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Attachment Site Cysteine Thiol pKa Is a Key Driver for Site-Dependent Stability of THIOMAB Antibody-Drug Conjugates.

Bioconjugate chemistry - 18 Oct 2017

Vollmar Breanna S, Wei Binqing, Ohri Rachana, Zhou Jianhui, He Jintang, Yu Shang-Fan, Leipold Douglas, Cosino Ely, Yee Sharon, Fourie-O'Donohue Aimee, Li Guangmin, Phillips Gail L, Kozak Katherine R, Kamath Amrita, Xu Keyang, Lee Genee, Lazar Greg A, Erickson Hans K

Abstract excerpt

The incorporation of cysteines into antibodies by mutagenesis allows for the direct conjugation of small molecules to specific sites on the antibody via disulfide bonds. The stability of the disulfide bond linkage between the small molecule and the antibody is highly dependent on the location of the engineered cysteine in either the heavy chain (HC) or the light chain (LC) of the antibody. Here, we explore the...

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PMID: 28885827
DOI: 10.1021/acs.bioconjchem.7b00365

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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