New York, USA – May 14, 2021 – The occurrence of tumors is closely related to the expression of tumor-specific oncoproteins. One novel approach to eliminate cancer cells is to degrade oncoproteins. The ubiquitin-dependent proteolysis system (UPS) controls most of the selective protein degradation in all eukaryotic cells. PROTACs-induced targeted protein degradation has emerged as a novel therapeutic strategy in drug development and attracted the favor of academic institutions and biotechnology companies (e.g., Creative Biolabs).
A typical PROTAC contains three elements. One of the elements binds to a given ubiquitin ligase and another one functions as the ligand to recognize target protein. These two elements are connected by a flexible linker. It has become increasingly clear that the length and composition of the linker play critical roles on the physicochemical properties and bioactivity of PROTACs.
“Linker optimization in each series is required as the optimal linker is an important prerequisite for target proteins to develop specific drugs,” said a scientist at Creative Biolabs. “While adhering to the highest standards and meeting the needs of customers, we ensure that the length and location of the linker can be optimized to maximize the interaction between the target protein and the E3 ligase, so as to achieve the effective ubiquitination of the target protein and its ultimate degradation.”
A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently linked ligand of an E3 ubiquitin ligase (E3). Upon binding to the POI, the PROTAC can recruit E3 for POI ubiquitination, which is subjected to proteasome-mediated degradation. Since ubiquitination tags guide the degradation caused by proteasomes which are hijacked by PROTAC to promote the degradation of POIs, it is important to rationally choose and design the recruiting moiety.
As a novel and powerful strategy, PROTACs have attracted great attention for discovering new types of therapeutic agents relying on their unique characteristic of degrading target proteins instead of inhibiting them. Since PROTACs act catalytically, the scope of proteins used for treating diseases has been expanded by PROTACs.
To explore more effective potential of PROTAC technology, Creative Biolabs offers PROTAC based drug development services for specific needs, covering all aspects of small molecule discovery, from screening to optimization. It also provides a complete set of in vitro evaluation assays for compounds to validate the efficacy of PROTACs in preclinical drug development. Explore more at https://www.creative-biolabs.com/protac.
About Creative Biolabs
Creative Biolabs, a leading product manufacturer and service provider in the field of PROTAC, has been supporting drug discovery research for more than ten years. Driven by a passionate group of biological innovators, Creative Biolabs is committed to providing global customers with the largest and most diverse portfolio of standard and customized in vitro evaluation assays for PROTAC screening and profiling.