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To develop an ideal PROTAC molecule with huge potential to treat diseases, the specificity and affinity of ligands for target disease-causing proteins are very important. Empowered by our experienced scientists and advanced drug discovery platform, Creative Biolabs is fully competent and dedicated to providing various ligands for target proteins of interest or ligand design service to meet the drug discovery goals of our clients.
A wide range of therapeutic targets has been identified in the human proteome for malignant tumors and other diseases. While a majority of these targets can't be curative by current existing small molecules that inhibit the functions of these proteins. Herein, a novel therapeutic approach to target these “undruggable” proteins is inevitable. In the meantime, high drug dosages and continuous exposure to small molecule inhibitors may inadvertently result in off-target effects. To target a wider range of proteins with high specificity and affinity, PROTAC is emerging as a promising technique in the development of therapeutics. For PROTAC design and development, identifying a specific ligand is very important to determine the specificity of the PROTAC molecule.
With huge advantages, PROTAC can be broadly applicable to a variety of target classes (see Fig.1). In addition, PROTAC is capable of offering greater degradation selectivity compared with binding selectivity derived from the target ligand used, this means even the ligand candidate is weak binding to the target protein, it still can drive robust degradation. Creative Biolabs is committed to providing the following services including but not limited to:
Fig.1 Selected bifunctional molecules hijacking the VHL E3 ligase to degrade various target proteins. (Collins, 2017)
Here is a simple list of ideal targets for PROTAC technology for your reference.
Fig.2 PROTAC-mediated protein degradation.
As a leader in therapeutic small molecule discovery and development, Creative Biolabs is dedicated to exploring novel small molecules to promote the field of drug discovery. Using the advanced ligand design platform, we are confident in presenting a comprehensive set of services to develop an ideal PROTAC for worldwide clients. Please feel free to contact us with any questions.