Abstract 1779: Anti-Müllerian hormone type II receptor (AMHRII), a cancer target for GM103, a novel antibody-drug conjugate (ADC)

Cancer Research(2018)

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摘要
The anti-Mullerian hormone (AMH) belongs to the TGF-β family and plays a key role during fetal sexual development. Its receptor, AMHRII, is selectively expressed in normal sexual organs in healthy adults. RT-PCR and In Situ Hybridization studies have confirmed that AMHRII expression in normal tissues is restricted to ovary, testis and adrenal gland. AMHRII is re-expressed in gynecologic cancers including ovarian tumors especially in progenitor cancer cells, which makes it an outstanding antigen to be exploited as a target for a novel ADC.Recently, AMHRII expression was also demonstrated in major cancers such as colorectal, non-small cell lung and hepatocarcinoma cancers. GM103 is an ADC, composed of a humanized IgG1 antibody against AMHRII, linked via a cleavable linker to a potent auristatin derivative, using a site-directed conjugation methodology. In this study, we evaluated the in-vitro and in-vivo (xenograft and PDX) efficacy profile of GM103.In vitro experiments using GM103 showed high affinity for AMHRII (K D Citation Format: Olivier Dubreuil, Jean-Marc M. Barret, Raghav Mohan, Martine Pugniere, David Pepin, Delphine Desigaud, William McDowell, Anais Manin, Nicolas Camper, Andre Nicolas, Patricia K. Donahoe, Jean-Francois F. Prost. Anti-Mullerian hormone type II receptor (AMHRII), a cancer target for GM103, a novel antibody-drug conjugate (ADC) [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2018; 2018 Apr 14-18; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2018;78(13 Suppl):Abstract nr 1779.
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关键词
receptor,cancer target,amhrii,antibody-drug
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