BPS Bioscience is a leading product manufacturer and service provider in the PROTAC space. Using our services, we can design and conduct homogeneous proximity assays to assess the chemical adaptor function of PROTACs.

BPS Bioscience has designed many assays to measure and study

• Cereblon Binding

• Cereblon Ubiquitination

• PROTAC Optimization for BET Bromodomain-Cereblon Binding

• PROTAC Optimization for BET Bromodomain-Von Hippel Lindau (VHL) Binding

• PROTAC Optimization for CDK Kinase-Cereblon Binding

In addition to our existing assay portfolio, we have the capabilities to develop custom PROTAC and Protein Degradation assays specialized for your project details. Please contact us to learn more.

Example Assay

The PROTAC Optimization Assay for BET Bromodomain-Cereblon Binding is designed for testing and profiling of PROTACs directed against BET Bromodomain family and Cereblon complex. Cereblon (CRBN) is a Substrate recognition component of a DCX (DDB1-CUL44-Rbx1 ) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins.

With this assay, only three simple steps on a microtiter plate are required for PROTAC activity detection. First, a sample containing PROTAC is incubated with CRBN and BRD3(BD2), one of BET bromodomains. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.

Inhibition by (+)-JQ1 (BPS Bioscience #27401) or Pomalidomide of dBET1-mediated interaction of Cereblon with BRD3(BD2), measured using the PROTAC Optimization Kit for BET Bromodomain Cereblon Binding, BPS Bioscience #79770.

PROTACs ^®

Targeted protein degradation using Proteolysis Targeting Chimeras, or PROTAC , 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.

PROTACs function by hijacking the final action of E3 ligases and subsequently tagging the protein of interest for ubiquitination. A PROTAC is composed of three parts; an E3 ligａnd that binds to an E3 ligase, a ligａnd that binds to the protein of interest, and a linker connecting the two ligands. When each ligａnd binds its respective partner, it triggers ubiquitination of the protein of interest. The PROTAC itself is not degraded by this process, making PROTACs a valuable tool for mediating protein degradation. A single PROTAC can promote the degradation of many subsequent proteins and functions substoichiometrically.

Advantages

• Promotes degradation that circumvents the native resistance of proteins against sustained inhibition

• Select weak binding and promiscuous ligands can be utilized with PROTACs and still demonstrate high degradation efficacy

• Ineffectual ligands which do not modulate the cellular functions of the protein of interest can be used to mediate degradation through PROTACs

• PROTACs could have the ability to degrade proteins previously believed to be 'undruggable' through conventional small molecule inhibition

PROTAC ^® is a registered trademark of Arvinas Operations Inc., and is used under license

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