期刊
JOURNAL OF BIOLOGICAL CHEMISTRY
卷 296, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.jbc.2021.100647
关键词
-
资金
- Howard Hughes Medical Institute Gilliam Fellowship
Targeted protein degradation (TPD) is an innovative therapeutic approach that completely removes protein molecules using protein degradation pathways, expanding the druggable space beyond small-molecule inhibitors.
Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates complete removal of the protein molecules from within or outside the cell. While the pioneering Proteolysis-Targeting Chimera (PROTAC) technology and molecular glues hijack the ubiquitin-proteasome system, newer modalities co-opt autophagy or the endo-lysosomal pathway. Using this mechanism, TPD is posited to largely expand the druggable space far beyond small-molecule inhibitors. In this review, we discuss the major advances in TPD, highlight our current understanding, and explore outstanding questions in the field.
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