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Ref Type Journal Article
PMID (27401612)
Authors Jackson H, Granger D, Jones G, Anderson L, Friel S, Rycroft D, Fieles W, Tunstead J, Steward M, Wattam T, Walker A, Griggs J, Al-Hajj M, Shelton C
Title Novel Bispecific Domain Antibody to LRP6 Inhibits Wnt and R-spondin Ligand-Induced Wnt Signaling and Tumor Growth.
Journal Vol Issue Date Pages Journal Short Title
Molecular cancer research : MCR 14 9 2016 Sep 859-68 Mol Cancer Res
URL
Abstract Text Aberrant WNT signaling is associated with the formation and growth of numerous human cancer types. The low-density lipoprotein receptor-related protein 6 (LRP6) is the least redundant component of the WNT receptor complex with two independent WNT ligand-binding sites. Using domain antibody (dAb) technology, a bispecific antibody (GSK3178022) to LRP6 was identified that is capable of blocking stimulation in the presence of a range of WNT and R-spondin (RSPO) ligands in vitro GSK3178022 was also efficacious in reducing WNT target gene expression in vivo, in both cancer cell line and patient-derived xenograft models, and delays tumor growth in a patient-derived RSPO fusion model of colorectal cancer.This article demonstrates the inhibition of a key oncogenic receptor, intractable to mAb inhibition due to multiple independent ligand interaction sites, using an innovative dAb approach. Mol Cancer Res; 14(9); 859-68. ©2016 AACR.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
GSK3178022 GSK3178022 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
GSK3178022 WNT Inhibitor 15 GSK3178022 is an antibody that targets LRP6 and blocks both Wnt binding domains, resulting in decreased Wnt-mediated signaling and potentially leading to decreased tumor growth (PMID: 27401612).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References