{Reference Type}: Journal Article
{Title}: Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery.
{Author}: Xi JY;Zhang RY;Chen K;Yao L;Li MQ;Jiang R;Li XY;Fan L;
{Journal}: Bioorg Chem
{Volume}: 125
{Issue}: 0
{Year}: 08 2022
{Factor}: 5.307
{DOI}: 10.1016/j.bioorg.2022.105848
{Abstract}: 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.