LGK974 inhibits PORCN

Stable Identifier
Homo sapiens
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Aberrant WNT signaling is associated with the development of numerous cancers, and strategies for targeting this pathway are under intense investigation (reviewed in Polakis, 2012; Polakis, 2000; Yao et al, 2011). Secretion of WNT ligand depends on its PORCN-dependent palmitoleoylation in the ER, making PORCN a attractive therapeutic target in cases where WNT is aberrantly over-expressed (reviewed in MacDonald et al, 2009). LGK974 is a PORCN-inhibitor that was identified in a screen for compounds that abrogate the secretion of WNT ligands, and is in Phase I clinical trials for the treatment of WNT-dependent cancers (Liu et al, 2013)
Literature References
PubMed ID Title Journal Year
22438566 Wnt signaling in cancer

Polakis, P

Cold Spring Harb Perspect Biol 2012
24277854 Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974

Li, C, Li, AG, Kowal, C, Kasibhatla, S, Harris, JL, Pferdekamper, A, Petruzzelli, L, McNamara, P, Wang, T, Sellers, WR, Carey, TE, Steffy, A, Liu, J, Brenner, JC, Hsieh, MH, Boral, AL, Pan, S, Seidel, HM, Schultz, PG, Ng, N, McLaughlin, ME, Schuller, AG, Li, J, Wang, Y, Phung, V, Wu, X, Guo, G, Villarroel, MC, Graham, MP, Vanasse, G, Flynn, S, Cheng, J, Tompkins, C, Sun, F, Cheng, D, Che, J

Proc. Natl. Acad. Sci. U.S.A. 2013
10921899 Wnt signaling and cancer

Polakis, P

Genes Dev. 2000
21486121 Targeting the Wnt/?-catenin signaling pathway in human cancers

Ashihara, E, Maekawa, T, Yao, H

Expert Opin. Ther. Targets 2011
19619488 Wnt/beta-catenin signaling: components, mechanisms, and diseases

MacDonald, BT, Tamai, K, He, X

Dev Cell 2009
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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