As a service leader in the field of drug discovery and development, Creative Biolabs now offers proprietary one-stop PROTAC® service platform to clients from scratch to full development. To monitor the affinity and specificity of PROTAC®s with target proteins or specific E3 ligases, we provide a comprehensive set of various binary target engagement assays to promote your drug discovery progression.
PROTAC®s are heterobifunctional compounds which are able to bind both a target protein and a specific E3 ligase simultaneously, via two separate heads, to remove a particular protein by the proteasome-mediated degradation mechanism. Therefore, the affinity and specificity of PROTAC®s with target protein and E3 ligase is regarded as fundamental cornerstone of PROTAC® efficiency. To enhance the PROTAC® efficiency and furthest avoid "off-target effects", it's ideally that the PROTAC® candidate can exhibit high affinity and specificity profiles.
To date, the design and optimization of PROTAC®s are largely guided by the binary target engagement between target protein/E3 ligase and respective warheads of the PROTAC®s. This is driven by the general recognition that improved binary affinity does more likely translate to improved degradation of target proteins. To evaluate the binding affinity and specificity of binary target engagement, Creative Biolabs has explored comprehensive assays to fulfill different requirements of our clients. The interactions that occur between two reactants, as well as the degree of affinity for which the reactants bind together, such as IC50, Kd can be measured to predict weak, strong, or no binding. The available assays including but not limited to:
Creative Biolabs provides label-free ligand binding assays including fluorescence polarization (FP), fluorescence resonance energy transfer (FRET), and surface plasmon resonance (SPR), shown in Fig.1.
Creative Biolabs offers structure-based ligand binding assays including nuclear magnetic resonance (NMR) and X-ray crystallography.
Creative Biolabs is capable of thermodynamic binding assays including isothermal titration calorimetry (ITC) and thermal denaturation assays (TDA).
Creative Biolabs provides whole cell ligand-binding assays such as surface acoustic wave (SAW) biosensor and RWG biosensor.
Fig.1 Schematic of FRET, ITC, and SPR.
Highlight Features of Our Services
Experienced in drug discovery area and with dedicated commitment to a healthier world, Creative Biolabs has perfected our technical pipelines in the in vitro PROTAC® evaluation assays such as binary target engagement. We aim to be your best companion for PROTAC® service. We are always here to provide the best service for you. Please contact us for more information.
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