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Near-IR Light-Mediated Cleavage of Antibody-Drug Conjugates Using Cyanine Photocages.


ABSTRACT: Despite significant progress in the clinical application of antibody drug conjugates (ADCs), novel cleavage strategies that provide improved selectivity are still needed. Herein is reported the first approach that uses near-IR light to cleave a small molecule from a biomacromolecule, and its application to the problem of ADC linkage. The preparation of cyanine antibody conjugates, drug cleavage mediated by 690?nm light, and initial in vitro and in vivo evaluation is described. These studies provide the critical chemical underpinning from which to develop this near-IR light cleavable linker strategy.

SUBMITTER: Nani RR 

PROVIDER: S-EPMC4743669 | biostudies-literature | 2015 Nov

REPOSITORIES: biostudies-literature

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Near-IR Light-Mediated Cleavage of Antibody-Drug Conjugates Using Cyanine Photocages.

Nani Roger R RR   Gorka Alexander P AP   Nagaya Tadanobu T   Kobayashi Hisataka H   Schnermann Martin J MJ  

Angewandte Chemie (International ed. in English) 20150925 46


Despite significant progress in the clinical application of antibody drug conjugates (ADCs), novel cleavage strategies that provide improved selectivity are still needed. Herein is reported the first approach that uses near-IR light to cleave a small molecule from a biomacromolecule, and its application to the problem of ADC linkage. The preparation of cyanine antibody conjugates, drug cleavage mediated by 690 nm light, and initial in vitro and in vivo evaluation is described. These studies prov  ...[more]

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