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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: dragovich ps. 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
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties.
Dragovich PS, Pillow TH, Blake RA, Sadowsky JD, Adaligil E, Adhikari P, Bhakta S, Blaquiere N, Chen J, Dela Cruz-Chuh J, Gascoigne KE, Hartman SJ, He M, Kaufman S, Kleinheinz T, Kozak KR, Liu L, Liu L, Liu Q, Lu Y, Meng F, Mulvihill MM, O'Donohue A, Rowntree RK, Staben LR, Staben ST, Wai J, Wang J, Wei B, Wilson C, Xin J, Xu Z, Yao H, Zhang D, Zhang H, Zhou H, Zhu X. Dragovich PS, et al. J Med Chem. 2021 Mar 11;64(5):2534-2575. doi: 10.1021/acs.jmedchem.0c01845. Epub 2021 Feb 17. J Med Chem. 2021. PMID: 33596065
Systematic Variation of Pyrrolobenzodiazepine (PBD)-Dimer Payload Physicochemical Properties Impacts Efficacy and Tolerability of the Corresponding Antibody-Drug Conjugates.
Staben LR, Chen J, Cruz-Chuh JD, Del Rosario G, Go MA, Guo J, Khojasteh SC, Kozak KR, Li G, Ng C, Lewis Phillips GD, Pillow TH, Rowntree RK, Wai J, Wei B, Xu K, Xu Z, Yu SF, Zhang D, Dragovich PS. Staben LR, et al. Among authors: dragovich ps. J Med Chem. 2020 Sep 10;63(17):9603-9622. doi: 10.1021/acs.jmedchem.0c00691. Epub 2020 Aug 18. J Med Chem. 2020. PMID: 32787101
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.
Dragovich PS, Pillow TH, Blake RA, Sadowsky JD, Adaligil E, Adhikari P, Chen J, Corr N, Dela Cruz-Chuh J, Del Rosario G, Fullerton A, Hartman SJ, Jiang F, Kaufman S, Kleinheinz T, Kozak KR, Liu L, Lu Y, Mulvihill MM, Murray JM, O'Donohue A, Rowntree RK, Sawyer WS, Staben LR, Wai J, Wang J, Wei B, Wei W, Xu Z, Yao H, Yu SF, Zhang D, Zhang H, Zhang S, Zhao Y, Zhou H, Zhu X. Dragovich PS, et al. J Med Chem. 2021 Mar 11;64(5):2576-2607. doi: 10.1021/acs.jmedchem.0c01846. Epub 2021 Feb 17. J Med Chem. 2021. PMID: 33596073
Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).
Dragovich PS, Adhikari P, Blake RA, Blaquiere N, Chen J, Cheng YX, den Besten W, Han J, Hartman SJ, He J, He M, Rei Ingalla E, Kamath AV, Kleinheinz T, Lai T, Leipold DD, Li CS, Liu Q, Lu J, Lu Y, Meng F, Meng L, Ng C, Peng K, Lewis Phillips G, Pillow TH, Rowntree RK, Sadowsky JD, Sampath D, Staben L, Staben ST, Wai J, Wan K, Wang X, Wei B, Wertz IE, Xin J, Xu K, Yao H, Zang R, Zhang D, Zhou H, Zhao Y. Dragovich PS, et al. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126907. doi: 10.1016/j.bmcl.2019.126907. Epub 2019 Dec 18. Bioorg Med Chem Lett. 2020. PMID: 31902710
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Giannetti AM, Zheng X, Skelton NJ, Wang W, Bravo BJ, Bair KW, Baumeister T, Cheng E, Crocker L, Feng Y, Gunzner-Toste J, Ho YC, Hua R, Liederer BM, Liu Y, Ma X, O'Brien T, Oeh J, Sampath D, Shen Y, Wang C, Wang L, Wu H, Xiao Y, Yuen PW, Zak M, Zhao G, Zhao Q, Dragovich PS. Giannetti AM, et al. Among authors: dragovich ps. J Med Chem. 2014 Feb 13;57(3):770-92. doi: 10.1021/jm4015108. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24405419
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.
Zak M, Hurley CA, Ward SI, Bergeron P, Barrett K, Balazs M, Blair WS, Bull R, Chakravarty P, Chang C, Crackett P, Deshmukh G, DeVoss J, Dragovich PS, Eigenbrot C, Ellwood C, Gaines S, Ghilardi N, Gibbons P, Gradl S, Gribling P, Hamman C, Harstad E, Hewitt P, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Labadie S, Lee WP, Liao J, Liimatta M, Mendonca R, Narukulla R, Pulk R, Reeve A, Savage S, Shia S, Steffek M, Ubhayakar S, van Abbema A, Aliagas I, Avitabile-Woo B, Xiao Y, Yang J, Kulagowski JJ. Zak M, et al. Among authors: dragovich ps. J Med Chem. 2013 Jun 13;56(11):4764-85. doi: 10.1021/jm4004895. Epub 2013 May 31. J Med Chem. 2013. PMID: 23659214
Antibody-Drug Conjugates for Immunology.
Dragovich PS. Dragovich PS. J Med Chem. 2022 Mar 24;65(6):4496-4499. doi: 10.1021/acs.jmedchem.2c00339. Epub 2022 Mar 14. J Med Chem. 2022. PMID: 35285623
91 results