New York, USA – March 9, 2021 – Drug-resistance continues being a predominant and unavoidable issue in clinical medicine, worsened by the limited number of drug targets whose current explorations are focused on the enzymatic functions, not the protein scaffolds. Proteolysis targeting chimeras (PROTACs) draw scientists’ attention and seem to be a promising solution to the hereto issue.
Compared with other small molecule inhibitors, PROTAC reduces on-target toxicity at a smaller dose. It significantly promotes the development of targeted small molecule drugs to some degrees since most proteins are non-druggable. In response to the PROTAC research, Creative Biolabs forms a group of experts to deliver PROTACs development services, including custom peptide and compound synthesis.
Introduction to PROTAC and Its Mechanism of Action
Literally, PROTAC is a bifunctional molecule composed of three parts: one end is the ligand for recognizing target protein, and the other end is the ligand for E3 ligase, and a linker connecting the two ligands.
PROTAC binds to the target protein and attracts it to approach the E3 ligase for ubiquitination labeling, ending with protein degradation via the proteasome pathway.
Creative Biolabs Promotes PROTAC Development by Synthesis and Modification
The PROTAC technology is based on the Ubiquitin-Proteasome System (UPS) in mammalian cells to degrade proteins. As long as there are suitable ligands for the protein of interest (POI) and related E3 ligases, PROTAC can make the undruggable target proteins druggable.
Thus, promoting the therapeutic effect of proteins could be accomplished by peptide or compound synthesis, and PROTAC structural modification. Scientists at Creative Biolabs focus on therapeutic ligands to optimize the performance of PROTAC and novel synthesized PROTAC.
Creative Biolabs synthesizes small peptides with a current well-received FMOC solid-phase technology and purifies the related products, such as linkers, ligands, E3 ligase, and target proteins, by the HPLC technique. Moreover, to optimize molecules’ stability, biodistribution, and cellular permeability in vivo, experts design and modify molecules from aspects of hydrogen bonding, polar surface area, lipophilicity, molecular weight, reactivity, and pKa to expand the internal compound library.
Comprehensive Custom Options at Creative Biolabs for PROTAC Research
Creative Biolabs also involves in PROTAC based drug development services for specific requirements. It is making efforts to design custom packages for scientists, from early discovery to pre-clinical evaluation and clinical trials, returning various modifications and purity levels, synthesis platforms, formats, etc.
Solutions include but are not limited to:
* PROTAC molecule discovery
* PROTAC in vitro evaluation
* PROTAC in vivo animal test
At a competitive price, Creative Biolabs’ solutions are featured with reproducibility and consistency. Discover more customized services and products at https://www.creative-biolabs.com/protac.
About Creative Biolabs
Creative Biolabs has been committed to drug discovery for decades. The outstanding research team and optimal technology render Creative Biolabs one of the most eminent companies that contribute to PROTAC exploration and launch worldwide satisfying services and products.