Today George prepared a new topic to discover for you – “Clinical considerations for the design of PROTACs in cancer”!

Please also check out our PROTACs compound sets!

Chemspace offers Anchors and Linkers libraries, as well as a separate service of designing a custom anchor library for your protein of interest!  

Degradation of target proteins using proteolysis targeting chimera (PROTACs) has gained momentum. These agents demonstrate strong potency compared to the corresponding small molecule inhibitors. Some of them were already clinically tested against the estrogen and androgen receptors in prostate cancer.   

The selection of the right target protein is crucial for this type of research, because exhaustion of certain genes may affect cell viability in oncogenic and non-transformed tissues. To prevent this, the developed cancer therapies usually focus on the selected ligase enzymes expressed only in tumor cells.  

In this article, the authors review the development stage of PROTACs and explore if targeting only the ligase of the tumor cells can reduce toxicity in healthy tissue. Here is the full information.