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Antibody-drug Conjugates & Bioconjugates


Chuprakov, S.C., et al. (2021) Tandem-cleavage linkers improve the in vivo stability and tolerability of antibody-drug conjugates. Bioconjugate Chemistry. 32: 746-754.

Barfield, R.M. et al. (2020) A novel HER2-targeted antibody-drug conjugate offers the possibility of clinical dosing at trastuzumab-equivalent exposure levels. Molecular Cancer Therapeutics. 19: 1866-1874.

Hernandez-Alba O et al. A Case Study to Identify the Drug Conjugation Site of a Site-Specific Antibody-Drug Conjugate Using Middle-Down Mass Spectrometry. J Am Soc Mass Spectrum. 2019.

Bauzon, M. et al. (2019) Maytansine-bearing antibody-drug conjugates induce in vitro hallmarks of immunogenic cell death selectively in antigen-positive target cells. OncoImmunology. doi: 10.1080/2162402X.2019.1565859

Tsui, K. et al. (2019) CRISPR-Cas9 screens identify regulators of antibody-drug conjugate toxicity. Nature Chemical Biology. 15:949-958.

Huang, B.C.B. et al. (2018) Antibody-drug conjugate library prepared by scanning insertion of the aldehyde tag into IgG1 constant regions. mAbs. 10:1182-1189.

Drake, P. et al. (2018) CAT-02-106, a Site-Specifically Conjugated Anti-CD22 Antibody Bearing an MDR1-Resistant Maytansine Payload Yields Excellent Efficacy and Safety in Preclinical Models. Molecular Cancer Therapeutics. 17:161-168.

Linz, T. et al. (2018) Systematic LC/MS/MS investigations for the IND-enabling extended characterization of antibody-drug conjugate modifications. Antibodies. doi: 10.3390/antib7040040.

Drake, P. and D. Rabuka. (2017) Recent developments in ADC technology: Preclinical studies signal future clinical trends. BioDrugs. doi: 10.1007/s40259-017-0254-1.

Botzanowski, T. et al. (2017) Insights from native mass spectrometry approaches for top- and middle-level characterization of site-specific antibody-drug conjugates. MAbs. 9(5):801-811. doi: 10.1080/19420862.2017.1316914.

Kudirka, R. et al. (2016) Site-specific tandem Knoevenagel condensation-Michael addition to generate antibody-drug conjugates. ACS Medicinal Chemistry Letters. 7(11):994-998.

Zmolek, W. et al. (2016) A simple LC/MRM-MS-based method to quantify free linker-payload in antibody-drug conjugate preparations. Journal of Chromatography B. 1032:144-148.

York, D. et al. (2016) Generating aldehyde-tagged antibodies with high titers and high formylglycine yields by supplementing culture media with copper(II). BMC Biotechnology. 16:23. doi: 10.1186/s12896-016-0254-0.

Drake, P. and D. Rabuka. (2015) An emerging playbook for antibody-drug conjugates: lessons from the laboratory and clinic suggest a strategy for improving efficacy and safety. Current Opinion in Chemical Biology. 28:174-180.

Holder, P. et al. (2015) Reconstitution of formylglycine-generating enzyme with copper(II) for aldehyde tag conversion. Journal of Biological Chemistry 290:15730-15745.

Kudirka, R. et al. (2015) Generating site-specifically modified proteins via a versatile and stable nucleophilic carbon ligation. Chemistry & Biology 22, 293-298.

Liu, J. et al. (2015) An efficient site-specific method for irreversible covalent labeling of protein with a fluorophore. Scientific Reports doi: 10.1038/srep16883.

Albers, A. et al. (2014) Exploring the effects of linker composition on site-specifically modified antibody-drug conjugates. European J. Medicinal Chemistry 88, 3-9

Drake, P. et al. (2014) Aldehyde tag coupled with HIPS chemistry enables the production of ADCs conjugated site-specifically to different antibody regions with distinct in vivo efficacy and PK outcomes. Bioconjugate Chemistry 25, 1331-1341

Liang, S. et al. (2014) A modular approach for assembling aldehyde-tagged proteins on DNA scaffolds. J. Am. Chem. Soc. 136:10850-10853.

Agarwal, P. et al. (2013) HydrazinoPictet-Spengler ligation as a biocompatible method for the generation of stable protein conjugates. Bioconjugate Chemistry 24, 846-851

Hudak, J., et al. (2012) Synthesis of heterobifunctional protein fusions using copper-free click chemistry and the aldehyde tag. Agnew Chem Int Ed Engl. 4161-5

Rabuka, D. et al. (2012) Site-specific chemical protein conjugation using genetically encoded aldehyde tags. Nature Protocols. 7:1052-1067.