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Page 1
Optimization of a Novel DEL Hit That Binds in the Cbl-b SH2 Domain and Blocks Substrate Binding.
Liang J, Lambrecht MJ, Arenzana TL, Aubert-Nicol S, Bao L, Broccatelli F, Cai J, Eidenschenk C, Everett C, Garner T, Gruber F, Haghshenas P, Huestis MP, Hsu PL, Kou P, Jakalian A, Larouche-Gauthier R, Leclerc JP, Leung DH, Martin A, Murray J, Prangley M, Rutz S, Kakiuchi-Kiyota S, Satz AL, Skelton NJ, Steffek M, Stoffler D, Sudhamsu J, Tan S, Wang J, Wang S, Wang Q, Wendorff TJ, Wichert M, Yadav A, Yu C, Wang X. Liang J, et al. Among authors: broccatelli f. ACS Med Chem Lett. 2024 May 29;15(6):864-872. doi: 10.1021/acsmedchemlett.4c00068. eCollection 2024 Jun 13. ACS Med Chem Lett. 2024. PMID: 38894924
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: broccatelli f. 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
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: broccatelli f. Pharmaceutics. 2023 Aug 8;15(8):2098. doi: 10.3390/pharmaceutics15082098. Pharmaceutics. 2023. PMID: 37631312 Free PMC article.
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: broccatelli f. Nat Commun. 2022 Nov 10;13(1):6814. doi: 10.1038/s41467-022-34562-5. Nat Commun. 2022. PMID: 36357397 Free PMC article.
Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays.
Pierrat OA, Liu M, Collie GW, Shetty K, Rodrigues MJ, Le Bihan YV, Gunnell EA, McAndrew PC, Stubbs M, Rowlands MG, Yahya N, Shehu E, Talbot R, Pickard L, Bellenie BR, Cheung KJ, Drouin L, Innocenti P, Woodward H, Davis OA, Lloyd MG, Varela A, Huckvale R, Broccatelli F, Carter M, Galiwango D, Hayes A, Raynaud FI, Bryant C, Whittaker S, Rossanese OW, Hoelder S, Burke R, van Montfort RLM. Pierrat OA, et al. Among authors: broccatelli f. Sci Rep. 2022 Nov 3;12(1):18633. doi: 10.1038/s41598-022-23264-z. Sci Rep. 2022. PMID: 36329085 Free PMC article.
34 results