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Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity.
Pillow TH, Adhikari P, Blake RA, Chen J, Del Rosario G, Deshmukh G, Figueroa I, Gascoigne KE, Kamath AV, Kaufman S, Kleinheinz T, Kozak KR, Latifi B, Leipold DD, Sing Li C, Li R, Mulvihill MM, O'Donohue A, Rowntree RK, Sadowsky JD, Wai J, Wang X, Wu C, Xu Z, Yao H, Yu SF, Zhang D, Zang R, Zhang H, Zhou H, Zhu X, Dragovich PS. Pillow TH, et al. Among authors: xu z. ChemMedChem. 2020 Jan 7;15(1):17-25. doi: 10.1002/cmdc.201900497. Epub 2019 Nov 14. ChemMedChem. 2020. PMID: 31674143
Conjugation of Indoles to Antibodies through a Novel Self-Immolating Linker.
Dragovich PS, Blake RA, Chen C, Chen J, Chuh J, den Besten W, Fan F, Fourie A, Hartman SJ, He C, He J, Ingalla ER, Kozak KR, Leong SR, Lu J, Ma Y, Meng L, Nannini M, Oeh J, Ohri R, Lewis Phillips G, Pillow TH, Rowntree RK, Sampath D, Vandlen R, Vollmar B, Wai J, Wertz IE, Xu K, Xu Z, Zhang D. Dragovich PS, et al. Among authors: xu k, xu z. Chemistry. 2018 Apr 3;24(19):4830-4834. doi: 10.1002/chem.201800859. Epub 2018 Mar 25. Chemistry. 2018. PMID: 29493023
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: xu z. 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
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: xu z. 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
Linker Immolation Determines Cell Killing Activity of Disulfide-Linked Pyrrolobenzodiazepine Antibody-Drug Conjugates.
Zhang D, Pillow TH, Ma Y, Cruz-Chuh JD, Kozak KR, Sadowsky JD, Lewis Phillips GD, Guo J, Darwish M, Fan P, Chen J, He C, Wang T, Yao H, Xu Z, Chen J, Wai J, Pei Z, Hop CE, Khojasteh SC, Dragovich PS. Zhang D, et al. Among authors: xu z. ACS Med Chem Lett. 2016 Aug 26;7(11):988-993. doi: 10.1021/acsmedchemlett.6b00233. eCollection 2016 Nov 10. ACS Med Chem Lett. 2016. PMID: 27882196 Free PMC article.
Development of Efficient Chemistry to Generate Site-Specific Disulfide-Linked Protein- and Peptide-Payload Conjugates: Application to THIOMAB Antibody-Drug Conjugates.
Sadowsky JD, Pillow TH, Chen J, Fan F, He C, Wang Y, Yan G, Yao H, Xu Z, Martin S, Zhang D, Chu P, Dela Cruz-Chuh J, O'Donohue A, Li G, Del Rosario G, He J, Liu L, Ng C, Su D, Lewis Phillips GD, Kozak KR, Yu SF, Xu K, Leipold D, Wai J. Sadowsky JD, et al. Among authors: xu k, xu z. Bioconjug Chem. 2017 Aug 16;28(8):2086-2098. doi: 10.1021/acs.bioconjchem.7b00258. Epub 2017 Jul 13. Bioconjug Chem. 2017. PMID: 28636382
Exploration of Pyrrolobenzodiazepine (PBD)-Dimers Containing Disulfide-Based Prodrugs as Payloads for Antibody-Drug Conjugates.
Pei Z, Chen C, Chen J, Cruz-Chuh JD, Delarosa R, Deng Y, Fourie-O'Donohue A, Figueroa I, Guo J, Jin W, Khojasteh SC, Kozak KR, Latifi B, Lee J, Li G, Lin E, Liu L, Lu J, Martin S, Ng C, Nguyen T, Ohri R, Lewis Phillips G, Pillow TH, Rowntree RK, Stagg NJ, Stokoe D, Ulufatu S, Verma VA, Wai J, Wang J, Xu K, Xu Z, Yao H, Yu SF, Zhang D, Dragovich PS. Pei Z, et al. Among authors: xu k, xu z. Mol Pharm. 2018 Sep 4;15(9):3979-3996. doi: 10.1021/acs.molpharmaceut.8b00431. Epub 2018 Aug 6. Mol Pharm. 2018. PMID: 30040421
Antibody-Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo.
Su D, Chen J, Cosino E, Dela Cruz-Chuh J, Davis H, Del Rosario G, Figueroa I, Goon L, He J, Kamath AV, Kaur S, Kozak KR, Lau J, Lee D, Lee MV, Leipold D, Liu L, Liu P, Lu GL, Nelson C, Ng C, Pillow TH, Polakis P, Polson AG, Rowntree RK, Saad O, Safina B, Stagg NJ, Tercel M, Vandlen R, Vollmar BS, Wai J, Wang T, Wei B, Xu K, Xue J, Xu Z, Yan G, Yao H, Yu SF, Zhang D, Zhong F, Dragovich PS. Su D, et al. Among authors: xu k, xu z. Bioconjug Chem. 2019 May 15;30(5):1356-1370. doi: 10.1021/acs.bioconjchem.9b00133. Epub 2019 Apr 22. Bioconjug Chem. 2019. PMID: 30966735
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: xu k, xu z. 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
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