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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: staben lr. 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 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. Among authors: staben lr. 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 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. Among authors: staben lr. 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. 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
Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.
Wei B, Gunzner-Toste J, Yao H, Wang T, Wang J, Xu Z, Chen J, Wai J, Nonomiya J, Tsai SP, Chuh J, Kozak KR, Liu Y, Yu SF, Lau J, Li G, Phillips GD, Leipold D, Kamath A, Su D, Xu K, Eigenbrot C, Steinbacher S, Ohri R, Raab H, Staben LR, Zhao G, Flygare JA, Pillow TH, Verma V, Masterson LA, Howard PW, Safina B. Wei B, et al. Among authors: staben lr. J Med Chem. 2018 Feb 8;61(3):989-1000. doi: 10.1021/acs.jmedchem.7b01430. Epub 2017 Dec 21. J Med Chem. 2018. PMID: 29227683
Stabilizing a Tubulysin Antibody-Drug Conjugate To Enable Activity Against Multidrug-Resistant Tumors.
Staben LR, Yu SF, Chen J, Yan G, Xu Z, Del Rosario G, Lau JT, Liu L, Guo J, Zheng B, Cruz-Chuh JD, Lee BC, Ohri R, Cai W, Zhou H, Kozak KR, Xu K, Lewis Phillips GD, Lu J, Wai J, Polson AG, Pillow TH. Staben LR, et al. ACS Med Chem Lett. 2017 Sep 5;8(10):1037-1041. doi: 10.1021/acsmedchemlett.7b00243. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057047 Free PMC article.
Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody-drug conjugates.
Staben LR, Koenig SG, Lehar SM, Vandlen R, Zhang D, Chuh J, Yu SF, Ng C, Guo J, Liu Y, Fourie-O'Donohue A, Go M, Linghu X, Segraves NL, Wang T, Chen J, Wei B, Phillips GD, Xu K, Kozak KR, Mariathasan S, Flygare JA, Pillow TH. Staben LR, et al. Nat Chem. 2016 Dec;8(12):1112-1119. doi: 10.1038/nchem.2635. Epub 2016 Oct 17. Nat Chem. 2016. PMID: 27874860
Site-specific trastuzumab maytansinoid antibody-drug conjugates with improved therapeutic activity through linker and antibody engineering.
Pillow TH, Tien J, Parsons-Reponte KL, Bhakta S, Li H, Staben LR, Li G, Chuh J, Fourie-O'Donohue A, Darwish M, Yip V, Liu L, Leipold DD, Su D, Wu E, Spencer SD, Shen BQ, Xu K, Kozak KR, Raab H, Vandlen R, Lewis Phillips GD, Scheller RH, Polakis P, Sliwkowski MX, Flygare JA, Junutula JR. Pillow TH, et al. Among authors: staben lr. J Med Chem. 2014 Oct 9;57(19):7890-9. doi: 10.1021/jm500552c. Epub 2014 Sep 18. J Med Chem. 2014. PMID: 25191794
Discovery of N-[4-[6-tert-butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a potent inhibitor of the hepatitis C virus NS5B polymerase.
Talamas FX, Abbot SC, Anand S, Brameld KA, Carter DS, Chen J, Davis D, de Vicente J, Fung AD, Gong L, Harris SF, Inbar P, Labadie SS, Lee EK, Lemoine R, Le Pogam S, Leveque V, Li J, McIntosh J, Nájera I, Park J, Railkar A, Rajyaguru S, Sangi M, Schoenfeld RC, Staben LR, Tan Y, Taygerly JP, Villaseñor AG, Weller PE. Talamas FX, et al. Among authors: staben lr. J Med Chem. 2014 Mar 13;57(5):1914-31. doi: 10.1021/jm401329s. Epub 2013 Nov 6. J Med Chem. 2014. PMID: 24195700 Free PMC article.