurodegener Dis 2007 ;4(2-3):94-100

CEINGE Biotecnologie Avanzate, Dipartimento di Biochimica e Biotecnologie Mediche, Università di Napoli Federico II, Napoli, Italia.

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http://dx.doi.org/10.1159/000101833DOI Listing
October 2007

Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants.

Clin Cancer Res 2007 Jun;13(11):3363-9

Istituto di Endocrinologia ed Oncologia Sperimentale del CNR, Dipartimento di Biologia e Patologia Cellulare e Molecolare, Università di Napoli Federico II, Naples, Italy.

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http://dx.doi.org/10.1158/1078-0432.CCR-06-2667DOI Listing
June 2007

Activation of the Erk8 mitogen-activated protein (MAP) kinase by RET/PTC3, a constitutively active form of the RET proto-oncogene.

J Biol Chem 2006 Apr 16;281(15):10567-76. Epub 2006 Feb 16.

Dipartimento di Biologia e Patologia Cellulare e Molecolare, Università degli Studi di Napoli Federico II, Via Pansini 5, 80131 Naples, Italy.

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http://www.jbc.org/lookup/doi/10.1074/jbc.M513397200
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http://dx.doi.org/10.1074/jbc.M513397200DOI Listing
April 2006

Clinical case seminar: in vivo and in vitro characterization of a novel germline RET mutation associated with low-penetrant nonaggressive familial medullary thyroid carcinoma.

J Clin Endocrinol Metab 2006 Mar 29;91(3):754-9. Epub 2005 Dec 29.

Unit of Endocrinology and Division of Anatomic Pathology, Istituto di Ricovero e Cura a Carattere Scientifico-Csa Sollievo della Sofferenza Hospital, Foggia, Italy.

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http://dx.doi.org/10.1210/jc.2005-2338DOI Listing
March 2006

BAY 43-9006 inhibition of oncogenic RET mutants.

J Natl Cancer Inst 2006 Mar;98(5):326-34

Istituto di Endocrinologia ed Oncologia Sperimentale del CNR, Dipartimento di Biologia e Patologia Cellulare e Molecolare, Università di Napoli Federico II, Naples, Italy.

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http://jnci.oxfordjournals.org/content/98/5/326.full.pdf
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http://jnci.oxfordjournals.org/cgi/doi/10.1093/jnci/djj069
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http://dx.doi.org/10.1093/jnci/djj069DOI Listing
March 2006

BRAF is a therapeutic target in aggressive thyroid carcinoma.

Clin Cancer Res 2006 Mar;12(5):1623-9

Istituto di Endocrinologia ed Oncologia Sperimentale del Consiglio Nazionale delle Ricerche, c/o Dipartimento di Biologia e Patologia Cellulare e Molecolare, Università di Napoli Federico II, Naples, Italy.

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http://clincancerres.aacrjournals.org/cgi/doi/10.1158/1078-0
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http://dx.doi.org/10.1158/1078-0432.CCR-05-2378DOI Listing
March 2006

Drug insight: Small-molecule inhibitors of protein kinases in the treatment of thyroid cancer.

Nat Clin Pract Endocrinol Metab 2006 Jan;2(1):42-52

Department of Cellular and Molecular Biology and Pathology L Califano, University Federico II, Naples, Italy.

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http://www.nature.com/doifinder/10.1038/ncpendmet0073
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http://dx.doi.org/10.1038/ncpendmet0073DOI Listing
January 2006

Receptor tyrosine kinases as targets for anticancer therapeutics.

Curr Med Chem 2005 ;12(15):1773-81

Istituto di Endocrinologia ed Oncologia Sperimentale del CNR/Dipartimento di Biologia e Patologia Cellulare e Molecolare, Universita' di Napoli Federico II, via S. Pansini 5, 80131 Napoli, Italy.

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http://dx.doi.org/10.2174/0929867054367266DOI Listing
October 2005

Mitogenic effects of the up-regulation of minichromosome maintenance proteins in anaplastic thyroid carcinoma.

J Clin Endocrinol Metab 2005 Aug 17;90(8):4703-9. Epub 2005 May 17.

Istituto di Endocrinologia ed Oncologia Sperimentale del Consiglio Nazionale delle Ricerche, Dipartimento di Biologia e Patologia Cellulare e Molecolare L. Califano, via S. Pansini 5, 80131 Naples, Italy.

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http://dx.doi.org/10.1210/jc.2004-2459DOI Listing
August 2005

Minireview: RET: normal and abnormal functions.

Endocrinology 2004 Dec 26;145(12):5448-51. Epub 2004 Aug 26.

Dipartimento di Biologia e Patologia Cellulare e Molecolare, University Federico II c/o Istituto di Endocrinologia ed Oncologia Sperimentale del Consiglio Nazionale delle Ricerche, Naples, Italy.

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http://dx.doi.org/10.1210/en.2004-0922DOI Listing
December 2004

Disease associated mutations at valine 804 in the RET receptor tyrosine kinase confer resistance to selective kinase inhibitors.

Oncogene 2004 Aug;23(36):6056-63

Dipartimento di Biologia e Patologia Cellulare e Molecolare, University 'Federico II', c/o Istituto di Endocrinologia ed Oncologia Sperimentale del CNR, via S. Pansini 5, Napoli, Italia.

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http://dx.doi.org/10.1038/sj.onc.1207810DOI Listing
August 2004

Regulation of p27Kip1 protein levels contributes to mitogenic effects of the RET/PTC kinase in thyroid carcinoma cells.

Cancer Res 2004 Jun;64(11):3823-9

Dipartimento di Biologia e Patologia Cellulare e Molecolare, University 'Federico II' c/o Istituto di Endocrinologia ed Oncologia Sperimentale, Consiglio Nazionale delle Ricerche, Naples, Italy.

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http://dx.doi.org/10.1158/0008-5472.CAN-03-3918DOI Listing
June 2004

Protein kinase Calpha activation by RET: evidence for a negative feedback mechanism controlling RET tyrosine kinase.

Oncogene 2003 May;22(19):2942-9

Dipartimento di Biologia e Patologia Cellulare e Molecolare 'L Califano', Università degli Studi di Napoli 'Federico II', via S Pansini 5, 80131 Napoli, Italy.

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http://dx.doi.org/10.1038/sj.onc.1206475DOI Listing
May 2003

Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine (PP2).

J Clin Endocrinol Metab 2003 Apr;88(4):1897-902

Istituto di Endocrinologia ed Oncologia Sperimentale del Consiglio Nazionale delle Ricerche c/o Dipartimento di Biologia e Patologia Cellulare e Molecolare L. Califano, Università Federico II, 80131 Naples, Italy.

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http://dx.doi.org/10.1210/jc.2002-021278DOI Listing
April 2003

ZD6474, an orally available inhibitor of KDR tyrosine kinase activity, efficiently blocks oncogenic RET kinases.

Cancer Res 2002 Dec;62(24):7284-90

Istituto di Endocrinologia ed Oncologia Sperimentale del Consiglio Nazionale delle Ricerche, Dipartimento di Biologia e Patologia Cellulare e Molecolare Luigi Califano, University Federico II, Naples, Italy.

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December 2002

Molecular mechanisms of RET activation in human cancer.

Ann N Y Acad Sci 2002 Jun;963:116-21

Centro di Endocrinologia ed Oncologia Sperimentale del CNR c/o Dipartimento di Biologia e Patologia Cellulare e Molecolare, Facoltá di Medicina e Chirurgia, Universitá di Napoli Federico II, 80131 Naples, Italy.

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http://dx.doi.org/10.1111/j.1749-6632.2002.tb04102.xDOI Listing
June 2002

The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes.

Cancer Res 2002 Feb;62(4):1077-82

Centro di Endocrinologia ed Oncologia Sperimentale del CNR c/o Dipartimento di Biologia e Patologia Cellulare e Molecolare L. Califano, Facoltà di Medicina e Chirurgia, Università di Napoli Federico II, 80131 Naples, Italy.

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February 2002