Creative Biolabs releases novel platforms associated with proteolysis-targeting chimeras (PROTAC) technology, which are helpful to design and develop PROTAC molecules with designated properties efficiently.
PROTAC technology, and is proud to announce its improved platforms capable of developing PROTAC molecules with desired properties.— Compared with conventional drugs which work predominantly on the regulation of protein or enzyme activities to treat diseases, proteolysis targeting chimera is a novel approach that takes advantage of the ubiquitin-proteasome system to clear disease-causing oncogenic proteins from cells, a booming technology gaining more and more market share since its birth in 2001. Creative Biolabs gathered a group of doctoral-level scientists who focus their energy on excavating solutions regarding
The featured in-cell click-formed proteolysis-targeting chimera (CLIPTAC) platform contributes to obtaining CRBN-based and VHL-based CLIPTACs that have a polar surface of the separate reaction partners, lower molecular weight, and better cell permeability. By click chemistry after sequential administration of the precursors (made up of E3 ubiquitin ligase and the binding domain for the target molecule separately on 2 molecules), the functional molecules are obtained.
Creative Biolabs can assist with developing VHL-based Homo-PROTAC, CRBN-based Homo-PROTAC, and VHL-CRBN heterodimeric PROTAC, groups of small molecules which can dimerize an E3 ligase to trigger its suicide-type chemical knockdown inside cells, which therefore provide new approaches of drugging E3 ligases, more effective than E3 ligase inhibition.
One of the platforms is specialized in developing HaloPROTAC with better drug-like properties. It utilizes the HaloTag protein to stimulate the degradation of cytosolic, endosomal and nuclear-localized proteins. The process starts from the combination of HaloPROTACs and HaloTag fusion protein, which then recruits the designated E3 ligase to induce degradation thereafter. VHL-based and cIAP-based HaloPROTACs are developed and more can be customized according to specific requirements, based upon the HaloPROTAC platform.
Another exceptional ATTEC platform makes it possible to generate PROTAC molecules using autophagosome-tethering compound as a linker, which interacts with both the disease-causing protein and phagophore protein LC3, therefore opening a new path to drug discovery focused on Huntington disease (HD).
Those platforms are valuable supplements to the available comprehensive PROTAC discovery solutions starting from molecule design, followed by screening, optimization, synthesis, and ended up with in vitro/in vivo tests, to meet with various research purposes. For more details, please refer to https://www.creative-biolabs.com/protac/.
Creative Biolabs, set up in 2004 in New York, has a specialized team of scientific researchers who are devoted to the research & discovery of novel drugs and therapeutics. After years of dedicated exploration in the area of proteolysis targeting chimera as a novel target therapy, Creative Biolabs is confident to provide technical support covering the entire pipeline of PROTAC-based drug development from early discovery to pre-clinical evaluation and clinical trials.
Release ID: 88964138