Article
Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
Journal of medicinal chemistry - 25 Jan 2024
Visser Michael, Papillon Julien P N, Luzzio Michael, LaMarche Matthew J, Fan Jianmei, Michael Walter, Wang David, Zhang Alan, Straub Christopher, Mathieu Simon, Kato Mitsunori, Palermo Mark, Chen Christine, Ramsey Timothy, Joud Carol, Barrett Rosemary, Vattay Anthony, Guo Ribo, Bric Anka, Chung Franklin, Liang Guiqing, Romanowski Michael J, Lam Joni, Thohan Sanjeev, Atassi Faraj, Wylie Andrew, Cooke Vesselina G
Abstract excerpt
Uveal melanoma (UM) is the most common primary intraocular malignancy in the adult eye. Despite the aggressive local management of primary UM, the development of metastases is common with no effective treatment options for metastatic disease. Genetic analysis of UM samples reveals the presence of mutually exclusive activating mutations in the Gq alpha subunits GNAQ and GNA11. One of the key downstream targets of...
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