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1.
Bioconjug Chem ; 35(2): 140-146, 2024 02 21.
Artigo em Inglês | MEDLINE | ID: mdl-38265691

RESUMO

Antibody-drug conjugates (ADCs) are an established modality that allow for targeted delivery of a potent molecule, or payload, to a desired site of action. ADCs, wherein the payload is a targeted protein degrader, are an emerging area in the field. Herein we describe our efforts of delivering a Bruton's tyrosine kinase (BTK) bifunctional degrader 1 via a CD79b mAb (monoclonal antibody) where the degrader is linked at the ligase binding portion of the payload via a cleavable linker to the mAb. The resulting CD79b ADCs, 3 and 4, exhibit in vitro degradation and cytotoxicity comparable with that of 1, and ADC 3 can achieve more sustained in vivo degradation than intravenously administered 1 with markedly reduced systemic exposure of the payload.


Assuntos
Imunoconjugados , Imunoconjugados/química , Tirosina Quinase da Agamaglobulinemia , Anticorpos Monoclonais/química
2.
Commun Biol ; 4(1): 1085, 2021 09 15.
Artigo em Inglês | MEDLINE | ID: mdl-34526658

RESUMO

We present two high-throughput compatible methods to detect the interaction of ectopically expressed (RT-Bind) or endogenously tagged (EndoBind) proteins of interest. Both approaches provide temporal evaluation of dimer formation over an extended duration. Using examples of the Nrf2-KEAP1 and the CRAF-KRAS-G12V interaction, we demonstrate that our method allows for the detection of signal for more than 2 days after substrate addition, allowing for continuous monitoring of endogenous protein-protein interactions in real time.


Assuntos
Ensaios de Triagem em Larga Escala/métodos , Proteína 1 Associada a ECH Semelhante a Kelch/química , Fator 2 Relacionado a NF-E2/química , Proteínas Proto-Oncogênicas p21(ras)/química , Células HEK293 , Humanos , Ligação Proteica
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