Breaking down KRAS: small-molecule degraders for cancer therapy

IF 40.8 1区医学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY

Signal Transduction and Targeted Therapy Pub Date : 2025-03-14 DOI:10.1038/s41392-025-02172-4

Tina Kos, Dieter Saur

引用次数: 0

Abstract

In their recently published study in Science, Popow and colleagues developed a proteolysis-targeting chimera (PROTAC) for the in vivo degradation of several oncogenic KRAS variants.¹ Leveraging detailed biophysical analyses and crystal structures of ternary complexes of candidate ligands for KRAS and the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex, they designed a small molecule capable of potently and selectively targeting 13 of the 17 most common KRAS mutants.

Abstract Image

查看原文本刊更多论文

求助全文

约1分钟内获得全文求助全文

来源期刊

Signal Transduction and Targeted Therapy Biochemistry, Genetics and Molecular Biology-Genetics

CiteScore

44.50

自引率

1.50%

发文量

384

审稿时长

5 weeks

期刊介绍： Signal Transduction and Targeted Therapy is an open access journal that focuses on timely publication of cutting-edge discoveries and advancements in basic science and clinical research related to signal transduction and targeted therapy. Scope: The journal covers research on major human diseases, including, but not limited to: Cancer,Cardiovascular diseases,Autoimmune diseases,Nervous system diseases.