Heterobifunctional proteomimetic polymers for targeted degradation of MYC and KRAS.

用于靶向降解 MYC 和 KRAS 的异双功能蛋白质模拟聚合物。

阅读:3
作者:
Targeted protein degradation (TPD) has enabled modulation of previously undruggable proteins. However, existing small-molecule approaches require arduous optimization and are largely confined to targets bearing ligandable pockets. To address these challenges, we introduce the HYbrid DegRAding Copolymer (HYDRAC), a polymeric platform that integrates target‑binding peptides with peptide-based or small‑molecule degrons to orchestrate selective degradation of disease‑relevant proteins. HYDRACs are amenable to scalable synthetic methods, exhibit broad structural tunability, and support multivalent payload conjugation. This intrinsic modularity enables incorporation of a diverse repertoire of target‑binding motifs and E3‑ligase recruiters. These include von Hippel-Lindau protein (VHL), Kelch-like ECH-associated protein 1 (KEAP1), and Cereblon (CRBN). We deploy HYDRACs against two historically intractable targets, Myelocytomatosis proto-oncogene (MYC) and Kirsten rat sarcoma viral oncogene homolog (KRAS), achieving potent degradation in vitro and durable tumor suppression in murine models. Notably, HYDRACs bearing consensus RAS-binding motifs effectuate degradation of KRAS across multiple alleles, suggesting pan‑KRAS potential. We envision HYDRACs as a generalizable paradigm that substantially expands the TPD armamentarium.

特别声明

1、本页面内容包含部分的内容是基于公开信息的合理引用;引用内容仅为补充信息,不代表本站立场。

2、若认为本页面引用内容涉及侵权,请及时与本站联系,我们将第一时间处理。

3、其他媒体/个人如需使用本页面原创内容,需注明“来源:[生知库]”并获得授权;使用引用内容的,需自行联系原作者获得许可。

4、投稿及合作请联系:info@biocloudy.com。