New York Chronicle

New York, April 17, 2019—One of the world’s leading chemical vendors BOC Sciences announces to launch the Targeted Protein Degradation Platform in response to addressing customers’ concerns in finding a cure for difficult diseases.

Mediated by small molecule degraders, targeted protein degradation represents an exciting new therapeutic opportunity to eliminate disease-causing proteins through the use of hetero-bifunctional small molecule “degraders” (e.g. PROTACs™). The new modality promises to open up the human proteome to drug developers, but before that they will need to work out the rules behind.

“The idea is quite simple,” says Prof. Jones, a senior scientist from BOC Sciences. “Researchers want to develop protein degraders that can break into ubiquitin-proteasome machinery to change the destiny of disease-causing proteins. Aiming at this, they design small molecules with two active ends: one that binds to the protein of interest and the other that binds to a protein called E3 ubiquitin ligase. These bifunctional molecules force a handshake between the ubiquitin and the protein, sending it to the trash. They will keep on to repeat the same process, and as a result, quickly depleting levels of the unwanted protein.”

Ever since the initial design of proteolysis-targeting chimera (PROTAC) by Sakamoto et al. in 2001, this technology has been successfully applied in the development of hetero-bifunctional molecules that work to prompt target protein degradation. By directly removing target proteins instead of blocking them, protein degraders act kind of like an enzyme or catalyst, showing multiple advantages over small molecule inhibitor drugs. While traditional drugs may only allow access to about 20% of the proteome, TPD techniques may open the door to the other 80%. And for reasons still being explored, they upend conventional wisdom about drug potency and selectivity.

“Another advantage of peptide modulators over small-molecule drugs is that peptide modulators could significantly facilitate the modification of drugs and target protein−protein interactions, which can hardly be done by small molecules,” further adds Prof. Jones. “However, while PROTAC technology has been a rising star in drug development in recent years, this technique is still facing some issues like toxicity, stability, pharmacokinetics or bioavailability. BOC Sciences will continue to investigate more on this technique, together with folks in the industry. We believe by overcoming these limitations, PROTACs could be eventually developed as a novel class of drugs for the treatment of human diseases.”

To support TPD research and development, BOC Sciences provides a wide range of protein degraders (PROTAC molecules) targeting various protein targets, along with degrader building blocks, linkers and peptides. To know more about these chemicals, please visit https://www.bocsci.com/targeted-protein-degradation-platform-protacs.html or email at [email protected].

About BOC Sciences

Starting from 2007 as a small chemical provider for industry and academia, BOC Sciences never ceases its step of moving forward. Its business range has expanded to custom and GMP development and manufacturing of bioactive chemicals, peptides as well as catalog products. In addition to offering a broad range of high quality chemicals like inhibitors, ADC linkers, impurities, APIs, metabolites, BOC Sciences also focuses on an integrated service related to drug discovery, R&D, hoping to assist scientists and researchers in addressing the now major disease threats facing humankind like cancer, Alzheimer’s. Therefore, a comprehensive laboratory services such as nucleoside synthesis, isotope labeling, virtual screening, x-ray crystallography, bioconjugation, chiral synthesis, etc. are offered as well.

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Website: https://www.bocsci.com