Selpercatinib：首个获批的选择性 RET 抑制剂。
Selpercatinib: First approved selective RET inhibitor.
发表日期：2023 Apr 13
作者：
Larissa C B Oliveira, Lois M Mulligan
来源：
CELL
摘要：
Selpercatinib是一种小分子，可以与RET激酶活性位点结合。它抑制恒定二聚化的RET融合蛋白和激活的点突变体的活性，从而阻断促增殖和促存活的下游信号。它是FDA批准的第一种选择性RET抑制剂，用于针对癌性RET融合蛋白的肿瘤无关靶向。要查看这个概念的 实践和理论相结合,请打开或下载PDF。版权所有©2023 Elsevier Inc。
Selpercatinib is a small molecule that binds at the RET kinase active site. It inhibits activity of constitutively dimerized RET fusion proteins and activated point mutants, thereby blocking downstream signals for proliferation and survival. It is the first selective RET inhibitor to be FDA approved for tumor agnostic targeting of oncogenic RET fusion proteins. To view this Bench to Bedside, open or download the PDF.Copyright © 2023 Elsevier Inc. All rights reserved.