Mesh : Humans Smoothened Receptor / antagonists & inhibitors metabolism Drug Resistance, Neoplasm / drug effects Cholesterol / metabolism chemistry Diterpenes / pharmacology chemistry Hedgehog Proteins / metabolism antagonists & inhibitors Neoplasms / drug therapy metabolism pathology Animals Receptors, G-Protein-Coupled / metabolism antagonists & inhibitors Antineoplastic Agents / pharmacology chemistry Signal Transduction / drug effects

来  源:   DOI:10.1016/j.chembiol.2024.06.005

Abstract:
In this issue of Cell Chemical Biology, Liu et al.1 report the identification of Q29, a synthetic diterpenoid that blocks covalent cholesterol modification of smoothened (SMO) and inhibits hedgehog signaling. Q29 is capable of suppressing tumor cell growth, both in vitro and in vivo, and overcoming resistance to SMO inhibitors.
摘要:
在本期《细胞化学生物学》中,Liu等人1报道了Q29的鉴定,Q29是一种合成的二萜,可阻断平滑(SMO)的共价胆固醇修饰并抑制刺猬信号传导。Q29能够抑制肿瘤细胞生长,在体外和体内,克服对SMO抑制剂的抗性。
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