Publications

Serafim RAM, Gehringer M, Borsari C. Targeted Covalent Inhibitors in Drug Discovery, Chemical Biology and Beyond. Pharmaceuticals (Basel). 2024, 17 (2) 206. doi: 10.3390/ph17020206

Jauslin WT, Schild M, Schaefer T, Borsari C, Orbegozo C, Bissegger L, Zhanybekova S, Ritz D, Schmidt A, Wymann M, Gillingham D. A high affinity pan-PI3K binding module supports selective targeted protein degradation of PI3Kα. Chem Sci. 2023, 15 (2),683-691.

DOI: 10.1039/d3sc04629j

Galbiati A, Bova S, Pacchiana R, Borsari C, Persico M, Zana A, Bruno S, Donadelli M, Fattorusso C, Conti P. Discovery of a spirocyclic 3-bromo-4,5-dihydroisoxazole covalent inhibitor of hGAPDH with antiproliferative activity against pancreatic cancer cells. Eur J Med Chem. 2023, 254, 115286.

DOI: 10.1016/j.ejmech.2023.115286.

De Pascale M, Bissegger L, Tarantelli C, Beaufils F, Prescimone A, Mohamed Seid Hedad H, Kayali O, Orbegozo C, Raguž L, Schaefer T, Hebeisen P, Bertoni F, Wymann MP, Borsari C. Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor. Eur J Med Chem. 2023, 248, 115038.

DOI: 10.1016/j.ejmech.2022.115038.

Uros Stojiljkovic U, Meyer C, Boulay P, Hebeisen P, Rageot D, Wymann MP, Borsari C. Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks. Synthesis. 2023, 55 (03), 499-509.

DOI: 10.1055/a-1915-7794.

Galbiati A, Zana A, Borsari C, Persico M, Bova S, Tkachuk O, Corfu I.A, Tamborini L, Basilico N, Fattorusso C, Bruno S, Parapini S, Conti P. Role of Stereochemistry on the Biological Activity of Nature-Inspired 3-Br-Acivicin Isomers and Derivatives. Molecules 2023, 28, 3172.

DOI:  10.3390/molecules28073172.

Ferrins L, Olson ME, Haranahalli K, Grenier-Davies MC, Boudreau MW, Matagne B, Donckele EJ, Borsari C. YMCC and YSN: An Opportunity for Scientific and Cultural Exchange.

ACS Med Chem Lett. 2023, 14, 1129-1130. DOI: 10.1021/acsmedchemlett.3c00337.

J Med Chem. 2023, 66 (17), 11591-11592. DOI: 10.1021/acs.jmedchem.3c01401.

Borsari C, Keles E, McPhail JA, Schaefer A, Sriramaratnam R, Goch W, Schaefer T, De Pascale M, Bal W, Gstaiger M, Burke JE, Wymann MP. Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα. J Am Chem Soc. 2022, 144 (14), 6326-6342.

DOI: 10.1021/jacs.1c13568.

Wymann MP, Borsari C. Two-drug trick to target the brain blocks toxicity in the body. Nature. 2022, 609 (7928), 681-683.

DOI: 10.1038/d41586-022-02892-5.

Borsari C, De Pascale M, Wymann MP. Chemical and Structural Strategies to Selectively Target mTOR Kinase. ChemMedChem. 2021, 16 (18), 2744-2759.

DOI: 10.1002/cmdc.202100332.

Borsari C, Keles E, Treyer A, De Pascale M, Hebeisen P, Hamburger M, Wymann MP. Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability. RSC Med Chem. 2021, 12 (4), 579-583.

DOI: 10.1039/d0md00408a.

Rathinaswamy MK, Gaieb Z, Fleming KD, Borsari C, Harris NJ, Moeller BE, Wymann MP, Amaro RE, Burke JE. Disease-related mutations in PI3Kγ disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors. Elife. 2021, 10:e64691.

DOI: 10.7554/eLife.64691.

Borsari C, Wymann MP. Chimia (Aarau). Targeting Phosphoinositide 3-Kinase – Five Decades of Chemical Space Exploration. 2021, 75 (12), 1037-1044.

DOI: 10.2533/chimia.2021.1037.

Borsari C, Keles E, Rageot D, Treyer A, Bohnacker T, Bissegger L, De Pascale M, Melone A, Sriramaratnam R, Beaufils F, Hamburger M, Hebeisen P, Löscher W, Fabbro D, Hillmann P, Wymann MP. 4-(Difluoromethyl)-5-(4-((3 R,5 S)-3,5-dimethylmorpholino)-6-(( R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders. J Med Chem. 2020, 63 (22), 13595-13617.

DOI: 10.1021/acs.jmedchem.0c00620.

Franchini S, Linciano P, Puja G, Tait A, Borsari C, Denora N, Iacobazzi RM, Brasili L, Sorbi C. Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents. ACS Med Chem Lett. 2020, 11 (5), 1028-1034.

DOI: 10.1021/acsmedchemlett.0c00129.

Borsari C, Trader DJ, Tait A, Costi MP. Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology. J Med Chem. 2020, 63 (5), 1908-1928.

DOI: 10.1021/acs.jmedchem.9b01456.

Linciano P, Cullia G, Borsari C, Santucci M, Ferrari S, Witt G, Gul S, Kuzikov M, Ellinger B, Santarém N, Cordeiro da Silva A, Conti P, Bolognesi ML, Roberti M, Prati F, Bartoccini F, Retini M, Piersanti G, Cavalli A, Goldoni L, Bertozzi SM, Bertozzi F, Brambilla E, Rizzo V, Piomelli D, Pinto A, Bandiera T, Costi MP. Identification of a 2,4-diaminopyrimidine scaffold targeting Trypanosoma brucei pteridine reductase 1 from the LIBRA compound library screening campaign. Eur J Med Chem. 2020, 189, 112047.

DOI: 10.1016/j.ejmech.2020.112047.

Borsari C, Rageot D, Dall’Asen A, Bohnacker T, Melone A, Sele AM, Jackson E, Langlois JB, Beaufils F, Hebeisen P, Fabbro D, Hillmann P, Wymann MP. A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor. J Med Chem. 2019, 62 (18), 8609-8630.

DOI: 10.1021/acs.jmedchem.9b00972.

Rageot D, Bohnacker T, Keles E, McPhail JA, Hoffmann RM, Melone A, Borsari C, Sriramaratnam R, Sele AM, Beaufils F, Hebeisen P, Fabbro D, Hillmann P, Burke JE, Wymann MP. ( S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. J Med Chem. 2019, 62 (13), 6241-6261.

DOI: 10.1021/acs.jmedchem.9b00525.

Landi G, Linciano P, Borsari C, Bertolacini CP, Moraes CB, Cordeiro-da-Silva A, Gul S, Witt G, Kuzikov M, Costi MP, Pozzi C, Mangani S. Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors. ACS Infect Dis. 2019, 5 (7), 1105-1114.

DOI: 10.1021/acsinfecdis.8b00358.

Borsari C, Santarem N, Macedo S, Jiménez-Antón MD, Torrado JJ, Olías-Molero AI, Corral MJ, Tait A, Ferrari S, Costantino L, Luciani R, Ponterini G, Gul S, Kuzikov M, Ellinger B, Behrens B, Reinshagen J, Alunda JM, Cordeiro-da-Silva A, Costi MP. SAR Studies and Biological Characterization of a Chromen-4-one Derivative as an Anti- Trypanosoma brucei Agent. ACS Med Chem Lett. 2019, 10 (4), 528-533.

DOI: 10.1021/acsmedchemlett.8b00565.

Borsari C, Rageot D, Beaufils F, Bohnacker T, Keles E, Buslov I, Melone A, Sele AM, Hebeisen P, Fabbro D, Hillmann P, Wymann MP. Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl-Pyrimidine Moiety. ACS Med Chem Lett. 2019, 10 (10), 1473-1479.

DOI: 10.1021/acsmedchemlett.9b00333.

Borsari C, Jiménez-Antón MD, Eick J, Bifeld E, Torrado JJ, Olías-Molero AI, Corral MJ, Santarem N, Baptista C, Severi L, Gul S, Wolf M, Kuzikov M, Ellinger B, Reinshagen J, Witt G, Linciano P, Tait A, Costantino L, Luciani R, Tejera Nevado P, Zander-Dinse D, Franco CH, Ferrari S, Moraes CB, Cordeiro-da-Silva A, Ponterini G, Clos J, Alunda JM, Costi MP. Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics. Eur J Med Chem. 2019, 183, 111676.

DOI: 10.1016/j.ejmech.2019.111676.

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. Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform. SLAS Discov. 2019, 24 (3), 346-361.

DOI: 10.1177/2472555218823171.

Vanossi D, Caselli M, Pavesi G, Borsari C, Linciano P, Costi MP, Ponterini G. Excited-state intramolecular proton transfer in a bioactive flavonoid provides fluorescence observables for recognizing its engagement with target proteins. Photochem Photobiol Sci. 2019, 18 (9), 2270-2280.

DOI: 10.1039/c9pp00026g.