Ontology highlight
ABSTRACT:
SUBMITTER: Hwang D
PROVIDER: S-EPMC6754284 | biostudies-literature | 2019 Sep
REPOSITORIES: biostudies-literature
Cell chemical biology 20190620 9
Homogeneous antibody-drug conjugates (ADCs) that use a highly reactive buried lysine (Lys) residue embedded in a dual variable domain (DVD)-IgG1 format can be assembled with high precision and efficiency under mild conditions. Here we show that replacing the Lys with an arginine (Arg) residue affords an orthogonal ADC assembly that is site-selective and stable. X-ray crystallography confirmed the location of the reactive Arg residue at the bottom of a deep pocket. As the Lys-to-Arg mutation is c ...[more]