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Patents & Publications

Patents Mercurio

  1. Pasqualato, Sebastiano; Pasi, Maurizio; Amici, Raffaella; Varasi, Mario; Mercurio, Ciro; Sartori, Luca; Polo, Simona; Maspero, Elena; Faga`, Giovanni
    Hect e3 ligase inhibitors and uses thereof
    PCT Int. Appl. (2020), WO 2020245213 A1 20201210

  2. Varasi, Mario; Cappa, Anna; Vianello, Paola; Moretti, Loris; Sartori, Luca; Mercurio, Ciro
    Thieno[2,?3-?b]?pyrrole and thieno[3,?2-?b]?pyrrole derivatives as histone demethylase inhibitors and their preparation
    PCT Int. Appl. (2019), WO 2019034774 A1 20190221

  3. Varasi, Mario; Villa, Manuela; Trifiró, Paolo; Fancelli, Daniele; Mercurio, Ciro; Vianello, Paola; Sartori, Luca
    Oxime derivatives useful as inhibitors of histone demethylase KDM4C and their preparation
    PCT Int. Appl. (2017), WO 2017198785 A1 20171123.

  4. Vianello, Paola; Romussi, Alessia; Cappa, Anna; Trifiró, Paolo; Varasi, Mario; Sartori, Luca; Mercurio, Ciro
    Preparation of imidazol-2-ylthienopyrrole compounds as histone demethylase inhibitors
    PCT Int. Appl. (2017), WO 2017198780 A1 20171123.

  5. Vianello, Paola; Sartori, Luca;Varasi, Mario; Mercurio, Ciro; Zagarri, Elisa; Cappa, Anna; Romussi, Alessia; Villa, Manuela; Meroni, Giuseppe; Moretti, Loris
    Thienopyrroles as histone demethylase inhibitors
    PCT Int. Appl. (2016), WO2016034946 A2 20160310

  6. Vianello, Paola; Varasi, Mario; Mercurio, Ciro; Cappa, Anna; Meroni, Giuseppe Villa, Manuela; Mai, Antonello; Valente, Sergio
    Cyclopropylamine compounds as histone demethylase inhibitors
    PCT Int. Appl. (2015), WO 2015181380 A1 20151203.

  7. Varasi, Mario; Vianello, Paola; Thaler, Florian; Trifiro, Paolo; Mercurio, Ciro; Meroni, Giuseppe
    Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
    PCT Int. Appl. (2014), WO 2014086790 A1 20140612.

  8. Amici, Raffaella; Colombo, Andrea; Courtney, Stephen Martin; Mercurio, Ciro; Montalbetti, Christian Aldo Georges Napoleon; Mortoni, Annalisa; Varasi, Mario
    Preparation of quinazoline derivatives with Hsp90 inhibitory activity for therapy
    PCT Int. Appl. (2013), WO 2013064919 A1 20130510.

  9. Varasi, Mario; Thaler, Florian; Amici, Raffaella; Abate, Agnese; Fulco, Maria Carmela; Minucci, Saverio; Mercurio, Ciro.
    Spirocyclic derivatives as histone deacetylase inhibitors U.S.
    Pat. Appl. Publ. (2012), US 20120258949 A1 20121011

  10. Minucci, Saverio; Pelicci, Pier Giuseppe; Mai, Antonello; Ballarini, Marco; Gargiulo, Gaetano; Massa, Silvio; Thaler, Florian; Pain, Gilles; Colombo, Andrea; Gagliardi, Stefania; Varasi, Mario; Ciro, Mercurio
    Preparation of N-hydroxy piperazinyl-phenyl-oxo-propenyl-phenyl-acrylamides and related compounds as histone deacetylase inhibitors U.S.
    Pat. Appl. Publ. (2012), US 20120115867 A1 20120510

  11. Varasi, Mario; Thaler, Florian; Amici, Raffaella; Abate, Agnese; Fulco, Maria Carmela; Minucci, Saverio; Mercurio, Ciro.
    Preparation of oxospirochromane derivatives as histone deacetylase inhibitors.
    PCT Int. Appl. (2011), WO 2011045265 A2 20110421

  12. Thaler, Florian; Varasi, Mario; Gagliardi, Stefania; Colombo, Andrea; Minucci, Saverio; Mercurio, Ciro.
    Heterocyclic derivatives as HDAC inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases.
    PCT Int. Appl. (2009), 98pp. WO 2009150129 A1 20091217

  13. Thaler, Florian; Varasi, Mario; Mercurio, Ciro; Minucci, Saverio; Colombo, Andrea; Gagliardi, Stefania.
    Preparation of N-hydroxy piperazinylphenyloxopropenylphenylacrylamides and related compounds as histone deacetylase inhibitors.
    PCT Int. Appl. (2009), WO 2009027395 A1 20090305

  14. Mercurio Ciro., Pesenti Enrico. ,Porro MariaGraziaPevarello? Paolo.
    COMBINATIONS COMPRISING A CDK INHIBITOR AND A GROWTH FACTOR ANTIBODY OR ANTI-MITOTIC
    PCT/EP2007/051020. WO/2007/090794


    15.  

Publications

  1. Faletti S, Osti D, Ceccacci E, Richichi C, Costanza B, Nicosia L, Noberini R, Marotta G, Furia L, Faretta MR, Brambillasca S, Quarto M, Bertero L, Boldorini R, Pollo B, Gandini S, Cora D, Minucci S, Mercurio C, Varasi M, Bonaldi T, Pelicci G.
    LSD1-directed therapy affects glioblastoma tumorigenicity by deregulating the protective ATF4-dependent integrated stress response
    Sci Transl Med. 2021 Dec 8;13(623):eabf7036

  2. Zwergel C, Di Bello E, Fioravanti R, Conte M, Nebbioso A, Mazzone R, Brosch G, Mercurio C, Varasi M, Altucci L, Valente S, Mai A.
    Novel Pyridine-Based Hydroxamates and 2'-Aminoanilides as Histone Deacetylase Inhibitors: Biochemical Profile and Anticancer Activity
    ChemMedChem?. 2021 Mar 18;16(6):989-999

  3. Cavallo F, Troglio F, Fagà G, Fancelli D, Shyti R, Trattaro S, Zanella M, D'Agostino G, Hughes JM, Cera MR, Pasi M, Gabriele M, Lazzarin M, Mihailovich M, Kooy F, Rosa A, Mercurio C, Varasi M, Testa G.
    High-throughput screening identifies histone deacetylase inhibitors that modulate GTF2I expression in 7q11.23 microduplication autism spectrum disorder patient-derived cortical neurons.
    Molecular Autism (2020), 11(1), 88

  4. Romussi A, Cappa A, Vianello P, Brambillasca S, Cera MR, Dal Zuffo R, Fagà G, Fattori R, Moretti L, Trifirò P, Villa M, Vultaggio S, Cecatiello V, Pasqualato S, Dondio G, So CWE, Minucci S, Sartori L, Varasi M, Mercurio C
    Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models
    ACS Med Chem Lett. 2020 Feb 13;11(5):754-759

  5. Ravasio R, Ceccacci E, Nicosia L, Hosseini A, Rossi PL, Barozzi I, Fornasari L, Zuffo RD, Valente S, Fioravanti R, Mercurio C, Varasi M, Mattevi A, Mai A, Pavesi G, Bonaldi T, Minucci S.
    Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoic acid-induced differentiation
    Sci Adv. 2020 Apr 8;6(15)

  6. Mercurio C And Varasi M.
    New targets to modulate the DNA damage response.
    Future Med Chem. 2018 Oct;10(20):2377-2380

  7. La Regina G, Bai R, Coluccia A, Naccarato V, Famiglini V, Nalli M, Masci D, Verrico A, Rovella P, Mazzoccoli C, Da Pozzo E, Cavallini C, Martini C, Vultaggio S, Dondio G, Varasi M, Mercurio C, Hamel E, Lavia P, Silvestri R.
    New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.
    Eur J Med Chem. 2018 May 25; 152:283-297

  8. Trifirò P, Cappa A, Brambillasca S, Botrugno OA, Cera MR, Zuffo RD, Dessanti P, Meroni G, Thaler F, Villa M, Minucci S, Mercurio C, Varasi M, Vianello P.
    Novel potent inhibitors of the histone demethylase KDM1A (LSD1), orally active in a murine promyelocitic leukemia model.
    Future Med Chem. 2017 Jul;9(11):1161-1174

  9. La Regina G, Bai R, Coluccia A, Famiglini V, Passacantilli S, Naccarato V, Ortar G, Mazzoccoli C, Ruggieri V, Agriesti F, Piccoli C, Tataranni T, Nalli M, Brancale A, Vultaggio S, Mercurio C, Varasi M, Saponaro C, Sergio S, Maffia M, Coluccia AML, Hamel E, Silvestri R.
    3-Aroyl-1,4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction Tubulin.
    ACS Med Chem Lett. 2017 Apr 26;8(5):521-526.

  10. Vianello P, Sartori L, Amigoni F, Cappa A, Fagá G, Fattori R, Legnaghi E, Ciossani G, Mattevi A, Meroni G, Moretti L, Cecatiello V, Pasqualato S, Romussi A, Thaler F, Trifiró P, Villa M, Botrugno OA, Dessanti P, Minucci S, Vultaggio S, Zagarrí E, Varasi M, Mercurio C.
    Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure-Activity Relationship.
    J Med Chem. 2017 Mar 9;60(5):1693-1715.

  11. Sartori L, Mercurio C, Amigoni F, Cappa A, Fagá G, Fattori R, Legnaghi E, Ciossani G, Mattevi A, Meroni G, Moretti L, Cecatiello V, Pasqualato S, Romussi A, Thaler F, Trifiró P, Villa M, Vultaggio S, Botrugno OA, Dessanti P, Minucci S, Zagarrí E, Carettoni D, Iuzzolino L, Varasi M, Vianello P.
    Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration.
    J Med Chem. 2017 Mar 9;60(5):1673-1692

  12. Elgendy M, Abdel-Aziz AK, Renne SL, Bornaghi V, Procopio G, Colecchia M, Kanesvaran R, Toh CK, Bossi D, Pallavicini I, Perez-Gracia JL, Lozano MD, Giandomenico V, Mercurio C, Lanfrancone L, Fazio N, Nole F, Teh BT, Renne G, Minucci S.
    Dual modulation of MCL-1 and mTOR determines the response to sunitinib.
    J Clin Invest. 2017 Jan 3;127(1):153-168

  13. Thaler F, Mercurio C.
    Compounds and methods for inhibiting histone demethylases: a patent evaluation of US20160102096A1.
    Expert Opin Ther Pat. 2016 Dec;26(12):1367-1370

  14. Vianello P, Botrugno OA, Cappa A, Dal Zuffo R, Dessanti P, Mai A, Marrocco B, Mattevi A, Meroni G, Minucci S, Stazi G, Thaler F, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C.
    Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent.
    J Med Chem. 2016 Feb 25;59(4):1501-17.

  15. Thaler F, Moretti L, Amici R, Abate A, Colombo A, Carenzi G, Fulco MC, Boggio R, Dondio G, Gagliardi S, Minucci S, Sartori L, Varasi M, Mercurio C.
    Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
    Eur J Med Chem. 2016 Jan 27;108:53-67

  16. La Regina G, Bai R, Coluccia A, Famiglini V, Pelliccia S, Passacantilli S, Mazzoccoli C, Ruggieri V, Verrico A, Miele A, Monti L, Nalli M, Alfonsi R, Di Marcotullio L, Gulino A, Ricci B, Soriani A, Santoni A, Caraglia M, Porto S, Da Pozzo E, Martini C, Brancale A, Marinelli L, Novellino E, Vultaggio S, Varasi M, Mercurio C, Bigogno C, Dondio GM, Hamel E, Lavia P, Silvestri R.
    New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity and Repression of Hedgehog-dependent Cancer.
    J Med Chem. 2015 Aug 13;58(15):5789-807

  17. Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Monaldi D, Ruoppolo G, Tilset M, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A.
    Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts.
    Eur J Med Chem. 2015 Apr 13;94:163-74

  18. Valente S., Rodriguez V., Mercurio C., Vianello P., Saponara B., Cirilli R., Ciossani G., abella D., Marrocco B., Ruoppolo G., Botrugno O.A., Dessanti P., Minucci S., Mattevi A., Varasi M., and Mai A.
    Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.
    ACS Med Chem Lett. 2014 Dec 8;6(2):173-7.

  19. Rodriguez V., Valente S., Rovida S., Rotili D., Stazi G., Lucidi A., Ciossani G., Mattevi A., Botrugno O.A., Dessanti P., Mercurio C., Vianello P., Minucci S., Varasi M. and Mai A. Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells Med. Chem. Commun., 2015, 2015, 6, 665-670
  20. Pieroni M, Annunziato G., Azzali E.a, Dessanti P., Mercurio C., Meroni G., Trifirò P., Vianello P., Villa M., Beato C., Varasi M., Costantino G.
    Further insights into the SAR of a-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A
    Eur. J. Med Chem. 92 (2015) 377e386

  21. Elgendy M., Ciró M., Amal Kamal Abdel-Aziz, Belmonte G., Dal Zuffo R., Mercurio C., Miracco C., Lanfrancone L., Foiani M., and Minucci S.
    Beclin 1 restrains tumorigenesis through Mcl-1 destabilization in an autophagy-independent, reciprocal manner.
    Nature Communication. 2014 Dec 4; 5:5637.

  22. Vianello P, Botrugno OA, Cappa A, Ciossani G, Dessanti P, Mai A, Mattevi A, Meroni G, Minucci S, Thaler F, Tortorici M, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C.
    Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.
    Eur. J Med Chem. 2014 Oct 30; 86:352-63.

  23. La Regina G, Bai R, Coluccia A, Famiglini V, Pelliccia S, Passacantilli S, Mazzoccoli C, Ruggieri V, Sisinni L, Bolognesi A, Rensen WM, Miele A, Nalli M, Alfonsi R, Di Marcotullio L, Gulino A, Brancale A, Novellino E, Dondio G, Vultaggio S, Varasi M, Mercurio C, Hamel E, Lavia P, Silvestri R
    New Pyrrole Derivatives with Potent Tubulin Polymerization Inhibiting Activity As Anticancer Agents Including Hedgehog-Dependent Cancer.
    J Med Chem. 2014 Aug 14;57(15):6531-52.

  24. Amici R., Bigogno C., Boggio R., Colombo A., M. Courtney S., Dal Zuffo R., Dondio G., Fusar F., Gagliardi S., Minucci S., Molteni M., Montalbetti C., Mortoni A., Varasi M., Vultaggio S.,and Mercurio C.
    The Chiral Resolution and Pharmacological Characterization of the Enantiomers of the Hsp90 Inhibitor 2-Amino-7-[4-fluoro-2-(3-pyridyl) phenyl]-4-methyl-7,8-dihydro-6h-quinazolin-5-one oxime"
    ChemMedChem?.2014 Jul;9(7):1574-85.

  25. Thaler F. and Mercurio C.
    Towards Selective Inhibition of Histone Deacetylase Isoforms: What has been Achieved, Where We Are and What Will be Next
    ChemMedChem?. 2014 March; 9(3):523-536

  26. Guandalini L, Balliu M, Cellai C, Martino MV, Nebbioso A, Mercurio C, Carafa V, Bartolucci G, Dei S, Manetti D, Teodori E, Scapecchi S, Altucci L, Paoletti F, Romanelli MN.
    Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
    Eur. J. Med Chem. 2013 Aug; 66:56-68

  27. Thaler F, Varasi M, Abate A, Carenzi G, Colombo A, Bigogno C, Boggio R, Zuffo RD, Rapetti D, Resconi A, Regalia N, Vultaggio S,Dondio G,Gagliardi S,Minucci S, Mercurio C.
    Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
    Eur. J. Med Chem. 2013 Apr 10;64C:273-284.

  28. Valente S, Trisciuoglio D, Tardugno M, Benedetti R, Labella D, Secci D, Mercurio C, Boggio R, Tomassi S, Di Maro S, Novellino E, Altucci L, Del Bufalo D, Mai A, Cosconati S.
    tert-Butylcarbamate-Containing Histone Deacetylase Inhibitors: Apoptosis Induction, Cytodifferentiation, and Antiproliferative Activities in Cancer Cells.
    ChemMedChem?. 2013 May; 8(5):800-11.

  29. Albanese C, Alzani R, Amboldi N, Degrassi A, Festuccia C, Fiorentini F, Gravina GL, Mercurio C, Pastori W, Brasca MG, Pesenti E, Galvani A, Ciomei M.
    Antitumor efficacy on glioma models of PHA-848125, a multikinase inhibitor able to cross the blood brain barrier.
    Br. J. Pharmacol. 2013 May;169(1):156-66.

  30. La Regina G, Bai R, Rensen WM, Di Cesare E, Coluccia A, Piscitelli F, Famiglini V, Reggio A, Nalli M, Pelliccia S, Da Pozzo E, Costa B, Granata I, Porta A, Maresca B, Soriani A, Iannitto ML, Santoni A, Li J, Miranda Cona M, Chen F, Ni Y, Brancale A, Dondio G, Vultaggio S, Varasi M, Mercurio C, Martini C, Hamel E, Lavia P, Novellino E, Silvestri R.
    Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
    J Med Chem. 2013 Jan 10;56(1):123-49.

  31. Thaler F, Varasi M, Carenzi G, Colombo A, Abate A, Bigogno C, Boggio R, Carrara S, Cataudella T, Dal Zuffo R, Reali V, Vultaggio S, Dondio G, Gagliardi S, Minucci S, Mercurio C.
    Spiro[chromane-2,4'-piperidine]-based histone deacetylase inhibitors with improved in vivo activity.
    ChemMedChem?. 2012 Apr; 7(4):709-21

  32. Leiva M, Moretti S, Soilihi H, Pallavicini I, Peres L, Mercurio C, Dal Zuffo R, Minucci S, de Thé H.
    Valproic acid induces differentiation and transient tumor regression, but spares leukemia-initiating activity in mouse models of APL.
    Leukemia. 2012 Jul; 26(7):1630-7

  33. La Regina G, BaiR?,Rensen W,Coluccia A,Piscitielli F,Gatti V,Bolognesi A,Lavecchia A,Granata I,Porta A,Maresca b, Soriani A, Iannitto ML,Mariani M,Santoni A,Brancale A,Ferlini C,Dondio G,Varasi M, Mercurio C,Hamel E,Lavia P,Novellino E,Silvestri R.
    Design and Synthesis of 2-Heterocyclyl-3-arylthio-1H-indoles as Potent Tubulin Polymerization and Cell Growth Inhibitors with Improved Metabolic Stability.
    J.Med Chem. 2011 Dec 22; 54(24):8394-406

  34. Varasi M, Thaler F, Abate A, Bigogno C, Boggio R, Carenzi G, Cataudella T, Dal Zuffo R, Fulco MC, Rozio MG, Mai A, Dondio G, Minucci S, Mercurio C
    Discovery, Synthesis, and Pharmacological Evaluation of Spiropiperidine-Hydroxamic Acid Based Derivatives as Structurally Novel Histone Deacetylase (HDAC) Inhibitors.
    J.Med Chem. 2011 Apr 28; 54(8):3051-64

  35. Di Micco R, Sulli G, Dobreva M, Liontos M, Botrugno OA, Gargiulo G, Dal Zuffo R, Matti V, d'Ario G, Montani E,Mercurio C,Hahn WC,Gorgoulis V, Minucci S,d'Adda di Fagagna F.
    Interplay between oncogene-induced DNA damage response and heterochromatin in senescence and cancer.
    Nat Cell Biol. 2011 Mar; 13(3):292-302.

  36. Fanelli M, Amatori S, Barozzi I, Soncini M, Dal Zuffo R, Bucci G, Capra M, Quarto M, Dellino GI, Mercurio C, Alcalay M, Viale G, Pelicci PG, Minucci S
    Pathology tissue-chromatin immunoprecipitation, coupled with high-throughput sequencing, allows the epigenetic profiling of patient samples.
    Proc Natl Acad Sci U S A. 2010 Dec 14; 107(50):21535-40

  37. Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M.
    Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy.
    Mol. Cancer Ther. 2010 Aug; 9(8):2243-54

  38. Conti P, Tamborini L, Pinto A, Sola L, Ettari R, Mercurio C, De Micheli C
    Design and synthesis of novel isoxazole-based HDAC inhibitors.
    Eur J Med Chem. 2010 Sep; 45(9):4331-8

  39. Thaler F, Varasi M, Colombo A, Boggio R, Munari D, Regalia N, Rozio MG, Reali V, Resconi AE, Mai A, Gagliardi S, Dondio G, Minucci S, Mercurio C.
    Synthesis and biological characterization of amidopropenyl hydroxamates as HDAC inhibitors.
    ChemMedChem?. 2010 Aug 2; 5(8):1359-72.

  40. Locatelli G, Bosotti R, Ciomei M, Brasca MG, Calogero R, Mercurio C, Fiorentini F, Bertolotti M, Scacheri E, Scaburri A, Galvani A, Pesenti E, De Baere T, Soria JC, Lazar V, Isacchi A. Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study.
    Mol. Cancer Ther. 2010 May; 9(5):1265-73.

  41. Mercurio C, Minucci S, Pelicci PG.
    Histone deacetylases and epigenetic therapies of hematological malignancies.
    Pharmacol Res. 2010 Jul; 62(1):18-34.

  42. Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M.
    Optimization of 6,6-dimethyl pyrrolo[3,4-c] pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
    Bioorg Med Chem. 2010 Mar 1; 18(5):1844-53

  43. Traquandi G, Ciomei M, Ballinari D, Casale E, Colombo N, Croci V, Fiorentini F, Isacchi A, Longo A, Mercurio C, Panzeri A, Pastori W, Pevarello P, Volpi D, Roussel P, Vulpetti A, Brasca MG.
    Identification of Potent Pyrazolo[4,3-h] quinazoline-3-carboxamides as Multi-Cyclin-Dependent Kinase Inhibitors (dagger).
    J Med Chem. 2010 Mar 11;53(5):2171-87.

  44. Thaler F, Colombo A, Mai A, Amici R, Bigogno C, Boggio R, Cappa A, Carrara S, Cataudella T, Fusar F, Gianti E, di Ventimiglia SJ, Moroni M, Munari D, Pain G, Regalia N, Sartori L, Vultaggio S, Dondio G, Gagliardi S, Minucci S, Mercurio C, Varasi M.
    Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
    J Med Chem. 2010 Jan 28;53(2):822-39

  45. Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M
    Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl) phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor.
    J Med Chem. 2009 Aug 27;52(16):5152-63

  46. Barker JJ, Barker O, Boggio R, Chauhan V, Cheng RK, Corden V, Courtney SM, Edwards N, Falque VM, Fusar F, Gardiner M, Hamelin EM, Hesterkamp T, Ichihara O, Jones RS, Mather O, Mercurio C, Minucci S, Montalbetti CA, Müller A, Patel D, Phillips BG, Varasi M, Whittaker M, Winkler D, Yarnold CJ.
    Fragment-based identification of Hsp90 inhibitors.
    ChemMedChem?. 2009 Jun; 4(6):963-6

  47. Pirali T, Pagliai F, Mercurio C, Boggio R, Canonico PL, Sorba G, Tron GC, Genazzani A.
    Triazole-modified histone deacetylase inhibitors as a rapid route to drug discovery.
    J Comb Chem. 2008 Sep-Oct; 10(5):624-7.

  48. Brasca MG, Albanese C, Amici R, Ballinari D, Corti L, Croci V, Fancelli D, Fiorentini F, Nesi M, Orsini P, Orzi F, Pastori W, Perrone E, Pesenti E, Pevarello P, Riccardi-Sirtori F, Roletto F, Roussel P, Varasi M, Vulpetti A, Mercurio C.
    6-Substituted pyrrolo[3,4-c] pyrazoles: an improved class of CDK2 inhibitors.
    ChemMedChem?. 2007 Jun;2(6):841-52.

  49. Bosotti R, Locatelli G, Healy S, Scacheri E, Sartori L, Mercurio C, Calogero R, Isacchi A. Cross platform microarray analysis for robust identification of differentially expressed genes. BMC Bioinformatics. 2007 Mar 8;8 Suppl 1: S5

  50. Deans AJ, Khanna KK, McNees? CJ, Mercurio C, Heierhorst J, McArthur? GA
    Cyclin-dependent kinase 2 functions in normal DNA repair and is a therapeutic target in BRCA1-deficient cancers.
    Cancer Res. 2006 Aug 15; 66(16):8219-26.

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    -Amino-1, 4, 5, 6-tetrahydropyrrolo [3, 4-c] pyrazoles: A new class of CDK2 inhibitors
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  52. PevarelloP?,brascaMG,Orsini P.,Traquandi G,Longo A,Nesi M,Orzi F., Piutti C.,Sansonna P, Varasi M.,Cameron A.,Vulpetti A.,Roletto F.,Alzani R.,Ciomei M.,Albanese C.,Pastori W.,Marsiglio A., Pesenti E., FiorentiniF?., Bischoff JR,Mercurio C
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  53. Dominguez JE.,Munoz MC.,Zafra D.,Sanchez-perez I.,Baque S.,Caron M,Mercurio C.,Barbera A.,Perona R.,Gomiz R.,Juinovart JJ.
    The anti-diabetic agent sodium tungstate activates glycogen synthesis through an insulin receptor-independent pathway
    J Biol Chem. 2003 Oct 31; 278(44): 42785-94

  54. A. Montagnoli, R.Bosotti, F.Villa, M.Rialland, D.Brotherton, C.Mercurio, J.Berthelsen and C.Santocanale
    DRF1, a novel regulatory subunit for human Cdc7 kinase
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  55. M.Molinari, C.Mercurio (co-first authorship), J.Dominguez, F.Goubin and G.F.Draetta.
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  56. Gl.Russo, V.della Pietra, Mercurio C.,R.Palumbo,G.Iacomino,M.Russo,M.Tosto,V.Zappia.
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    Adv.exp.med.biol. 1999; 472:131-47

  57. Gl.Russo,V.della Pietra, C.Mercurio, F.della Ragione,D.R.Marshak,A.Oliva,V. Zappia.
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  61. A.Iolascon, E.Miraglia del Giudice, S. Perrotta, Gl.Russo, A.Oliva, C.Mercurio and F. della Ragione.
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    Leuk Res. 1995 Nov; 19(11):883-5


    62.  
Mario Varasi

Experimental Therapeutics Program