An antibody-drug conjugate targeting GPR56 demonstrates efficacy in preclinical models of colorectal cancer.

ABSTRACT:

Background

Long-term prognosis remains poor for colorectal cancer (CRC) patients with advanced disease due to treatment resistance. The identification of novel targets is essential for the development of new therapeutic approaches. GPR56, an adhesion GPCR, is highly expressed in CRC tumours and correlates with poor survival. Here, we describe the generation and preclinical evaluation of a novel ADC consisting of an anti-GPR56 antibody (10C7) conjugated with the DNA-damaging payload duocarmycin.

Methods

RNA-seq dataset analysis was performed to determine GPR56 expression in CRC subtypes. The specificity of binding, epitope mapping, and internalisation of 10C7 was examined. 10C7 was conjugated to payload and ADC cytotoxicity was assessed against a panel of CRC cell lines and t

SUBMITTER: Jacob J 

PROVIDER: S-EPMC10070492 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature