Publications by authors named "Antonello Mai"

100Publications

Lysine Acetyltransferase Inhibitors From Natural Sources.

Front Pharmacol 2020 12;11:1243. Epub 2020 Aug 12.

Department of Chemistry and Technology of Drugs, Sapienza University of Rome, Rome, Italy.

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http://dx.doi.org/10.3389/fphar.2020.01243DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7434864PMC
August 2020

Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs).

Eur J Med Chem 2020 Dec 18;207:112750. Epub 2020 Aug 18.

Department of Chemistry and Technology of Drugs, "Sapienza" University of Rome, 00185, Rome, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2020.112750DOI Listing
December 2020

The Innovative Potential of Statins in Cancer: New Targets for New Therapies.

Front Chem 2020 18;8:516. Epub 2020 Jun 18.

Department of Drug Chemistry and Technologies, Sapienza University of Rome, Rome, Italy.

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http://dx.doi.org/10.3389/fchem.2020.00516DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7312214PMC
June 2020

Targeting histone acetylation/deacetylation in parasites: an update (2017-2020).

Curr Opin Chem Biol 2020 08 29;57:65-74. Epub 2020 Jun 29.

Department of Chemistry and Technologies of Drugs, Sapienza University of Rome, P. le A. Moro 5, 00185, Rome, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.cbpa.2020.05.008DOI Listing
August 2020

Diphenylene Iodonium Is a Noncovalent MAO Inhibitor: A Biochemical and Structural Analysis.

ChemMedChem 2020 Aug 10;15(15):1394-1397. Epub 2020 Jun 10.

Department of Biology and Biotechnology "Lazzaro Spallanzani", University of Pavia, Via Ferrata 9, 27100, Pavia, Italy.

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http://dx.doi.org/10.1002/cmdc.202000264DOI Listing
August 2020

Sirt4: A Multifaceted Enzyme at the Crossroads of Mitochondrial Metabolism and Cancer.

Front Oncol 2020 15;10:474. Epub 2020 Apr 15.

Department of Chemistry and Technology of Drugs, "Sapienza" University of Rome, Rome, Italy.

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http://dx.doi.org/10.3389/fonc.2020.00474DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7177044PMC
April 2020

Discovery of the First Human Arylsulfatase A Reversible Inhibitor Impairing Mouse Oocyte Fertilization.

ACS Chem Biol 2020 06 14;15(6):1349-1357. Epub 2020 Apr 14.

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.

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http://dx.doi.org/10.1021/acschembio.9b00999DOI Listing
June 2020

Sirtuin modulators: where are we now? A review of patents from 2015 to 2019.

Expert Opin Ther Pat 2020 Jun 13;30(6):389-407. Epub 2020 Apr 13.

Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma, Rome, Italy.

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http://dx.doi.org/10.1080/13543776.2020.1749264DOI Listing
June 2020

A closer look into NADPH oxidase inhibitors: Validation and insight into their mechanism of action.

Redox Biol 2020 05 15;32:101466. Epub 2020 Feb 15.

Department of Biology and Biotechnology "Lazzaro Spallanzani", University of Pavia, Via Ferrata 9, 27100, Pavia, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.redox.2020.101466DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7042484PMC
May 2020

Inhibition of class I HDACs imprints adipogenesis toward oxidative and brown-like phenotype.

Biochim Biophys Acta Mol Cell Biol Lipids 2020 04 2;1865(4):158594. Epub 2020 Jan 2.

Dipartimento di Scienze Farmacologiche e Biomolecolari, Università degli Studi di Milano, Milano, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.bbalip.2019.158594DOI Listing
April 2020

Structure-Reactivity Relationships on Substrates and Inhibitors of the Lysine Deacylase Sirtuin 2 from (Sirt2).

J Med Chem 2019 10 20;62(19):8733-8759. Epub 2019 Sep 20.

Institute of Pharmaceutical Sciences , University of Freiburg , Albertstr. 25 , 79104 Freiburg , Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00638DOI Listing
October 2019

Epigenetic polypharmacology: A new frontier for epi-drug discovery.

Med Res Rev 2020 01 20;40(1):190-244. Epub 2019 Jun 20.

Department of Chemistry and Technologies of Drugs, "Sapienza" University of Rome, Rome, Italy.

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http://dx.doi.org/10.1002/med.21600DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6917854PMC
January 2020

Histone Deacetylases Contribute to Excitotoxicity-Triggered Degeneration of Retinal Ganglion Cells In Vivo.

Mol Neurobiol 2019 Dec 3;56(12):8018-8034. Epub 2019 Jun 3.

Neurobiology, Interdisciplinary Center for Neurosciences, Heidelberg University, Im Neuenheimer Feld 366, 69120, Heidelberg, Germany.

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http://dx.doi.org/10.1007/s12035-019-01658-xDOI Listing
December 2019

α,γ-Diketocarboxylic Acids and Their Esters Act as Carbonic Anhydrase IX and XII Selective Inhibitors.

ACS Med Chem Lett 2019 Apr 19;10(4):661-665. Epub 2019 Feb 19.

Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Via U. Schiff 6, 50019 Sesto Fiorentino, Firenze, Italy.

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http://dx.doi.org/10.1021/acsmedchemlett.9b00023DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6466837PMC
April 2019

Histone deacetylases as an epigenetic pillar for the development of hybrid inhibitors in cancer.

Curr Opin Chem Biol 2019 06 12;50:89-100. Epub 2019 Apr 12.

Department of Chemistry and Technologies of Drugs, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S13675931193001
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http://dx.doi.org/10.1016/j.cbpa.2019.03.002DOI Listing
June 2019

Comparison of the effects of synthetic and plant-derived mTOR regulators on healthy human ovarian cells.

Eur J Pharmacol 2019 Jul 5;854:70-78. Epub 2019 Apr 5.

King Saud University, Department of Zoology, College of Science, Riyadh, 11451, Saudi Arabia.

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http://dx.doi.org/10.1016/j.ejphar.2019.03.048DOI Listing
July 2019

The emerging role of epigenetics in human autoimmune disorders.

Clin Epigenetics 2019 02 26;11(1):34. Epub 2019 Feb 26.

Department of Chemistry and Technologies of Drugs, Sapienza University of Rome, P.le A. Moro 5, 00185, Rome, Italy.

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https://clinicalepigeneticsjournal.biomedcentral.com/article
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http://dx.doi.org/10.1186/s13148-019-0632-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6390373PMC
February 2019

Histone deacetylase inhibitors exert anti-tumor effects on human adherent and stem-like glioma cells.

Clin Epigenetics 2019 01 17;11(1):11. Epub 2019 Jan 17.

Laboratory of Molecular Neurobiology, Neurobiology Center, The Nencki Institute of Experimental Biology, 3 Pasteur Str, 02-093, Warsaw, Poland.

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http://dx.doi.org/10.1186/s13148-018-0598-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6337817PMC
January 2019

Intergenerational inheritance of high fat diet-induced cardiac lipotoxicity in Drosophila.

Nat Commun 2019 01 14;10(1):193. Epub 2019 Jan 14.

Development, Aging and Regeneration Program, Sanford-Burnham-Prebys Medical Discovery Institute, 10901 N. Torrey Pines Road, La Jolla, CA, 92037, USA.

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http://dx.doi.org/10.1038/s41467-018-08128-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6331650PMC
January 2019

Application of Small Epigenetic Modulators in Pediatric Medulloblastoma.

Front Pediatr 2018 3;6:370. Epub 2018 Dec 3.

Department of Drug Chemistry and Technologies, Sapienza University of Rome, Rome, Italy.

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http://dx.doi.org/10.3389/fped.2018.00370DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6286966PMC
December 2018

Identification of novel quinazoline derivatives as potent antiplasmodial agents.

Eur J Med Chem 2019 Jan 17;161:277-291. Epub 2018 Oct 17.

CIIL U1019-CNRS UMR 8204, Université de Lille, Institut Pasteur de Lille, 1 rue du Professeur Calmette, 59019, Lille, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2018.10.041DOI Listing
January 2019

Six Years (2012-2018) of Researches on Catalytic EZH2 Inhibitors: The Boom of the 2-Pyridone Compounds.

Chem Rec 2018 Dec 19;18(12):1818-1832. Epub 2018 Oct 19.

Department of Chemistry and Technologies of Drugs, Sapienza University of Rome, P.le Aldo Moro n. 5., 00185, Roma, Italy.

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https://onlinelibrary.wiley.com/doi/abs/10.1002/tcr.20180009
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http://dx.doi.org/10.1002/tcr.201800091DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7410397PMC
December 2018

Epigenetic Metalloenzymes.

Curr Med Chem 2019 ;26(15):2748-2785

Réseau Epigénétique du Cancéropôle Grand Ouest, France.

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http://www.eurekaselect.com/163573/article
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http://dx.doi.org/10.2174/0929867325666180706105903DOI Listing
September 2019

Trends of LSD1 inhibitors in viral infections.

Future Med Chem 2018 05 22;10(10):1133-1136. Epub 2018 May 22.

Department of Drug Chemistry & Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy.

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http://dx.doi.org/10.4155/fmc-2018-0065DOI Listing
May 2018

Lysine acetyltransferase inhibitors: structure-activity relationships and potential therapeutic implications.

Future Med Chem 2018 05 20;10(9):1067-1091. Epub 2018 Apr 20.

Department of Drug Chemistry & Technologies, Sapienza University of Rome, P.le A Moro 5, 00185 Rome, Italy.

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http://dx.doi.org/10.4155/fmc-2017-0244DOI Listing
May 2018

Disruptor of telomeric silencing 1-like (DOT1L): disclosing a new class of non-nucleoside inhibitors by means of ligand-based and structure-based approaches.

J Comput Aided Mol Des 2018 03 15;32(3):435-458. Epub 2018 Jan 15.

Rome Center for Molecular Design, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, P. le A. Moro 5, 00185, Roma, Italy.

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http://dx.doi.org/10.1007/s10822-018-0096-zDOI Listing
March 2018

Effect of Class II HDAC inhibition on glutamate transporter expression and survival in SOD1-ALS mice.

Neurosci Lett 2017 Aug 19;656:120-125. Epub 2017 Jul 19.

Department of Health Sciences, Section of Clinical Pharmacology and Oncology, University of Florence, Italy.

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http://dx.doi.org/10.1016/j.neulet.2017.07.033DOI Listing
August 2017

Epi-drugs in combination with immunotherapy: a new avenue to improve anticancer efficacy.

Clin Epigenetics 2017 30;9:59. Epub 2017 May 30.

Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, P.le Aldo Moro 5, 00185 Rome, Italy.

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http://dx.doi.org/10.1186/s13148-017-0358-yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5450222PMC
March 2018

The relevance of K calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor.

Eur J Med Chem 2017 Aug 5;136:480-486. Epub 2017 May 5.

University of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2017.05.015DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5720340PMC
August 2017

EZH2 inhibitors: a patent review (2014-2016).

Expert Opin Ther Pat 2017 Jul 20;27(7):797-813. Epub 2017 Apr 20.

a Dipartimento di Chimica e Tecnologie del Farmaco , Sapienza Università di Roma , Rome , Italy.

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https://www.tandfonline.com/doi/full/10.1080/13543776.2017.1
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http://dx.doi.org/10.1080/13543776.2017.1316976DOI Listing
July 2017

Structure-Activity Relationships on Cinnamoyl Derivatives as Inhibitors of p300 Histone Acetyltransferase.

ChemMedChem 2017 08 12;12(16):1359-1368. Epub 2017 Apr 12.

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, P.le Aldo Moro 5, 00185, Roma, Italy.

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http://dx.doi.org/10.1002/cmdc.201700040DOI Listing
August 2017

Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.

J Med Chem 2017 06 15;60(12):4780-4804. Epub 2017 Mar 15.

Dipartimento di Chimica e Tecnologie del Farmaco "Sapienza" Università di Roma , 00185 Rome, Italy.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01595DOI Listing
June 2017

Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules.

Angew Chem Int Ed Engl 2017 01 19;56(4):1007-1011. Epub 2016 Dec 19.

Universität Bayreuth, Lehrstuhl Biochemie und Forschungszentrum für Biomakromoleküle, Universitätsstr. 30, 95447, Bayreuth, Germany.

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http://dx.doi.org/10.1002/anie.201610082DOI Listing
January 2017

Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity.

Bioorg Med Chem 2017 02 1;25(3):847-856. Epub 2016 Dec 1.

Department of Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy, University of Groningen, Antonius Deusinglaan 1, Groningen 9713 AV, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2016.11.043DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5292237PMC
February 2017

MC1568 inhibits HDAC6/8 activity and influenza A virus replication in lung epithelial cells: role of Hsp90 acetylation.

Future Med Chem 2016 Nov 14;8(17):2017-2031. Epub 2016 Oct 14.

Department of Public Health & Infectious Diseases, 'Sapienza' University of Rome, P.le A. Moro 5, 00185 Rome, Italy.

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http://www.future-science.com/doi/10.4155/fmc-2016-0073
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http://dx.doi.org/10.4155/fmc-2016-0073DOI Listing
November 2016

The emerging role of lysine methyltransferase SETD8 in human diseases.

Clin Epigenetics 2016;8:102. Epub 2016 Sep 22.

Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, Fisciano, I-84084 Salerno, Italy ; Epigenetic Med Chem Lab, Università degli Studi di Salerno, Via Giovanni Paolo II 132, Fisciano, I-84084 Salerno, Italy.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5034662PMC
http://dx.doi.org/10.1186/s13148-016-0268-4DOI Listing
September 2016

Progress in the Development of Lysine Methyltransferase SETD8 Inhibitors.

ChemMedChem 2016 08 14;11(16):1680-5. Epub 2016 Jul 14.

Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084, Fisciano, SA, Italy.

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http://dx.doi.org/10.1002/cmdc.201600272DOI Listing
August 2016

Sirtuin functions and modulation: from chemistry to the clinic.

Clin Epigenetics 2016 25;8:61. Epub 2016 May 25.

Dipartimento di Biochimica, Biofisica e Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. De Crecchio 7, 80138 Napoli, Italy.

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http://dx.doi.org/10.1186/s13148-016-0224-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4879741PMC
December 2016

Tumour-specific metabolic adaptation to acidosis is coupled to epigenetic stability in osteosarcoma cells.

Am J Cancer Res 2016 15;6(4):859-75. Epub 2016 Mar 15.

Orthopaedic Pathophysiology and Regenerative Medicine Unit, Istituto Ortopedico RizzoliBologna, Italy; Department of Biomedical and Neuromotor Sciences, University of BolognaBologna, Italy.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4859889PMC
May 2016

LSD1 inhibitors: a patent review (2010-2015).

Expert Opin Ther Pat 2016 May 28;26(5):565-80. Epub 2016 Mar 28.

a Dipartimento di Chimica e Tecnologie del Farmaco , Sapienza Università di Roma , Rome , Italy.

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http://www.tandfonline.com/doi/full/10.1517/13543776.2016.11
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http://dx.doi.org/10.1517/13543776.2016.1165209DOI Listing
May 2016

The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases.

Biochem Pharmacol 2016 Feb 21;102:130-140. Epub 2015 Dec 21.

Pharmaceutical Gene Modulation, Groningen Research Institute of Pharmacy, University of Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.bcp.2015.12.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4871277PMC
February 2016

Enzyme kinetics and inhibition of histone acetyltransferase KAT8.

Eur J Med Chem 2015 Nov 22;105:289-96. Epub 2015 Oct 22.

Department of Pharmaceutical Gene Modulation, Groningen Research Institute of Pharmacy, University of Groningen, Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2015.10.016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4871228PMC
November 2015

Targeting Lysine Deacetylases (KDACs) in Parasites.

PLoS Negl Trop Dis 2015 24;9(9):e0004026. Epub 2015 Sep 24.

The Genome Institute, Washington University School of Medicine, St. Louis, Missouri, United States of America; Departments of Genetics and of Internal Medicine, Washington University School of Medicine, St. Louis, Missouri, United States of America.

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http://dx.doi.org/10.1371/journal.pntd.0004026DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4581690PMC
March 2016

Discovery of Inhibitors for the Ether Lipid-Generating Enzyme AGPS as Anti-Cancer Agents.

ACS Chem Biol 2015 Nov 4;10(11):2589-97. Epub 2015 Sep 4.

Department of Biology and Biotechnology, University of Pavia , via Ferrata 9, 27100 Pavia, Italy.

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http://dx.doi.org/10.1021/acschembio.5b00466DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4703096PMC
November 2015

DNA Methyltransferases Inhibitors from Natural Sources.

Curr Top Med Chem 2016 ;16(7):680-96

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.

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http://dx.doi.org/10.2174/1568026615666150825141505DOI Listing
August 2016

Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells.

J Med Chem 2015 May 30;58(9):4073-9. Epub 2015 Apr 30.

§Department of Drug Chemistry and Technologies, Sapienza University of Roma, P.le A. Moro 5, 00185 Roma, Italy.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.5b00126
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http://dx.doi.org/10.1021/acs.jmedchem.5b00126DOI Listing
May 2015

Emerging approaches for histone deacetylase inhibitor drug discovery.

Expert Opin Drug Discov 2015 Jun 20;10(6):599-613. Epub 2015 Apr 20.

Sapienza University of Rome, Department of Drug Chemistry and Technologies , Piazzale Aldo Moro 5, 00185 Rome , Italy +00390649913392 ; ;

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http://www.tandfonline.com/doi/full/10.1517/17460441.2015.10
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http://dx.doi.org/10.1517/17460441.2015.1038236DOI Listing
June 2015

A new water soluble MAPK activator exerts antitumor activity in melanoma cells resistant to the BRAF inhibitor vemurafenib.

Biochem Pharmacol 2015 May 17;95(1):16-27. Epub 2015 Mar 17.

The NAST Centre for Nanoscience & Nanotechnology & Innovative Instrumentation, University of "Tor Vergata", Rome, Italy; Department of Experimental Medicine and Surgery, University of "Tor Vergata", Rome, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.bcp.2015.03.004DOI Listing
May 2015