PROTACs (PROteolysis TArgeting Chimeras) are bifunctional molecules capable of degrading disease-causing proteins by inducing selective intracellular proteolysis. These small molecules simultaneously engage a target protein and an E3-ubiquitin ligase, thus causing selective ubiquitination and degradation of the target protein by the proteasome.
Autophagy and Ubiquitin
Recently PROTAC technology has emerged a novel method to address diseases driven by the aberrant expression of a disease-causing protein and has been applied by a number of drug discovery programs to various E3 ligases, including pVHL, MDM2, beta-TrCP1, cereblon, and c-IAP1. PROTAC technology has been described in the following figure.
LifeSensors has a number of commercially available PROTAC compounds as well as several PROTAC components designed for use as building blocks to help PROTAC research and development. Moreover, LifeSensors has intensive experience and expertise to test the ubiquitylation of your target proteins in both in vitro and in cellular context. Our ubiquitylation (E3LITE, UbiQuant S ELISA, UbiTEST) assays are specifically designed to quickly demonstrate the effect of PROTACs on their target proteins. Ranging in throughput from immunoblot to 384-well formats, our assay concepts can be readily adapted for a vast range of applications on a custom basis. Thus, our technologies will enable the advancement of your PROTACs from in vitro lead to in vivo and preclinical models.