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SynBioMed (SBM)

SynBioMed (SBM)

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Settore ERC

PE5_18 - Medicinal chemistry

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The main lines of SynBioMed research unit are:

  • Design, synthesis and biological evaluation of new chemical entities modulating NLRP3 inflammasome activity. (Target Pathologies: IBD, AD, PD, MS, CAPS)
  • Design, synthesis and ex vivo evaluation of dual TP-antagonists COX-2 inhibitors. (Chronic inflammatory diseases: arthritis, RA, AD, colon cancer, atherosclerosis)
  • Design and synthesis of protein degraders (PROTACs) for anticancer therapy. (Colon cancer, melanoma)
  • Design and synthesis of fluorescent probes for fluorescence guided surgery. (Application in different type of cancers: prostate cancer, breast cancer)

A_SynBioMed

  • Drug design, Drug synthesis, Heterocyclic chemistry, Inflammasome, PROTAC, Thromboxane, Cyclooxigenases.

  • Institute of Pharmaceutical Chemistry, Goethe-University, Frankfurt am Main (Germany)
  • BioMedical Research Institute of Murcia (IMIB-Arrixaca), University of Murcia, Murcia (Spain)
  • Centro de Investigação em Ciências da Saúd – University of Beira Interior (CICS-UBI), Beira Interior (Portugal)
  • Bracco Imaging spa – Global Research and Development (Italy)
  • Department of Clinical and Experimental Medicine, University of Pisa (Italy)
  • Department of Pharmaceutical Sciences, University of Milan (Italy)
  • Center for Advanced Studies and Technology (CAST), "G. d'Annunzio" University, Chieti (Italy)
  • Department of Biology, E. and E.S., University of Calabria (Italy)

Prodotti della ricerca

  • Marini E, Marino M, Gionfriddo G, Maione F, Pandini M, Oddo D, Giorgis M, Rolando B, Blua F, Gastaldi S, Marchio S, Kovachka S, Spyrakis F, Gianquinto E, Di Nicolantonio F, Bertinaria M. (2022) Investigation into the Use of Encorafenib to Develop Potential PROTACs Directed against BRAF(V600E) Protein. Molecules (Basel, Switzerland) 27(23) [DOI  PMID]
  • Marini E, Giorgis M, Leporati M, Rolando B, Chegaev K, Lazzarato L, Bertinaria M, Vincenti M, Di Stilo A. (2022) Multitarget Antioxidant NO-Donor Organic Nitrates: A Novel Approach to Overcome Nitrates Tolerance, an Ex Vivo Study. Antioxidants (Basel, Switzerland) 11(1) [DOI  PMID]
  • Gastaldi S, Boscaro V, Gianquinto E, Sandall CF, Giorgis M, Marini E, Blua F, Gallicchio M, Spyrakis F, MacDonald JA, Bertinaria M. (2021) Chemical Modulation of the 1-(Piperidin-4-yl)-1,3-dihydro-2H-benzo[d]imidazole-2-one Scaffold as a Novel NLRP3 Inhibitor. Molecules (Basel, Switzerland) 26(13) [DOI  PMID]
  • Penna C, Aragno M, Cento AS, Femmino S, Russo I, Bello FD, Chiazza F, Collotta D, Alves GF, Bertinaria M, Zicola E, Mercurio V, Medana C, Collino M, Pagliaro P. (2020) Ticagrelor Conditioning Effects Are Not Additive to Cardioprotection Induced by Direct NLRP3 Inflammasome Inhibition: Role of RISK, NLRP3, and Redox Cascades. Oxidative medicine and cellular longevity 2020 9219825 [DOI  PMID]
  • Pellegrini C, Fornai M, Colucci R, Benvenuti L, D'Antongiovanni V, Natale G, Fulceri F, Giorgis M, Marini E, Gastaldi S, Bertinaria M, Blandizzi C, Antonioli L. (2018) A Comparative Study on the Efficacy of NLRP3 Inflammasome Signaling Inhibitors in a Pre-clinical Model of Bowel Inflammation. Frontiers in pharmacology 9 1405 [DOI  PMID]
  • Bertinaria M, Gastaldi S, Marini E, Giorgis M. (2019) Development of covalent NLRP3 inflammasome inhibitors: Chemistry and biological activity. Archives of biochemistry and biophysics 670 116-139 [DOI  PMID]
  • Atlante S, Visintin A, Marini E, Savoia M, Dianzani C, Giorgis M, Surun D, Maione F, Schnutgen F, Farsetti A, Zeiher AM, Bertinaria M, Giraudo E, Spallotta F, Cencioni C, Gaetano C. (2018) alpha-ketoglutarate dehydrogenase inhibition counteracts breast cancer-associated lung metastasis. Cell death & disease 9(7) 756 [DOI  PMID]
  • Spallotta F, Cencioni C, Atlante S, Garella D, Cocco M, Mori M, Mastrocola R, Kuenne C, Guenther S, Nanni S, Azzimato V, Zukunft S, Kornberger A, Surun D, Schnutgen F, von Melchner H, Di Stilo A, Aragno M, Braspenning M, van Criekinge W, De Blasio MJ, Ritchie RH, Zaccagnini G, Martelli F, Farsetti A, Fleming I, Braun T, Beiras-Fernandez A, Botta B, Collino M, Bertinaria M, Zeiher AM, Gaetano C. (2018) Stable Oxidative Cytosine Modifications Accumulate in Cardiac Mesenchymal Cells From Type2 Diabetes Patients: Rescue by alpha-Ketoglutarate and TET-TDG Functional Reactivation. Circulation research 122(1) 31-46 [DOI  PMID]
  • Carnevali S, Buccellati C, Bolego C, Bertinaria M, Rovati GE, Sala A. (2017) Nonsteroidal Anti-Inflammatory Drugs: Exploiting Bivalent COXIB/ TP Antagonists for the Control of Cardiovascular Risk. Current medicinal chemistry 24(30) 3218-3230 [DOI  PMID]
  • Cocco M, Pellegrini C, Martinez-Banaclocha H, Giorgis M, Marini E, Costale A, Miglio G, Fornai M, Antonioli L, Lopez-Castejon G, Tapia-Abellan A, Angosto D, Hafner-Bratkovic I, Regazzoni L, Blandizzi C, Pelegrin P, Bertinaria M. (2017) Development of an Acrylate Derivative Targeting the NLRP3 Inflammasome for the Treatment of Inflammatory Bowel Disease. Journal of medicinal chemistry 60(9) 3656-3671 [DOI  PMID]
  • Mastrocola R, Penna C, Tullio F, Femmino S, Nigro D, Chiazza F, Serpe L, Collotta D, Alloatti G, Cocco M, Bertinaria M, Pagliaro P, Aragno M, Collino M. (2016) Pharmacological Inhibition of NLRP3 Inflammasome Attenuates Myocardial Ischemia/Reperfusion Injury by Activation of RISK and Mitochondrial Pathways. Oxidative medicine and cellular longevity 2016 5271251 [DOI  PMID]
  • Garella D, Atlante S, Borretto E, Cocco M, Giorgis M, Costale A, Stevanato L, Miglio G, Cencioni C, Fernandez-de Gortari E, Medina-Franco JL, Spallotta F, Gaetano C, Bertinaria M. (2016) Design and synthesis of N-benzoyl amino acid derivatives as DNA methylation inhibitors. Chemical biology & drug design 88(5) 664-676 [DOI  PMID]
  • Cocco M, Miglio G, Giorgis M, Garella D, Marini E, Costale A, Regazzoni L, Vistoli G, Orioli M, Massulaha-Ahmed R, Detraz-Durieux I, Groslambert M, Py BF, Bertinaria M. (2016) Design, Synthesis, and Evaluation of Acrylamide Derivatives as Direct NLRP3 Inflammasome Inhibitors. ChemMedChem 11(16) 1790-803 [DOI  PMID]
  • Marini E, Rolando B, Sodano F, Blua F, Concina G, Guglielmo S, Lazzarato L, Chegaev K. (2023) Comparative Study of Different H(2)S Donors as Vasodilators and Attenuators of Superoxide-Induced Endothelial Damage. Antioxidants (Basel, Switzerland) 12(2) [DOI  PMID]
  • Sodano F, Cristiano C, Rolando B, Marini E, Lazzarato L, Cuozzo M, Albrizio S, Russo R, Rimoli MG. (2022) Galactosylated Prodrugs: A Strategy to Improve the Profile of Nonsteroidal Anti-Inflammatory Drugs. Pharmaceuticals (Basel, Switzerland) 15(5) [DOI  PMID]
  • Sodano F, Gazzano E, Rolando B, Marini E, Lazzarato L, Fruttero R, Riganti C, Gasco A. (2021) Tuning NO release of organelle-targeted furoxan derivatives and their cytotoxicity against lung cancer cells. Bioorganic chemistry 111 104911 [DOI  PMID]
Ultimo aggiornamento: 31/03/2023 11:11
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