Giorgia Mori

University of Sydney

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Maria Rosalia Pasca

University of Pavia

Béatrice Silvia Orena

Fondazione IRCCS Ca' Granda Ospedale Maggiore Policlinico

Laurent R. Chiarelli

University of Pavia

Giovanna Riccardi

University of Pavia

Christian Lherbet

Molécules d'Intérêt Biologique

Michel Baltas

Laboratoire de Chimie de Coordination

Marco Giannetto

University of Parma

Francesco Dallavalle

University of Parma

A. Braibanti

University of Parma

Katarı́na Mikus̃ová

Comenius University Bratislava

Cooperative Institutions

University of Parma

Centre National de la Recherche Scientifique

University of Milan

University of Pavia

Université de Toulouse

Université Toulouse III - Paul Sabatier

Sapienza University of Rome

Istituti di Ricovero e Cura a Carattere Scientifico

University of Pisa

University of Modena and Reggio Emilia

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Ridotta attività degli osteoblasti nel mieloma multiplo: ruolo della sclerostina

Silvia Colucci Gian Luca Brunetti Angela Oranger Giorgia Mori Giorgina Specchia

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Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis

European Journal of Medicinal Chemistry (2013)

Tetiana Matviiuk Giorgia Mori Christian Lherbet Frédéric Rodriguez Maria Rosalia Pasca

INHA

Pyrrolidine

Michael reaction

10.1016/j.ejmech.2013.10.069

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Citations (47)

Effects of alpha-difluoromethylornithine on the Fas expression and apoptosis in Hep-2 cells.

PubMed (2000)

M. Gabriela Alvarez Carolina Marty Giorgia Mori Rivarola

DFMO is an irreversible inhibitor of ornithine decarboxilase (ODC), the key enzyme in mammalian polyamine biosynthesis, and has been shown to induce apoptosis. In this paper, the relation between the effects of DFMO on the polyamine content, apoptotic index and Fas expression in HEP-2 cells was determined. Fas is a type I membrane protein with a molecular mass of 45 kDa, which mediates apoptosis. The results suggest that the treatment with the polyamine inhibitor DFMO induced the expression of the surface antigen Fas, which could be responsible for trigger apoptosis in these cells.

Polyamine

Alpha (finance)

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Synthesis and evaluation of β-hydroxytriazoles and related compounds as antitubercular agents

French-Ukrainian Journal of Chemistry (2015)

Christophe Menendez Giorgia Mori Mathilde Maillot Isabelle Fabing Chantal Carayon

A new series of β-hydroxytriazoles were synthesized and evaluated as Mycobacterium tuberculosis inhibitors. Our strategy implied the synthesis of alkyne precursors through a Barbier reaction between benzaldehydes and propargyl bromide followed by click chemistry to afford substituted β-hydroxyl benzyltriazoles. These compounds are also key intermediates either for oxidation reactions leading to α,β-diketotriazoles or for elimination reactions affording styryl triazoles. Evaluation of all new compounds for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv resulted in compounds with MIC up to 7 μM.

Propargyl bromide

Propargyl

Alkyne

10.17721/fujcv3i1p82-96

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Citations (1)

Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043

ACS Medicinal Chemistry Letters (2016)

Rohit Tiwari Patricia A. Miller Laurent R. Chiarelli Giorgia Mori Michal Šarkan

Electron deficient nitroaromatic compounds such as BTZ043 and its closest congener, PBTZ169, and related agents are a promising new class of anti-TB compounds. Herein we report the design and syntheses of 1,3-benzothiazinone azide (BTZ-N3) and related click chemistry products based on the molecular mode of activation of BTZ043. Our computational docking studies indicate that BTZ-N3 binds in the essentially same pocket as that of BTZ043. Detailed biochemical studies with cell envelope enzyme fractions of Mycobacterium smegmatis combined with our model biochemical reactivity studies with nucleophiles indicated that, in contrast to BTZ043, the azide analogue may have a different mode of activation for anti-TB activity. Subsequent enzymatic studies with recombinant DprE1 from Mtb followed by MIC determination in NTB1 strain of Mtb (harboring Cys387Ser mutation in DprE1 and is BTZ043 resistant) unequivocally indicated that BTZ-N3 is an effective reversible and noncovalent inhibitor of DprE1.

Mycobacterium smegmatis

Docking (animal)

Molecular model

Reactivity

Rational design

10.1021/acsmedchemlett.5b00424

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Citations (62)

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

ACS Chemical Biology (2014)

João Neres Ruben C. Hartkoorn Laurent R. Chiarelli Ramakrishna Gadupudi Maria Rosalia Pasca

Phenotypic screening of a quinoxaline library against replicating Mycobacterium tuberculosis led to the identification of lead compound Ty38c (3-((4-methoxybenzyl)amino)-6-(trifluoromethyl)quinoxaline-2-carboxylic acid). With an MIC99 and MBC of 3.1 μM, Ty38c is bactericidal and active against intracellular bacteria. To investigate its mechanism of action, we isolated mutants resistant to Ty38c and sequenced their genomes. Mutations were found in rv3405c, coding for the transcriptional repressor of the divergently expressed rv3406 gene. Biochemical studies clearly showed that Rv3406 decarboxylates Ty38c into its inactive keto metabolite. The actual target was then identified by isolating Ty38c-resistant mutants of an M. tuberculosis strain lacking rv3406. Here, mutations were found in dprE1, encoding the decaprenylphosphoryl-d-ribose oxidase DprE1, essential for biogenesis of the mycobacterial cell wall. Genetics, biochemical validation, and X-ray crystallography revealed Ty38c to be a noncovalent, noncompetitive DprE1 inhibitor. Structure-activity relationship studies generated a family of DprE1 inhibitors with a range of IC50's and bactericidal activity. Co-crystal structures of DprE1 in complex with eight different quinoxaline analogs provided a high-resolution interaction map of the active site of this extremely vulnerable target in M. tuberculosis.

10.1021/cb5007163

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Citations (117)

CCDC 256812: Experimental Crystal Structure Determination

The Cambridge Structural Database (2005)

Roberto Cammi Marcello Gennari Marco Giannetto Maurizio Lanfranchi Luciano Marchiò

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

10.5517/cc8m78c

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Optimization of the DPV potential waveform for determination of ascorbic acid on PEDOT-modified electrodes

Sensors and Actuators B Chemical (2006)

Alessandra Bello Marco Giannetto Giorgia Mori Renato Seeber Fabio Terzi

Differential pulse voltammetry

10.1016/j.snb.2006.04.066

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Citations (74)

Analogous Mechanisms of Resistance to Benzothiazinones and Dinitrobenzamides in Mycobacterium smegmatis

PLoS ONE (2011)

Ana Ribeiro Giulia Degiacomi Fanny Ewann Silvia Buroni Maria Loreto Incandela

Tuberculosis is still a leading cause of death worldwide. The selection and spread of Mycobacterium tuberculosis multidrug-resistant (MDR-TB) and extensively drug-resistant strains (XDR-TB) is a severe public health problem. Recently, two different classes of chemical series, the benzothiazinones (BTZ) and the dinitrobenzamide (DNB) derivatives have been found to be highly active against M. tuberculosis, including XDR-TB strains. The target of BTZs is DprE1 protein which works in concert with DprE2 to form the heteromeric decaprenylphosphoryl-β-D-ribose 2′-epimerase, involved in Decaprenyl-Phospho-Arabinose (DPA) biosynthesis. Interestingly, it has been shown that the DNBs block the same pathway thus suggesting that both drugs could share the same target. Moreover, in Mycobacterium smegmatis the overexpression of the NfnB nitroreductase led to the inactivation of the BTZs by reduction of a critical nitro-group to an amino-group. In this work several spontaneous M. smegmatis mutants resistant to DNBs were isolated. Sixteen mutants, showing high levels of DNB resistance, exhibited a mutation in the Cys394 of DprE1. Using fluorescence titration and mass spectrometry it has been possible to monitor the binding between DprE1 and DNBs, achieving direct evidence that MSMEG_6382 is the cellular target of DNBs in mycobacteria. Additionally, M. smegmatis mutants having low levels of resistance to DNBs harbor various mutations in MSMEG_6503 gene encoding the transcriptional repressor of the nitroreductase NfnB. By LC/MS2 analysis it has been demonstrated that NfnB is responsible for DNB inactivation. Taken together, our data demonstrate that both DNB and BTZ drugs share common resistance mechanisms in M. smegmatis.

Mycobacterium smegmatis

Nitroreductase

10.1371/journal.pone.0026675

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Citations (50)

Development of Latent Fingerprints on Metallic Surfaces Using Electropolymerization Processes

Journal of Forensic Sciences (2001)

C Bersellini L Garofano Marco Giannetto F Lusardi Giorgia Mori

We propose a new process for developing latent fingerprints on metal items, applicable to unfired weapons made of Ergal in particular. The method is based on the presence of fatty acids that are contained in fingerprints and act as an insulator on the surface where fingerprints are to be developed. The process of polymerization occurs on the metal portions left untouched by finger contact. Hence, the developing process results as a negative pattern of the original fingerprint. The reaction consists in the electropolymerization of pyrrole and substituted porphyrins, i.e., tetra (o-aminophenyl) porphyrine: radical-cations are generated on superficial nucleation sites by oxidation of monomer, close to the electrode surface; subsequently, the radical species react with the neutral monomer, which begins to diffuse to the electrode. We have also studied the polymer's morphology by means of SEM and AFM, in order to find a correlation between the reagent to be used and the quality of the enhancement process. These are only preliminary results; however, they show that the suggested method is a new way to increase the rate of success in developing latent fingerprints on metal surfaces. In this regard, it may be considered complementary to other conventional procedures, due to the low costs of the instruments and reagents, and the rapidity and simplicity of the treatment.

Latent image

Pyrrole

10.1520/jfs15060j

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Citations (51)