Discovery of a novel 1,3,4-oxadiazol-2-one-based NLRP3 inhibitor as a pharmacological agent to mitigate cardiac and metabolic complications in an experimental model of diet-induced metaflammation

Authors: Gastaldi, Simone, Rocca, Carmine, Gianquinto, Eleonora, Granieri, Maria Concetta, Boscaro, Valentina, Blua, Federica, Rolando, Barbara, Marini, Elisabetta, Gallicchio, Margherita, De Bartolo, Anna, Romeo, Naomi, Mazza, Rosa, Fedele, Francesco, Pagliaro, Pasquale, Penna, Claudia, Spyrakis, Francesca, Bertinaria, Massimo, Angelone, Tommaso

Subject Terms: Physics - Biological Physics, Physics - Medical Physics

Access URL: http://arxiv.org/abs/2309.07939

NLRP3 monomer Functional Dynamics: from the Effects of Allosteric Binding to Implications for Drug Design

Authors: Casali, Emanuele, Serapian, Stefano A., Gianquinto, Eleonora, Castelli, Matteo, Bertinaria, Massimo, Spyrakis, Francesca, Colombo, Giorgio

Source: International Journal of Biological Macromolecules 246 (2023) 125609

Subject Terms: Quantitative Biology - Biomolecules

Access URL: http://arxiv.org/abs/2309.03589

Macrophage and cardiomyocyte roles in cardioprotection: Exploiting the NLRP3 Inflammasome inhibitor INF150

Authors: Giordano, Magalì ^{a, 1}, Femminò, Saveria ^{a, 1}, Blua, Federica ^b, Boccato, Francesca ^b, Rubeo, Chiara ^a, Mantuano, Beatrice ^a, Cioffi, Francesca ^a, Comità, Stefano ^a, Brovero, Arianna ^a, Ciullo, Rosa ^a, Bertinaria, Massimo ^{b, 2}, Penna, Claudia ^{a, c, 2}, Pagliaro, Pasquale ^{a, c, 2, ⁎}

Source: In Vascular Pharmacology June 2025 159

Novel NLRP3 inhibitor INF195: Low doses provide effective protection against myocardial ischemia/reperfusion injury

Authors: Gastaldi, Simone ^{a, 1}, Giordano, Magalì ^{b, 1}, Blua, Federica ^a, Rubeo, Chiara ^b, Boscaro, Valentina ^a, Femminò, Saveria ^b, Comità, Stefano ^b, Gianquinto, Eleonora ^a, Landolfi, Vanessa ^b, Marini, Elisabetta ^a, Gallicchio, Margherita ^a, Spyrakis, Francesca ^a, Pagliaro, Pasquale ^{b, c, ⁎, 2}, Bertinaria, Massimo ^{a, b, ⁎}, Penna, Claudia ^{b, c, 2}

Source: In Vascular Pharmacology September 2024 156

Exploring flavylium-based SWIR emitters: Design, synthesis and optical characterization of dyes derivatized with polar moieties

Authors: Blua, Federica, Boccalon, Mariangela, Rolando, Barbara, Napolitano, Roberta, Arena, Francesca, Blasi, Francesco, Bertinaria, Massimo

Source: In Bioorganic Chemistry July 2024 148

Discovery of a septin-4 covalent binder with antimetastatic activity in a mouse model of melanoma

Authors: Blua, Federica, Monge, Chiara, Gastaldi, Simone, Clemente, Nausicaa, Pizzimenti, Stefania, Lazzarato, Loretta, Senetta, Rebecca, Vittorio, Serena, Gigliotti, Casimiro Luca, Boggio, Elena, Dianzani, Umberto, Vistoli, Giulio, Altomare, Alessandra Anna, Aldini, Giancarlo, Dianzani, Chiara, Marini, Elisabetta, Bertinaria, Massimo

Source: In Bioorganic Chemistry March 2024 144

Discovery of a novel 1, 3, 4-oxadiazol-2-one-based NLRP3 inhibitor as a pharmacological agent to mitigate cardiac and metabolic complications in an experimental model of diet-induced metaflammation

Authors: Gastaldi, Simone, Rocca, Carmine, Gianquinto, Eleonora, Granieri, Maria Concetta, Boscaro, Valentina, Blua, Federica, Rolando, Barbara, Marini, Elisabetta, Gallicchio, Margherita, De Bartolo, Anna, Romeo, Naomi, Mazza, Rosa, Fedele, Francesco, Pagliaro, Pasquale, Penna, Claudia, Spyrakis, Francesca, Bertinaria, Massimo, Angelone, Tommaso

Source: European journal of medicinal chemistry. 257

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100194170659.0x000001&indx=1&recIds=ETOCvdc_100194170659.0x000001

Development of covalent NLRP3 inflammasome inhibitors: Chemistry and biological activity

Authors: Bertinaria, Massimo, Gastaldi, Simone, Marini, Elisabetta, Giorgis, Marta

Source: In Archives of Biochemistry and Biophysics 30 July 2019 670:116-139

657: GUT-DIRECTED LOCALLY ACTING NLRP3 INFLAMMASOME INHIBITOR AS A SUITABLE PHARMACOLOGICAL STRATEGY TARGETING GUT-BRAIN AXIS FOR THE TREATMENT OF ALZHEIMER'S DISEASE

Authors: Pellegrini, Carolina, Colucci, Rocchina, Benvenuti, Laura, D'Antongiovanni, Vanessa, Salvo, Clelia Di, Gastaldi, Simone, Blua, Federica, Marini, Elisabetta, Rolando, Barbara, Lazzarato, Loretta, Bernardini, Nunzia, Antonioli, Luca, Bertinaria, Massimo, Fornai, Matteo

Source: Gastroenterology. 162(7):S-163-S-163

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100167623732.0x000001&indx=1&recIds=ETOCvdc_100167623732.0x000001

Novel NLRP3 inflammasome inhibitors INF150 and INF195 attenuate isoproterenol-induced hypertrophy in H9c2 rat cardiac myoblast

Authors: Giordano, Magalì, Rubeo, Chiara, Angelone, Tommaso, Gambarotta, Giovanna, Comità, Stefano, Fedele, Francesco, Bertinaria, Massimo, Pagliaro, Pasquale, Penna, Claudia

Source: In Vascular Pharmacology June 2024 155

Stable Oxidative Cytosine Modifications Accumulate in Cardiac Mesenchymal Cells From Type2 Diabetes Patients

Authors: Spallotta, Francesco, Cencioni, Chiara, Atlante, Sandra, Garella, Davide, Cocco, Mattia, Mori, Mattia, Mastrocola, Raffaella, Kuenne, Carsten, Guenther, Stefan, Nanni, Simona, Azzimato, Valerio, Zukunft, Sven, Kornberger, Angela, Sürün, Duran, Schnütgen, Frank, von Melchner, Harald, Di Stilo, Antonella, Aragno, Manuela, Braspenning, Maarten, van Criekinge, Wim, De Blasio, Miles J., Ritchie, Rebecca H., Zaccagnini, Germana, Martelli, Fabio, Farsetti, Antonella, Fleming, Ingrid, Braun, Thomas, Beiras-Fernandez, Andres, Botta, Bruno, Collino, Massimo, Bertinaria, Massimo, Zeiher, Andreas M., Gaetano, Carlo

Source: Circulation research. 122(1):31-46

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100066172979.0x000001&indx=1&recIds=ETOCvdc_100066172979.0x000001

In vitro pharmacological evaluation of multitarget agents for thromboxane prostanoid receptor antagonism and COX-2 inhibition

Authors: Hoxha, Malvina, Buccellati, Carola, Capra, Valérie, Garella, Davide, Cena, Clara, Rolando, Barbara, Fruttero, Roberta, Carnevali, Silvia, Sala, Angelo, Rovati, G.Enrico, Bertinaria, Massimo

Source: In Pharmacological Research January 2016 103:132-143

Nonsteroidal Anti-Inflammatory Drugs: Exploiting Bivalent COXIB/ TP Antagonists for the Control of Cardiovascular Risk

Authors: Carnevali, Silvia, Buccellati, Carola, Bolego, Chiara, Bertinaria, Massimo, Rovati, G. Enrico, Sala, Angelo

Source: Current medicinal chemistry. 24(30):3218-3230

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100077940055.0x000001&indx=1&recIds=ETOCvdc_100077940055.0x000001

Cardioprotective effects of novel NLRP3 inflammasome inhibitors

Authors: Comità, Stefano, Pagliaro, Pasquale, Penna, Claudia, Bertinaria, Massimo, Spyrakis, Francesca, Gastaldi, Simone, Boscaro, Valentina, Gianquinto, Eleonora

Source: Journal of molecular and cellular cardiology. 173(S):S123-S124

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100194320390.0x000001&indx=1&recIds=ETOCvdc_100194320390.0x000001

Chapter 36 - Development of selective NLRP3 inflammasome inhibitors

Authors: Bertinaria, Massimo, Gastaldi, Simone, Marini, Elisabetta

Source: In Inflammasome Biology 2023:565-582

Novel R-roscovitine NO-donor hybrid compounds as potential pro-resolution of inflammation agents

Authors: Montanaro, Gabriele, Bertinaria, Massimo, Rolando, Barbara, Fruttero, Roberta, Lucas, Christopher D., Dorward, David A., Rossi, Adriano G., Megson, Ian L., Gasco, Alberto

Source: In Bioorganic & Medicinal Chemistry 1 April 2013 21(7):2107-2116

Do P2Y12 receptor antagonism and NLRP3 inhibition exert additive cardioprotective effects against ischemia/reperfusion injury?

Authors: Zicola, Elisa, Femminò, Saveria, Chiazza, Fausto, Collotta, Debora, Collino, Massimo, Aragno, Manuela, Bertinaria, Massimo, Pagliaro, Pasquale, Penna, Claudia

Source: Vascular pharmacology. 132

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100121294085.0x000001&indx=1&recIds=ETOCvdc_100121294085.0x000001

A Rapid Screening for Cytochrome P450 Catalysis on New Chemical Entities: Cytochrome P450 BM3 and 1,2,5-Oxadiazole Derivatives

Authors: Tsotsou, Georgia E. ^*, Di Nardo, Giovanna ^*, Sadeghi, Sheila J., Fruttero, Roberta, Lazzarato, Loretta, Bertinaria, Massimo, Gilardi, Gianfranco ^**

Source: In SLAS Discovery February 2013 18(2):211-218

Carnosine analogues containing NO-donor substructures: Synthesis, physico-chemical characterization and preliminary pharmacological profile

Authors: Bertinaria, Massimo, Rolando, Barbara, Giorgis, Marta, Montanaro, Gabriele, Marini, Elisabetta, Collino, Massimo, Benetti, Elisa, Daniele, Pier Giuseppe, Fruttero, Roberta, Gasco, Alberto

Source: In European Journal of Medicinal Chemistry August 2012 54:103-112

Amodiaquine analogues containing NO-donor substructures: Synthesis and their preliminary evaluation as potential tools in the treatment of cerebral malaria

Authors: Bertinaria, Massimo, Guglielmo, Stefano, Rolando, Barbara, Giorgis, Marta, Aragno, Cristina, Fruttero, Roberta, Gasco, Alberto, Parapini, Silvia, Taramelli, Donatella, Martins, Yuri C., Carvalho, Leonardo J.M.

Source: In European Journal of Medicinal Chemistry 2011 46(5):1757-1767