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. 2021 Jun 10;12:3528. doi: 10.1038/s41467-021-23793-7

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© The Author(s) 2021

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Fig. 1 — MTGase-mediated conjugation of bi-functional branched linkers and following orthogonal click reactions with two payload modules afford homogeneous dual-drug ADCs with defined DARs (magenta circle: MMAE; yellow triangle: MMAF). Preparation of anti-HER2 ADC with a DAR of MMAE/F 4 + 2 is shown as an example. The glutamic acid–valine–citrulline (GluValCit)–PABC linker ensures in vivo stability, while allowing for quick and traceless release of payloads upon internalization and following cathepsin-mediated cleavage in lysosomes. DAR, drug-to-antibody ratio; DBCO, dibenzocyclooctyne; MTGase, microbial transglutaminase; PABC, p-aminobenzyloxycarbonyl; PEG, polyethylene glycol; TCO, trans-cyclooctene.