LGK974抑制PORCN
中文名称
通路描述
异常WNT信号传导与多种癌症的发生发展相关，针对该通路的策略正受到 intense 调查（综述于Polakis, 2012; Polakis, 2000; Yao et al, 2011）。WNT配体的分泌依赖于其在ER中的PORCN依赖性棕榈酰化，因此当WNT异常高表达时，PORCN是一个有吸引力的治疗靶点（综述于MacDonald et al, 2009）。LGK974是一种PORCN抑制剂，在筛选能阻断WNT配体分泌的化合物时被鉴定，目前正在I期临床试验中用于治疗WNT依赖性癌症（Liu et al, 2013）
英文描述
LGK974 inhibits PORCN 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)
所含基因
1 个基因