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Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth.
Costantino L, Ferrari S, Santucci M, Salo-Ahen OMH, Carosati E, Franchini S, Lauriola A, Pozzi C, Trande M, Gozzi G, Saxena P, Cannazza G, Losi L, Cardinale D, Venturelli A, Quotadamo A, Linciano P, Tagliazucchi L, Moschella MG, Guerrini R, Pacifico S, Luciani R, Genovese F, Henrich S, Alboni S, Santarem N, da Silva Cordeiro A, Giovannetti E, Peters GJ, Pinton P, Rimessi A, Cruciani G, Stroud RM, Wade RC, Mangani S, Marverti G, D'Arca D, Ponterini G, Costi MP. Costantino L, et al. Among authors: linciano p. Elife. 2022 Dec 7;11:e73862. doi: 10.7554/eLife.73862. Elife. 2022. PMID: 36475542 Free PMC article.
Fibrate-derived N-(methylsulfonyl)amides with antagonistic properties on PPARα.
Ammazzalorso A, D'Angelo A, Giancristofaro A, De Filippis B, Di Matteo M, Fantacuzzi M, Giampietro L, Linciano P, Maccallini C, Amoroso R. Ammazzalorso A, et al. Among authors: linciano p. Eur J Med Chem. 2012 Dec;58:317-22. doi: 10.1016/j.ejmech.2012.10.019. Epub 2012 Oct 23. Eur J Med Chem. 2012. PMID: 23137448
Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs.
Giampietro L, D'Angelo A, Giancristofaro A, Ammazzalorso A, De Filippis B, Fantacuzzi M, Linciano P, Maccallini C, Amoroso R. Giampietro L, et al. Among authors: linciano p. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7662-6. doi: 10.1016/j.bmcl.2012.09.111. Epub 2012 Oct 6. Bioorg Med Chem Lett. 2012. PMID: 23102891
Exploiting the 2-Amino-1,3,4-thiadiazole Scaffold To Inhibit Trypanosoma brucei Pteridine Reductase in Support of Early-Stage Drug Discovery.
Linciano P, Dawson A, Pöhner I, Costa DM, Sá MS, Cordeiro-da-Silva A, Luciani R, Gul S, Witt G, Ellinger B, Kuzikov M, Gribbon P, Reinshagen J, Wolf M, Behrens B, Hannaert V, Michels PAM, Nerini E, Pozzi C, di Pisa F, Landi G, Santarem N, Ferrari S, Saxena P, Lazzari S, Cannazza G, Freitas-Junior LH, Moraes CB, Pascoalino BS, Alcântara LM, Bertolacini CP, Fontana V, Wittig U, Müller W, Wade RC, Hunter WN, Mangani S, Costantino L, Costi MP. Linciano P, et al. ACS Omega. 2017 Sep 30;2(9):5666-5683. doi: 10.1021/acsomega.7b00473. Epub 2017 Sep 11. ACS Omega. 2017. PMID: 28983525 Free PMC article.
Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
Linciano P, Moraes CB, Alcantara LM, Franco CH, Pascoalino B, Freitas-Junior LH, Macedo S, Santarem N, Cordeiro-da-Silva A, Gul S, Witt G, Kuzikov M, Ellinger B, Ferrari S, Luciani R, Quotadamo A, Costantino L, Costi MP. Linciano P, et al. Eur J Med Chem. 2018 Feb 25;146:423-434. doi: 10.1016/j.ejmech.2018.01.043. Epub 2018 Jan 31. Eur J Med Chem. 2018. PMID: 29407968
Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform.
Moraes CB, Witt G, Kuzikov M, Ellinger B, Calogeropoulou T, Prousis KC, Mangani S, Di Pisa F, Landi G, Iacono LD, Pozzi C, Freitas-Junior LH, Dos Santos Pascoalino B, Bertolacini CP, Behrens B, Keminer O, Leu J, Wolf M, Reinshagen J, Cordeiro-da-Silva A, Santarem N, Venturelli A, Wrigley S, Karunakaran D, Kebede B, Pöhner I, Müller W, Panecka-Hofman J, Wade RC, Fenske M, Clos J, Alunda JM, Corral MJ, Uliassi E, Bolognesi ML, Linciano P, Quotadamo A, Ferrari S, Santucci M, Borsari C, Costi MP, Gul S. Moraes CB, et al. Among authors: linciano p. SLAS Discov. 2019 Mar;24(3):346-361. doi: 10.1177/2472555218823171. SLAS Discov. 2019. PMID: 30784368 Free PMC article.
69 results