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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: xu k. J Med Chem. 2014 Oct 9;57(19):7890-9. doi: 10.1021/jm500552c. Epub 2014 Sep 18. J Med Chem. 2014. PMID: 25191794
Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates.
Shen BQ, Xu K, Liu L, Raab H, Bhakta S, Kenrick M, Parsons-Reponte KL, Tien J, Yu SF, Mai E, Li D, Tibbitts J, Baudys J, Saad OM, Scales SJ, McDonald PJ, Hass PE, Eigenbrot C, Nguyen T, Solis WA, Fuji RN, Flagella KM, Patel D, Spencer SD, Khawli LA, Ebens A, Wong WL, Vandlen R, Kaur S, Sliwkowski MX, Scheller RH, Polakis P, Junutula JR. Shen BQ, et al. Among authors: xu k. Nat Biotechnol. 2012 Jan 22;30(2):184-9. doi: 10.1038/nbt.2108. Nat Biotechnol. 2012. PMID: 22267010
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. Among authors: xu k. Nat Chem. 2016 Dec;8(12):1112-1119. doi: 10.1038/nchem.2635. Epub 2016 Oct 17. Nat Chem. 2016. PMID: 27874860
Modulating Therapeutic Activity and Toxicity of Pyrrolobenzodiazepine Antibody-Drug Conjugates with Self-Immolative Disulfide Linkers.
Pillow TH, Schutten M, Yu SF, Ohri R, Sadowsky J, Poon KA, Solis W, Zhong F, Del Rosario G, Go MAT, Lau J, Yee S, He J, Liu L, Ng C, Xu K, Leipold DD, Kamath AV, Zhang D, Masterson L, Gregson SJ, Howard PW, Fang F, Chen J, Gunzner-Toste J, Kozak KK, Spencer S, Polakis P, Polson AG, Flygare JA, Junutula JR. Pillow TH, et al. Among authors: xu k. Mol Cancer Ther. 2017 May;16(5):871-878. doi: 10.1158/1535-7163.MCT-16-0641. Epub 2017 Feb 21. Mol Cancer Ther. 2017. PMID: 28223423
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
Attachment Site Cysteine Thiol pKa Is a Key Driver for Site-Dependent Stability of THIOMAB Antibody-Drug Conjugates.
Vollmar BS, Wei B, Ohri R, Zhou J, He J, Yu SF, Leipold D, Cosino E, Yee S, Fourie-O'Donohue A, Li G, Phillips GL, Kozak KR, Kamath A, Xu K, Lee G, Lazar GA, Erickson HK. Vollmar BS, et al. Among authors: xu k. Bioconjug Chem. 2017 Oct 18;28(10):2538-2548. doi: 10.1021/acs.bioconjchem.7b00365. Epub 2017 Sep 22. Bioconjug Chem. 2017. PMID: 28885827
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. Among authors: xu k, xu z. 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.
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