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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: li g, li h. J Med Chem. 2014 Oct 9;57(19):7890-9. doi: 10.1021/jm500552c. Epub 2014 Sep 18. J Med Chem. 2014. PMID: 25191794
Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate.
Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, Blättler WA, Lambert JM, Chari RV, Lutz RJ, Wong WL, Jacobson FS, Koeppen H, Schwall RH, Kenkare-Mitra SR, Spencer SD, Sliwkowski MX. Lewis Phillips GD, et al. Among authors: li g. Cancer Res. 2008 Nov 15;68(22):9280-90. doi: 10.1158/0008-5472.CAN-08-1776. Cancer Res. 2008. PMID: 19010901
Engineered thio-trastuzumab-DM1 conjugate with an improved therapeutic index to target human epidermal growth factor receptor 2-positive breast cancer.
Junutula JR, Flagella KM, Graham RA, Parsons KL, Ha E, Raab H, Bhakta S, Nguyen T, Dugger DL, Li G, Mai E, Lewis Phillips GD, Hiraragi H, Fuji RN, Tibbitts J, Vandlen R, Spencer SD, Scheller RH, Polakis P, Sliwkowski MX. Junutula JR, et al. Among authors: li g. Clin Cancer Res. 2010 Oct 1;16(19):4769-78. doi: 10.1158/1078-0432.CCR-10-0987. Epub 2010 Aug 30. Clin Cancer Res. 2010. PMID: 20805300
Dual targeting of HER2-positive cancer with trastuzumab emtansine and pertuzumab: critical role for neuregulin blockade in antitumor response to combination therapy.
Phillips GD, Fields CT, Li G, Dowbenko D, Schaefer G, Miller K, Andre F, Burris HA 3rd, Albain KS, Harbeck N, Dieras V, Crivellari D, Fang L, Guardino E, Olsen SR, Crocker LM, Sliwkowski MX. Phillips GD, et al. Among authors: li g. Clin Cancer Res. 2014 Jan 15;20(2):456-68. doi: 10.1158/1078-0432.CCR-13-0358. Epub 2013 Oct 4. Clin Cancer Res. 2014. PMID: 24097864 Clinical Trial.
Antitumor efficacy of a bispecific antibody that targets HER2 and activates T cells.
Junttila TT, Li J, Johnston J, Hristopoulos M, Clark R, Ellerman D, Wang BE, Li Y, Mathieu M, Li G, Young J, Luis E, Lewis Phillips G, Stefanich E, Spiess C, Polson A, Irving B, Scheer JM, Junttila MR, Dennis MS, Kelley R, Totpal K, Ebens A. Junttila TT, et al. Among authors: li y, li j, li g. Cancer Res. 2014 Oct 1;74(19):5561-71. doi: 10.1158/0008-5472.CAN-13-3622-T. Epub 2014 Sep 16. Cancer Res. 2014. PMID: 25228655
The cryptophycins as potent payloads for antibody drug conjugates.
Verma VA, Pillow TH, DePalatis L, Li G, Phillips GL, Polson AG, Raab HE, Spencer S, Zheng B. Verma VA, et al. Among authors: li g. Bioorg Med Chem Lett. 2015 Feb 15;25(4):864-8. doi: 10.1016/j.bmcl.2014.12.070. Epub 2015 Jan 2. Bioorg Med Chem Lett. 2015. PMID: 25613677
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: li g. 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: li g. Bioconjug Chem. 2017 Oct 18;28(10):2538-2548. doi: 10.1021/acs.bioconjchem.7b00365. Epub 2017 Sep 22. Bioconjug Chem. 2017. PMID: 28885827
Pyrrolobenzodiazepine Dimer Antibody-Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers.
Gregson SJ, Masterson LA, Wei B, Pillow TH, Spencer SD, Kang GD, Yu SF, Raab H, Lau J, Li G, Lewis Phillips GD, Gunzner-Toste J, Safina BS, Ohri R, Darwish M, Kozak KR, Dela Cruz-Chuh J, Polson A, Flygare JA, Howard PW. Gregson SJ, et al. Among authors: li g. J Med Chem. 2017 Dec 14;60(23):9490-9507. doi: 10.1021/acs.jmedchem.7b00736. Epub 2017 Nov 16. J Med Chem. 2017. PMID: 29112410
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