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Molecular Basis of Valine-Citrulline-PABC Linker Instability in Site-Specific ADCs and Its Mitigation by Linker Design.
Dorywalska M, Dushin R, Moine L, Farias SE, Zhou D, Navaratnam T, Lui V, Hasa-Moreno A, Casas MG, Tran TT, Delaria K, Liu SH, Foletti D, O'Donnell CJ, Pons J, Shelton DL, Rajpal A, Strop P. Dorywalska M, et al. Among authors: zhou d. Mol Cancer Ther. 2016 May;15(5):958-70. doi: 10.1158/1535-7163.MCT-15-1004. Epub 2016 Mar 4. Mol Cancer Ther. 2016. PMID: 26944918
Location matters: site of conjugation modulates stability and pharmacokinetics of antibody drug conjugates.
Strop P, Liu SH, Dorywalska M, Delaria K, Dushin RG, Tran TT, Ho WH, Farias S, Casas MG, Abdiche Y, Zhou D, Chandrasekaran R, Samain C, Loo C, Rossi A, Rickert M, Krimm S, Wong T, Chin SM, Yu J, Dilley J, Chaparro-Riggers J, Filzen GF, O'Donnell CJ, Wang F, Myers JS, Pons J, Shelton DL, Rajpal A. Strop P, et al. Among authors: zhou d. Chem Biol. 2013 Feb 21;20(2):161-7. doi: 10.1016/j.chembiol.2013.01.010. Chem Biol. 2013. PMID: 23438745
Site-Dependent Degradation of a Non-Cleavable Auristatin-Based Linker-Payload in Rodent Plasma and Its Effect on ADC Efficacy.
Dorywalska M, Strop P, Melton-Witt JA, Hasa-Moreno A, Farias SE, Galindo Casas M, Delaria K, Lui V, Poulsen K, Sutton J, Bolton G, Zhou D, Moine L, Dushin R, Tran TT, Liu SH, Rickert M, Foletti D, Shelton DL, Pons J, Rajpal A. Dorywalska M, et al. Among authors: zhou d. PLoS One. 2015 Jul 10;10(7):e0132282. doi: 10.1371/journal.pone.0132282. eCollection 2015. PLoS One. 2015. PMID: 26161543 Free PMC article.
RN927C, a Site-Specific Trop-2 Antibody-Drug Conjugate (ADC) with Enhanced Stability, Is Highly Efficacious in Preclinical Solid Tumor Models.
Strop P, Tran TT, Dorywalska M, Delaria K, Dushin R, Wong OK, Ho WH, Zhou D, Wu A, Kraynov E, Aschenbrenner L, Han B, O'Donnell CJ, Pons J, Rajpal A, Shelton DL, Liu SH. Strop P, et al. Among authors: zhou d. Mol Cancer Ther. 2016 Nov;15(11):2698-2708. doi: 10.1158/1535-7163.MCT-16-0431. Epub 2016 Aug 31. Mol Cancer Ther. 2016. PMID: 27582525
Site-specific conjugation improves therapeutic index of antibody drug conjugates with high drug loading.
Strop P, Delaria K, Foletti D, Witt JM, Hasa-Moreno A, Poulsen K, Casas MG, Dorywalska M, Farias S, Pios A, Lui V, Dushin R, Zhou D, Navaratnam T, Tran TT, Sutton J, Lindquist KC, Han B, Liu SH, Shelton DL, Pons J, Rajpal A. Strop P, et al. Among authors: zhou d. Nat Biotechnol. 2015 Jul;33(7):694-6. doi: 10.1038/nbt.3274. Nat Biotechnol. 2015. PMID: 26154005 No abstract available.
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