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Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.
Carcache DA, Vulpetti A, Kallen J, Mattes H, Orain D, Stringer R, Vangrevelinghe E, Wolf RM, Kaupmann K, Ottl J, Dawson J, Cooke NG, Hoegenauer K, Billich A, Wagner J, Guntermann C, Hintermann S. Carcache DA, et al. Among authors: vulpetti a. J Med Chem. 2018 Aug 9;61(15):6724-6735. doi: 10.1021/acs.jmedchem.8b00529. Epub 2018 Jul 24. J Med Chem. 2018. PMID: 29990434
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.
Pulz R, Angst D, Dawson J, Gessier F, Gutmann S, Hersperger R, Hinniger A, Janser P, Koch G, Revesz L, Vulpetti A, Waelchli R, Zimmerlin A, Cenni B. Pulz R, et al. Among authors: vulpetti a. ACS Med Chem Lett. 2019 Sep 6;10(10):1467-1472. doi: 10.1021/acsmedchemlett.9b00317. eCollection 2019 Oct 10. ACS Med Chem Lett. 2019. PMID: 31620235 Free PMC article.
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G, Gutmann S, Scheufler C, Hinniger A, Zimmerlin A, Funhoff EG, Pulz R, Cenni B. Angst D, et al. Among authors: vulpetti a. J Med Chem. 2020 May 28;63(10):5102-5118. doi: 10.1021/acs.jmedchem.9b01916. Epub 2020 Mar 4. J Med Chem. 2020. PMID: 32083858
Ligandability Assessment of IL-1β by Integrated Hit Identification Approaches.
Vulpetti A, Rondeau JM, Bellance MH, Blank J, Boesch R, Boettcher A, Bornancin F, Buhr S, Connor LE, Dumelin CE, Esser O, Hediger M, Hintermann S, Hommel U, Koch E, Lapointe G, Leder L, Lehmann S, Lehr P, Meier P, Muller L, Ostermeier D, Ramage P, Schiebel-Haddad S, Smith AB, Stojanovic A, Velcicky J, Yamamoto R, Hurth K. Vulpetti A, et al. J Med Chem. 2024 May 23;67(10):8141-8160. doi: 10.1021/acs.jmedchem.4c00240. Epub 2024 May 10. J Med Chem. 2024. PMID: 38728572
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J. Lorthiois E, et al. Among authors: vulpetti a. J Med Chem. 2017 Jul 13;60(13):5717-5735. doi: 10.1021/acs.jmedchem.7b00425. Epub 2017 Jun 30. J Med Chem. 2017. PMID: 28621538
Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase.
Hoegenauer K, An S, Axford J, Benander C, Bergsdorf C, Botsch J, Chau S, Fernández C, Gleim S, Hassiepen U, Hunziker J, Joly E, Keller A, Lopez Romero S, Maher R, Mangold AS, Mickanin C, Mihalic M, Neuner P, Patterson AW, Perruccio F, Roggo S, Scesa J, Schröder M, Shkoza D, Thai B, Vulpetti A, Renatus M, Reece-Hoyes JS. Hoegenauer K, et al. Among authors: vulpetti a. ACS Med Chem Lett. 2023 Nov 13;14(12):1631-1639. doi: 10.1021/acsmedchemlett.3c00259. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116426
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.
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. Brasca MG, et al. Among authors: vulpetti a. J Med Chem. 2009 Aug 27;52(16):5152-63. doi: 10.1021/jm9006559. J Med Chem. 2009. PMID: 19603809
70 results