%0 Journal Article
%T Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery.
%A Xi JY
%A Zhang RY
%A Chen K
%A Yao L
%A Li MQ
%A Jiang R
%A Li XY
%A Fan L
%J Bioorg Chem
%V 125
%N 0
%D 08 2022
%M 35533582
%F 5.307
%R 10.1016/j.bioorg.2022.105848
%X Proteolysis-targeting chimeras (PROTACs), bifunctional molecules consisting of a ligand of protein of interest (POI), an E3 ligase ligand and a linker, have been developed to hijack the ubiquitin-proteasome system (UPS) to induce different POIs degradation. Currently, the first oral PROTACs (ARV-110 and ARV-471) have shown encouraging efficacy in clinical trials of prostate and breast cancer treatment, which turns a new avenue for the development of PROTAC research. In this review, we focus on a detailed summary of the latest progress of PROTACs and elucidate the advantages of PROTACs technology. In addition, potential challenges and perspectives of PRTOACs are discussed.