New York, USA – September 18, 2020 – The entire pharmaceutical industry is working on novel therapeutics that could improve human health with precision medicine. Proteolysis targeting chimeric (PROTAC) drug is a kind of target therapy that obtained full focus in recent years. Compared with conventional drugs, PROTAC molecule can degrade the disease-causing proteins selectively by using the proteasome-mediated proteolysis via E3 ligase, which is less toxic with lower dosage required, meanwhile targeting the undruggable proteins to achieve a better effect. Creative Biolabs is a professional solution provider regarding this novel drug discovery method, offering one-stop services of PROTAC molecule discovery.
PROTAC molecule discovery initiates with ligand design for the protein of interest, which is also the prerequisite to determine the specificity and affinity of the molecule. Clients can choose from the available ligand products (target ligand, E3 ligase ligand, ligand-linker conjugate, and PROTAC molecule), or designate target proteins for ligand design, which can be cytosolic, nuclear receptors and trans-membrane targets. Creative Biolabs can help develop ligand for transcription factors, non-enzymatic proteins, scaffold proteins, kinases, receptors, or bromodomains required with the synthesis solutions.
Ligands for E3 ligase shape the selectivity for target proteins and the efficacy of target protein degradation. Creative Biolabs offers ligand screening services for E3 ubiquitin ligases (Von Hippel-Lindau disease tumor suppressor protein (VHL), the Mouse Double Minute 2 homologue (MDM2), the Cellular Inhibitor of Apoptosis (cIAP), ereblon (CRBN), etc.) to develop the most efficient PROTACs.
A protac molecule is made up of a target-protein-binding moiety, a ligand for recruiting the degradation machinery, and a chemical linker. The linker connects one ligand for E3 ligase recognition, and another ligand for target protein recognition, which also shapes the efficiency of a PROTAC molecule. Technicians can design and optimize suitable linkers in length and position to reach maximal interaction.
A further step to get optimal PROTACs is the structural modification, in which process Creative Biolabs works to improve the cell permeability and degree of degradation selectivity.
There are also solutions to test the efficacy and safety of PROTAC molecules, including in vitro evaluation, and in vivo animal test, which comprehensively evaluate the solubility, chemical stability, cell permeability efficacy, toxicity, ADME (absorption, distribution, metabolism, and excretion of a candidate drug), etc.
Further details about PROTAC solutions are accessible at https://www.creative-biolabs.com/protac.
About Creative Biolabs
Creative Biolabs has been exploring in the field of Proteolysis Targeting Chimeric (PROTAC) drug discovery for years and accumulated rich experience. Supported by senior scientists, clients’ projects of various research purposes have been accomplished in the past decade, which won a good reputation and returned customers. Skills of Creative Biolabs on PROTAC lie in several parts, ranging from ligand identification to safety tests. To help with the clients as much as possible, all the solutions can be offered in a one-stop manner, which means that the entire project is processed by Creative Biolabs accompanied by timely feedback and ensured for reliable outcome delivery.