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Identification and therapeutic targeting of GPR20, selectively expressed in gastrointestinal stromal tumorswith DS-6157a, a first-in-class antibody-drug conjugate

Iida K, Abdelhamid Ahmed AH, Nagatsuma AK, Shibutani T, Yasuda S, Kitamura M, Hattori C, Abe M, Hasegawa J, Iguchi T, Karibe T, Nakada T, Inaki K, Kamei R, Abe Y, Nomura T, Andersen JL, Santagata S, Hemming ML, George S, Doi T, Ochiai A, Demetri GD, Agatsuma T (2021) Identification and therapeutic targeting of GPR20, selectively expressed in gastrointestinal stromal tumorswith DS-6157a, a first-in-class antibody-drug conjugate. Cancer Discov 11(6):1508-1523. doi: 10.1158/2159-8290.Cd-20-1434

Objective: Introduce DS-6157a, an anti-GPR20 antibody-drug therapeutic for gastrointestinal stromal tumors (GIST).

Summary: The only approved treatments for GIST are currently tyrosine kinase inhibitors (TKI) which can be problematic. They lead to secondary resistance mutations in KIT or PDGFRA and disease progression. The authors identified G protein-coupled receptor 20 (GPR20) as a non-tyrosine kinase target and assessed its expression in cell lines, xenografts, and clinical samples. Preclinical pharmacokinetics and safety profile support its development as a novel GIST therapy.

Usage: Internalization activity of anti-GPR20 mAbs were evaluated by using Rat-ZAP. GPR20-expressing 293T cells were plated at 2500 cells/well in 96-well plates. Cells were treated with dilutions of various anti-GPR20 and 500 ng/ml of Rat-ZAP for 3 days. The percentage of living cells were measured using a CellTiter-Glo Luminescent Cell Viability Assay.

Related Products: Rat-ZAP (Cat. #IT-26)

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