Stefano Guglielmo

University of Turin

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Roberta Fruttero

University of Turin

Barbara Rolando

University of Turin

Konstantin Chegaev

University of Turin

Loretta Lazzarato

University of Turin

Alberto Gasco

University of Turin

Chiara Riganti

University of Turin

Marialessandra Contino

University of Bari Aldo Moro

Nicola Antonio Colabufo

University of Bari Aldo Moro

Daniela Cortese

University of Turin

Maria Grazia Perrone

University of Bari Aldo Moro

Cooperative Institutions

University of Turin

Universidade Estadual Paulista (Unesp)

Sapienza University of Rome

National Research Council

Centro Universitário de Araraquara

University of Parma

Universidade de São Paulo

Torino e-district

University of Bologna

Instituto de Ciências Farmacêuticas

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Involvement of a lateral entorhinal cortex engram in episodic-like memory recall

Cell Reports (2024)

Francesca Tozzi Stefano Guglielmo Camilla Paraciani Michel C. van den Oever Marco Mainardi

Entorhinal cortex

Engram

Long-term memory

10.1016/j.celrep.2024.114795

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Synthesis, Physicochemical Characterization, and Biological Activities of New Carnosine Derivatives Stable in Human Serum As Potential Neuroprotective Agents

Journal of Medicinal Chemistry (2010)

Massimo Bertinaria Barbara Rolando Marta Giorgis Gabriele Montanaro Stefano Guglielmo

The synthesis and the physicochemical and biological characterization of a series of carnosine amides bearing on the amido group alkyl substituents endowed with different lipophilicity are described. All synthesized products display carnosine-like properties differentiating from the lead for their high serum stability. They are able to complex Cu2+ ions at physiological pH with the same stoichiometry as carnosine. The newly synthesized compounds display highly significant copper ion sequestering ability and are capable of protecting LDL from oxidation catalyzed by Cu2+ ions, the most active compounds being the most hydrophilic ones. All the synthesized amides show quite potent carnosine-like HNE quenching activity; in particular, 7d, the member of the series selected for this kind of study, is able to cross the blood−brain barrier (BBB) and to protect primary mouse hippocampal neurons against HNE-induced death. These products can be considered metabolically stable analogues of carnosine and are worthy of additional investigation as potential neuroprotective agents.

Carnosine

Lipophilicity

10.1021/jm101394n

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Citations (40)

DerivativesFuroxan and Benzofuroxan Leishmanicidal Activities of Novel

Márcia A. S. Graminha Konstantin Chegaev Stefano Guglielmo Isabel Martínez Rosângela Gonçalves Peccinini

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Praziquantel analogues containing NO-donor furoxans and related furazans as agents active against Schistosoma mansoni.

Daniela Cortese Stefano Guglielmo Vottero Francesca V. a. l. e. r. i. e. P. Kommer David L. Williams

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Design, Biological Evaluation, and Molecular Modeling of Tetrahydroisoquinoline Derivatives: Discovery of A Potent P-Glycoprotein Ligand Overcoming Multidrug Resistance in Cancer Stem Cells

Journal of Medicinal Chemistry (2018)

Chiara Riganti Marialessandra Contino Stefano Guglielmo Maria Grazia Perrone Iris C. Salaroglio

P-Glycoprotein is a well-known membrane transporter responsible for the efflux of an ample spectrum of anticancer drugs. Its relevance in the management of cancer chemotherapy is increased in view of its high expression in cancer stem cells, a population of cancer cells with strong tumor-promoting ability. In the present study, a series of compounds were synthesized through structure modulation of [4′-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-ylmethyl)biphenyl-4-ol] (MC70), modifying the phenolic group of the lead compound. Among them, compound 5b emerged for its activity against the transporter (EC50 = 15 nM) and was capable of restoring doxorubicin antiproliferative activity at nontoxic concentration. Its behavior was rationalized through a molecular modeling study consisting of a well-tempered metadynamics simulation, which allowed one to identify the most favorable binding pose, and of a subsequent molecular dynamics run, which indicated a peculiar effect of the compound on the motion pattern of the transporter.

P-glycoprotein

Efflux

Tetrahydroisoquinoline

Metadynamics

Molecular model

10.1021/acs.jmedchem.8b01655

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Citations (26)

Glucocorticoids rescue cell surface trafficking of R451C Neuroligin3 and enhance synapse formation

Traffic (2024)

Tamara Diamanti Laura Trobiani Lorenza Mautone Federica Serafini Roberta Gioia

Abstract Neuroligins are synaptic cell adhesion proteins with a role in synaptic function, implicated in neurodevelopmental disorders. The autism spectrum disorder‐associated substitution Arg451Cys (R451C) in NLGN3 promotes a partial misfolding of the extracellular domain of the protein leading to retention in the endoplasmic reticulum (ER) and the induction of the unfolded protein response (UPR). The reduced trafficking of R451C NLGN3 to the cell surface leads to altered synaptic function and social behavior. A screening in HEK‐293 cells overexpressing NLGN3 of 2662 compounds (FDA‐approved small molecule drug library), led to the identification of several glucocorticoids such as alclometasone dipropionate, desonide, prednisolone sodium phosphate, and dexamethasone (DEX), with the ability to favor the exit of full‐length R451C NLGN3 from the ER. DEX improved the stability of R451C NLGN3 and trafficking to the cell surface, reduced the activation of the UPR, and increased the formation of artificial synapses between HEK‐293 and hippocampal primary neurons. The effect of DEX was validated on a novel model system represented by neural stem progenitor cells and differentiated neurons derived from the R451C NLGN3 knock‐in mouse, expressing the endogenous protein. This work shows a potential rescue strategy for an autism‐linked mutation affecting cell surface trafficking of a synaptic protein.

HEK 293 cells

Neuroligin

10.1111/tra.12930

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Leishmanicidal Activities of Novel Synthetic Furoxan and Benzofuroxan Derivatives

Antimicrobial Agents and Chemotherapy (2014)

Luiz Antônio Dutra Letícia de Almeida Thaís G. Passalacqua Juliana Santana Reis Fábio Aurélio Esteves Torres

ABSTRACT A novel series of furoxan (1,2,5-oxadiazole 2-oxide) (compounds 3, 4a and -b, 13a and -b, and 14a to -f) and benzofuroxan (benzo[c][1,2,5]oxadiazole 1-oxide) (compounds 7 and 8a to -c) derivatives were synthesized, characterized, and evaluated for in vitro activity against promastigote and intracellular amastigote forms of Leishmania amazonensis . The furoxan derivatives exhibited the ability to generate nitric oxide at different levels (7.8% to 27.4%). The benzofuroxan derivative 8a was able to increase nitrite production in medium supernatant from murine macrophages infected with L. amazonensis at 0.75 mM after 48 h. Furoxan and benzofuroxan derivatives showed remarkable leishmanicidal activity against both promastigote and intracellular amastigote forms. Compounds 8a, 14a and -b, and 14d exerted selective leishmanicidal activities superior to those of amphotericin B and pentamidine. In vitro studies at pH 5.4 reveal that compound 8a is stable until 8 h and that compound 14a behaves as a prodrug, releasing the active aldehyde 13a. These compounds have emerged as promising novel drug candidates for the treatment of leishmaniasis.

Furoxan

Amastigote

10.1128/aac.00052-14

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Citations (47)

Time-resolved X-ray solution scattering unveils the events leading to hemoglobin heme capture by staphylococcal IsdB

Nature Communications (2025)

Omar De Bei Marialaura Marchetti Stefano Guglielmo Eleonora Gianquinto Francesca Spyrakis

Luminescent Measurements

10.1038/s41467-024-54949-w

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ChemInform Abstract: Synthesis and in vitro Antimicrobial Activities of New (Cyano‐NNO‐azoxy) Pyrazole Derivatives.

ChemInform (2011)

Donatella Boschi Stefano Guglielmo Stefania Aiello Giulia Morace Elisa Borghi

Abstract Treatment of nitroso derivatives (I) with a mixture of cyanamide (II) and (diacetoxy)iodobenzene yields the azoxycyano derivatives (III), probably through the intermediate formation of cyanonitrene.

Azoxy

Pyrazole

10.1002/chin.201144110

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Time-resolved X-ray solution scattering unveils the sequence of events leading to human Hb heme capture byStaphylococcus aureusIsdB

bioRxiv (Cold Spring Harbor Laboratory) (2023)

Omar De Bei Marialaura Marchetti Stefano Guglielmo Eleonora Gianquinto Francesca Spyrakis

Abstract Infections caused by Staphylococcus aureus depend on its ability to acquire nutrients. One essential nutrient is iron, which is obtained from the heme of the human host hemoglobin (Hb) through a protein machinery called Iron-regulated Surface Determinant (Isd). IsdB is the protein in charge of heme extraction from Hb, which is the first step of the chain of events leading to iron transfer to the bacterium cell interior. In order to elucidate the molecular events leading from the formation of the initial IsdB:Hb complex to heme extraction, we have performed a time-resolved X-ray solution scattering (TR-XSS) investigation combined with a rapid mixing triggering approach. We succeeded in defining the stoichiometry of IsdB:Hb binding and in describing the kinetics of the subsequent structural changes. The presented approach is potentially applicable to unveil the complex kinetic pathways generated by protein-protein interaction in different biological systems.

10.1101/2023.08.04.551941

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