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Targeted protein degradation for drug discovery

30th July 2019


 

AMS Bio has introduced a new range of homogeneous proximity assays, critical enzymes and small molecule inhibitors to assess the chemical adaptor function of Proteolysis Targeting Chimeras (PROTACs).

Targeted protein degradation using PROTACs is a new and promising therapeutic method in drug discovery. PROTACs have the ability to regulate protein degradation through targeted control of ubiquitin E3 ligases. This novel technology allows for the degradation of disease-related proteins and offers many advantages over traditional protein inhibition.

The PROTAC method offers many advantages compared to traditional protein inhibition. Inhibitors require sustained protein binding to evoke the intended biological reaction. This can be problematic in the incidence of target overexpression, the presence of competing ligands, or protein mutations that lead to binding resistance. The PROTAC model bypasses these issues by promoting degradation that circumvents the native resistance of proteins against sustained inhibition.

Even select weak binding and promiscuous ligands can be used with PROTACs and still demonstrate high degradation efficacy. Also, ineffectual ligands which do not modulate the cellular functions of the protein of interest can be used to mediate degradation through PROTACs. Whether the ligand is a strong inhibitor, a weak binder, promiscuous, or ineffectual, PROTACs offer the ability to degrade proteins previously believed to be 'undruggable' through conventional small molecule inhibition.





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