中国药科大学学报2025，Vol.56Issue(2)：252-263,12.DOI:10.11665/j.issn.1000-5048.2024031301
小分子疏水标签蛋白降解剂的研究进展
Research advances in small-molecule hydrophobic tagging protein degraders
摘要
Abstract
In In recent years,small-molecule targeted protein degraders inducing protein degradation have been developing rapidly.These molecules are attracting substantial interest from researchers since they can overcome such limitations of traditional small-molecule inhibitors as their inapplicability to'undruggable'targets and tendency to induce drug resistance.Compared with other targeted protein degraders,small-molecule hydrophobic tags(HyTs)may have a smaller number of hydrogen bond donors/acceptors,smaller molecular weights,and better pharmacokinetic profiles,thus attracting extensive attention from researchers.This review focuses on the possible mechanisms and popular types of HyTs,with special attention to the potential application value of adamantane,a typical hydrophobic tag,in the fields of cancer and neurodegeneration.In general,there are still some problems like fewer types of hydrophobic tags and insufficient research on degradation mechanisms,which still need to be further explored.This review is expected to provide researchers working in the fields of small-molecule targeted protein degraders with some valuable reference.关键词
疏水标签/靶蛋白降解/金刚烷/癌症Key words
hydrophobic tag/targeted protein degradation/adamantane/cancer分类
医药卫生引用本文复制引用
霍子瑞,裴捷雨,詹芳怡,谢绍文,徐进宜,徐盛涛..小分子疏水标签蛋白降解剂的研究进展[J].中国药科大学学报,2025,56(2):252-263,12.基金项目
This study was supported by the National Natural Science Foundation of China(No.82173672,No.82373743) （No.82173672,No.82373743）
and the National Innovation and Entrepreneurship Training Program for Undergraduate(202410316057Y) 国家自然科学基金项目(No.82173672,No.82373743) （202410316057Y）
2024年中国药科大学大学生创新创业训练计划项目(202410316057Y) （202410316057Y）
