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Page 1
PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models.
Berlin M, Cantley J, Bookbinder M, Bortolon E, Broccatelli F, Cadelina G, Chan EW, Chen H, Chen X, Cheng Y, Cheung TK, Davenport K, DiNicola D, Gordon D, Hamman BD, Harbin A, Haskell R, He M, Hole AJ, Januario T, Kerry PS, Koenig SG, Li L, Merchant M, Pérez-Dorado I, Pizzano J, Quinn C, Rose CM, Rousseau E, Soto L, Staben LR, Sun H, Tian Q, Wang J, Wang W, Ye CS, Ye X, Zhang P, Zhou Y, Yauch R, Dragovich PS. Berlin M, et al. Among authors: bortolon e. J Med Chem. 2024 Jan 25;67(2):1262-1313. doi: 10.1021/acs.jmedchem.3c01781. Epub 2024 Jan 5. J Med Chem. 2024. PMID: 38180485
Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers.
Cantley J, Ye X, Rousseau E, Januario T, Hamman BD, Rose CM, Cheung TK, Hinkle T, Soto L, Quinn C, Harbin A, Bortolon E, Chen X, Haskell R, Lin E, Yu SF, Del Rosario G, Chan E, Dunlap D, Koeppen H, Martin S, Merchant M, Grimmer M, Broccatelli F, Wang J, Pizzano J, Dragovich PS, Berlin M, Yauch RL. Cantley J, et al. Among authors: bortolon e. Nat Commun. 2022 Nov 10;13(1):6814. doi: 10.1038/s41467-022-34562-5. Nat Commun. 2022. PMID: 36357397 Free PMC article.
Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs.
Kou P, Levy ES, Nguyen AD, Zhang D, Chen S, Cui Y, Zhang X, Broccatelli F, Pizzano J, Cantley J, Bortolon E, Rousseau E, Berlin M, Dragovich P, Sethuraman V. Kou P, et al. Among authors: bortolon e. Pharmaceutics. 2023 Aug 8;15(8):2098. doi: 10.3390/pharmaceutics15082098. Pharmaceutics. 2023. PMID: 37631312 Free PMC article.
Sorafenib (BAY 43-9006) inhibits tumor growth and vascularization and induces tumor apoptosis and hypoxia in RCC xenograft models.
Chang YS, Adnane J, Trail PA, Levy J, Henderson A, Xue D, Bortolon E, Ichetovkin M, Chen C, McNabola A, Wilkie D, Carter CA, Taylor IC, Lynch M, Wilhelm S. Chang YS, et al. Among authors: bortolon e. Cancer Chemother Pharmacol. 2007 Apr;59(5):561-74. doi: 10.1007/s00280-006-0393-4. Epub 2006 Dec 8. Cancer Chemother Pharmacol. 2007. PMID: 17160391
Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.
Dumas J, Hatoum-Mokdad H, Sibley RN, Smith RA, Scott WJ, Khire U, Lee W, Wood J, Wolanin D, Cooley J, Bankston D, Redman AM, Schoenleber R, Caringal Y, Gunn D, Romero R, Osterhout M, Paulsen H, Housley TJ, Wilhelm SM, Pirro J, Chien DS, Ranges GE, Shrikhande A, Muzsi A, Bortolon E, Wakefield J, Gianpaolo Ostravage C, Bhargava A, Chau T. Dumas J, et al. Among authors: bortolon e. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1559-62. doi: 10.1016/s0960-894x(02)00238-x. Bioorg Med Chem Lett. 2002. PMID: 12039561