Publications by authors named "Giuseppe Campiani"

100Publications

Cinnamides Target Arginase Selectively.

Molecules 2020 Nov 12;25(22). Epub 2020 Nov 12.

Laboratório de Farmacologia e Bioquímica (LFBq), Departamento de Medicina Veterinária, Universidade de São Paulo Faculdade de Zootecnia e Engenharia de Alimentos, Pirassununga, SP 13635-900, Brazil.

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November 2020

Modulation of the Innate Immune Response by Targeting Toll-like Receptors: A Perspective on Their Agonists and Antagonists.

J Med Chem 2020 11 15;63(22):13466-13513. Epub 2020 Sep 15.

Department of Biotechnology, Chemistry and Pharmacy, Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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November 2020

Retinitis Pigmentosa and Retinal Degenerations: Deciphering Pathways and Targets for Drug Discovery and Development.

ACS Chem Neurosci 2020 08 9;11(15):2173-2191. Epub 2020 Jul 9.

Department of Biotechnology, Chemistry and Pharmacy, Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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August 2020

Computer-Driven Development of an in Silico Tool for Finding Selective Histone Deacetylase 1 Inhibitors.

Molecules 2020 Apr 22;25(8). Epub 2020 Apr 22.

Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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April 2020

Telomerase-based Cancer Therapeutics: A Review on their Clinical Trials.

Curr Top Med Chem 2020 ;20(6):433-457

Department of Biotechnology, Chemistry and Pharmacy, Department of Excellence 2018-2022, via Aldo Moro 2, I- 53100 Siena, University of Siena, Siena, Italy.

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December 2020

A Repurposing Approach for Uncovering the Anti-Tubercular Activity of FDA-Approved Drugs with Potential Multi-Targeting Profiles.

Molecules 2019 Nov 29;24(23). Epub 2019 Nov 29.

Department of Biotechnology (DoE 2018-2022), Chemistry and Pharmacy (DoE 2018-2022), University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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November 2019

Autophagy modulators for the treatment of oral and esophageal squamous cell carcinomas.

Med Res Rev 2020 05 19;40(3):1002-1060. Epub 2019 Nov 19.

Department of Biotechnology, Chemistry, and Pharmacy, Department of Excellence 2018-2022, University of Siena, Siena, Italy.

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May 2020

An integrated in silico screening strategy for identifying promising disruptors of p53-MDM2 interaction.

Comput Biol Chem 2019 Dec 16;83:107105. Epub 2019 Aug 16.

Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126, Pisa, Italy.

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December 2019

Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.

J Med Chem 2020 01 27;63(1):23-39. Epub 2019 Aug 27.

Department of Biotechnology, Chemistry and Pharmacy, Department of Excellence 2018-2022 , University of Siena , via Aldo Moro 2 , 53100 , Siena , Italy.

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January 2020

Raising the bar in anticancer therapy: recent advances in, and perspectives on, telomerase inhibitors.

Drug Discov Today 2019 07 25;24(7):1370-1388. Epub 2019 May 25.

University of Siena, Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, via Aldo Moro 2, I-53100 Siena, Italy. Electronic address:

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July 2019

Dietary polyphenols rutin, taxifolin and quercetin related compounds target Leishmania amazonensis arginase.

Food Funct 2019 Jun;10(6):3172-3180

Departamento de Medicina Veterinária, Faculdade de Zootecnia e Engenharia de Alimentos, Universidade de São Paulo, Avenida Duque de Caxias Norte, 225, 13635-900 Pirassununga, SP, Brazil.

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June 2019

A light in the dark: state of the art and perspectives in optogenetics and optopharmacology for restoring vision.

Future Med Chem 2019 03 25;11(5):463-487. Epub 2019 Mar 25.

Department of Biotechnology, Chemistry & Pharmacy, Department of Excellence 2018-2022, University of Siena, Via A. Moro 2, 53100 Siena, Italy.

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March 2019

Allosteric Modulation of Ionotropic Glutamate Receptors: An Outlook on New Therapeutic Approaches To Treat Central Nervous System Disorders.

ACS Med Chem Lett 2019 Mar 23;10(3):228-236. Epub 2019 Jan 23.

Department of Biotechnology, Chemistry and Pharmacy, University of Siena, DoE Department of Excellence 2018-2022, via Aldo Moro 2, I-53100 Siena, Italy.

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March 2019

Author Correction: The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.

Sci Rep 2018 Dec 14;8(1):17977. Epub 2018 Dec 14.

Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, Msida, Malta.

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December 2018

Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents.

Eur J Med Chem 2019 Jan 3;162:290-320. Epub 2018 Nov 3.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, via Aldo Moro 2, I-53100, Siena, Italy; Istituto Toscano Tumori, University of Siena, via Aldo Moro 2, I-53100, Siena, Italy; Department of Pharmacy, University of Napoli Federico II, DoE Department of Excellence 2018-2022, Via D. Montesano 49, 80131, Napoli, Italy.

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January 2019

Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.

Eur J Med Chem 2018 Sep 31;157:127-138. Epub 2018 Jul 31.

European Research Centre for Drug Discovery and Development (NatSynDrugs) and Department of Biotechnology, Chemistry, and Pharmacy, Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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September 2018

Development of Potent Inhibitors of Fatty Acid Amide Hydrolase Useful for the Treatment of Neuropathic Pain.

ChemMedChem 2018 10 30;13(19):2090-2103. Epub 2018 Aug 30.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Department of Biotechnology, Chemistry, and Pharmacy (DoE 2018-2020), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy.

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October 2018

Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues.

Eur J Med Chem 2018 Apr 10;150:698-718. Epub 2018 Mar 10.

Department of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.

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April 2018

Author Correction: The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.

Sci Rep 2018 Mar 12;8(1):4648. Epub 2018 Mar 12.

Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, Msida, Malta.

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March 2018

Activation of the Wnt Pathway by Small Peptides: Rational Design, Synthesis and Biological Evaluation.

ChemMedChem 2017 12 29;12(24):2074-2085. Epub 2017 Nov 29.

European Research Centre for Drug Discovery and Development, NatSynDrugs and Department of Biotechnology, Chemistry, and Pharmacy, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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December 2017

The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.

Sci Rep 2017 09 11;7(1):11152. Epub 2017 Sep 11.

Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, Msida, Malta.

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September 2017

First dual AK/GSK-3β inhibitors endowed with antioxidant properties as multifunctional, potential neuroprotective agents.

Eur J Med Chem 2017 Sep 9;138:438-457. Epub 2017 Jun 9.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Department of Biotechnology, Chemistry, and Pharmacy, Università degli Studi di Siena via Aldo Moro 2, 53100 Siena, Italy.

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September 2017

Computational Tool for Fast Evaluation of ERG K Channel Affinity.

Front Chem 2017 23;5. Epub 2017 Feb 23.

European Research Centre for Drug Discovery (NatSynDrugs), University of SienaSiena, Italy.

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February 2017

Structural characterization of Giardia duodenalis thioredoxin reductase (gTrxR) and computational analysis of its interaction with NBDHEX.

Eur J Med Chem 2017 Jul 24;135:479-490. Epub 2017 Apr 24.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Department of Biotechnology, Chemistry, and Pharmacy, Università di Siena via Aldo Moro 2, 53100 Siena, Italy.

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July 2017

Identification of novel fluorescent probes preventing PrP replication in prion diseases.

Eur J Med Chem 2017 Feb 1;127:859-873. Epub 2016 Nov 1.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy.

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February 2017

Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases.

Front Neurosci 2016 5;10:451. Epub 2016 Oct 5.

European Research Centre for Drug Discovery and Development and Department of Biotechnology, Chemistry and Pharmacy, University of Siena Siena, Italy.

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October 2016

Phenylpyrrole-based HDAC inhibitors: synthesis, molecular modeling and biological studies.

Future Med Chem 2016 09 24;8(13):1573-87. Epub 2016 Aug 24.

European Research Centre for Drug Discovery & Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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September 2016

Involvement of AMP-activated protein kinase in mediating pyrrolo-1,5-benzoxazepine-induced apoptosis in neuroblastoma cells.

Invest New Drugs 2016 10 22;34(5):663-76. Epub 2016 Jun 22.

School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, 152-160 Pearse Street, Dublin 2, Ireland.

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October 2016

Targeting clinically-relevant metallo-β-lactamases: from high-throughput docking to broad-spectrum inhibitors.

J Enzyme Inhib Med Chem 2016 28;31(sup1):98-109. Epub 2016 Apr 28.

a European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena , Siena , Italy.

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February 2017

Verbascoside Inhibits Promastigote Growth and Arginase Activity of Leishmania amazonensis.

J Nat Prod 2016 05 20;79(5):1459-63. Epub 2016 Apr 20.

Department of Veterinary Medicine, Universidade de São Paulo , Avenida Duque de Caxias Norte, 225, 13635-900 Pirassununga, SP, Brazil.

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May 2016

In silico study of subtilisin-like protease 1 (SUB1) from different Plasmodium species in complex with peptidyl-difluorostatones and characterization of potent pan-SUB1 inhibitors.

J Mol Graph Model 2016 Mar 19;64:121-130. Epub 2016 Jan 19.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100, Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.

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March 2016

Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.

Eur J Med Chem 2016 Oct 9;121:864-879. Epub 2015 Oct 9.

Laboratory of Medicinal Chemistry (IQOG, CSIC), C/Juan de la Cierva 3, 28006 Madrid, Spain. Electronic address:

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October 2016

Exploring clotrimazole-based pharmacophore: 3D-QSAR studies and synthesis of novel antiplasmodial agents.

Bioorg Med Chem Lett 2015 Nov 5;25(22):5412-8. Epub 2015 Sep 5.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.

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November 2015

Endocannabinoid Modulation of Predator Stress-Induced Long-Term Anxiety in Rats.

Neuropsychopharmacology 2016 Apr 11;41(5):1329-39. Epub 2015 Sep 11.

Department of Anatomy and Neurobiology, University of California, Irvine, CA, USA.

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April 2016

Unconventional Knoevenagel-type indoles: Synthesis and cell-based studies for the identification of pro-apoptotic agents.

Eur J Med Chem 2015 Sep 8;102:648-60. Epub 2015 Aug 8.

Dipartimento di Scienze Biomediche, Sezione di Microbiologia e Virologia, Università di Cagliari, Cittadella Universitaria, s.p. 8, Km 0.700, I-09042 Monserrato, Cagliari, Italy.

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September 2015

Induction of apoptosis in oral squamous carcinoma cells by pyrrolo-1,5-benzoxazepines.

Mol Med Rep 2015 Sep 25;12(3):3748-3754. Epub 2015 May 25.

School of Dental Science, Trinity College Dublin, Dublin 2, Ireland.

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September 2015

Structure-based discovery of the first non-covalent inhibitors of Leishmania major tryparedoxin peroxidase by high throughput docking.

Sci Rep 2015 May 7;5:9705. Epub 2015 May 7.

1] European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100, Siena [2] Dip. di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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May 2015

Disease-modifying anti-Alzheimer's drugs: inhibitors of human cholinesterases interfering with β-amyloid aggregation.

CNS Neurosci Ther 2014 Jul;20(7):624-32

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, Siena, Italy.

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July 2014

Rational design of the first difluorostatone-based PfSUB1 inhibitors.

Bioorg Med Chem Lett 2014 Aug 23;24(15):3582-6. Epub 2014 May 23.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100 Siena, Italy; Dip. di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100 Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.

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August 2014

Multifunctional cholinesterase and amyloid Beta fibrillization modulators. Synthesis and biological investigation.

ACS Med Chem Lett 2013 Dec 6;4(12):1178-82. Epub 2013 Oct 6.

European Research Centre for Drug Discovery and Development-NatSynDrugs and Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena , via Aldo Moro 2, 53100 Siena, Italy ; European Research Centre for Drug Discovery and Development-NatSynDrugs and Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena , via Aldo Moro 2, 53100 Siena, Italy.

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December 2013

Synthesis and structure-activity relationship studies in serotonin 5-HT4 receptor ligands based on a benzo[de][2,6]naphthridine scaffold.

Eur J Med Chem 2014 Jul 5;82:36-46. Epub 2014 May 5.

Dipartimento di Biotecnologie, Chimica e Farmacia and European Research Centre for Drug Discovery and Development, Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy. Electronic address:

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July 2014

The novel pyrrolo-1,5-benzoxazepine, PBOX-6, synergistically enhances the apoptotic effects of carboplatin in drug sensitive and multidrug resistant neuroblastoma cells.

Biochem Pharmacol 2014 Feb 6;87(4):611-24. Epub 2014 Jan 6.

School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, 152-160 Pearse Street, Dublin 2, Ireland. Electronic address:

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February 2014

A stereoselective approach to peptidomimetic BACE1 inhibitors.

Eur J Med Chem 2013 6;70:233-47. Epub 2013 Oct 6.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100 Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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September 2014

HCV-targeted antivirals: current status and future challenges.

Curr Pharm Des 2014 ;20(21):3445-64

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università di Siena, via Aldo Moro 2, 53100, Siena (Italy).

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March 2015

The structural evolution of β-secretase inhibitors: a focus on the development of small-molecule inhibitors.

Curr Top Med Chem 2013 ;13(15):1787-807

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro, 2, 53100 Siena, Italy.

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March 2014

Inhibition of late-stage autophagy synergistically enhances pyrrolo-1,5-benzoxazepine-6-induced apoptotic cell death in human colon cancer cells.

Int J Oncol 2013 Sep 25;43(3):927-35. Epub 2013 Jun 25.

School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, Dublin 2, Ireland.

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September 2013

Novel peptidomimetics as BACE-1 inhibitors: synthesis, molecular modeling, and biological studies.

Bioorg Med Chem Lett 2013 Jan 14;23(1):85-9. Epub 2012 Nov 14.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena, Via Aldo Moro 2, 53100 Siena, Italy.

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January 2013

A straightforward approach for engineering efficacy and selectivity at GPCRs.

J Med Chem 2012 Aug 18;55(15):6687-8. Epub 2012 Jul 18.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.

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August 2012

Quinolylhydrazones as novel inhibitors of Plasmodium falciparum serine protease PfSUB1.

Bioorg Med Chem Lett 2012 Aug 23;22(16):5317-21. Epub 2012 Jun 23.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via A. Moro, 53100 Siena, Italy.

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August 2012

Broad inhibition of plasmodium falciparum cytoadherence by (+)-epigallocatechin gallate.

Malar J 2011 Dec 1;10:348. Epub 2011 Dec 1.

European Research Centre for Drug Discovery and Development, Department of Pharmaceutical and Applied Chemistry, University of Siena, Italy.

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December 2011

Malaria chemotherapy: recent advances in drug development.

Recent Pat Antiinfect Drug Discov 2010 Nov;5(3):195-225

Department of Pharmaceutical and Applied Chemistry, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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November 2010

Paclitaxel directly binds to Bcl-2 and functionally mimics activity of Nur77.

Cancer Res 2009 Sep 11;69(17):6906-14. Epub 2009 Aug 11.

Laboratory of Antineoplastic Pharmacology, Department of Obstetrics and Gynecology, Catholic University of the Sacred Heart, Rome, Italy.

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September 2009