Chemistry:LGK974
From HandWiki
LGK974 (WNT974) is an experimental drug which acts as an inhibitor of the porcupine O-acyltransferase enzyme, which plays an important part in the growth of certain types of cancer, especially colorectal cancer, pancreatic cancer, hepatocellular carcinoma and head and neck cancers. It is in early stage clinical trials for a number of cancer types.[1][2][3]
LGK974 has recently shown promise in preclinical models of the ultra-rare disease sclerosteosis, providing an alternative to invasive surgeries commonly required to the management of pathologies.[4]
References
- ↑ "Chemical Modulation of WNT Signaling in Cancer". Progress in Molecular Biology and Translational Science 153: 245–269. January 2018. doi:10.1016/bs.pmbts.2017.11.008. ISBN 978-0-12-811429-2. PMID 29389519.
- ↑ "Porcupine inhibitors: Novel and emerging anti-cancer therapeutics targeting the Wnt signaling pathway". Pharmacological Research 167. May 2021. doi:10.1016/j.phrs.2021.105532. PMID 33677106.
- ↑ "Recent updates on Wnt signaling modulators: a patent review (2014-2020)". Expert Opinion on Therapeutic Patents 31 (11): 1009–1043. November 2021. doi:10.1080/13543776.2021.1940138. PMID 34128760.
- ↑ "Porcupine inhibition is a promising pharmacological treatment for severe sclerosteosis pathologies". Bone Research 13 (1). April 2025. doi:10.1038/s41413-025-00406-3. PMID 40189599.
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