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Once the design and modification of ligands for target protein/E3 ligase and linker are initially proposed by our scientists, Creative Biolabs will be dedicated to peptide/compound synthesis to offer high-quality products. With extensive experience and advanced peptide/compound synthesis platform, Creative Biolabs has provided reliable custom peptides/compounds for numerous worldwide scientists and now is able to deliver products at leading speed to expedite the research for our clients.
As hetero-bifunctional molecules, PROTAC consists of a ligand for E3 ligase, a linker and another ligand for target protein. To date, therapeutic ligands include peptide and small molecules. The first PROTAC was developed by Sakamoto, and the ligand for target protein MetAP-2 is ovalicin peptide, the ligand to recruit E3 ligase is a phosphopeptide. For CRBN-based PROTACs - ARV-825 and dBET1, the ligands for target proteins are derived from small molecules inhibitors - OTX015 and JQ1 (see Fig.1), we call them as small molecule compounds. Thus, custom peptide and small molecule compound synthesis are essential during optimizing the existing PROTACs or novel PROTACs synthesis.
Fig. 1 Chemical structure examples of PROTACs. (Gu, 2018)
Peptide synthesis is the production of peptides, compounds for which multiple amino acids are linked via amide bonds. Through the condensation reaction of the carboxyl group of one amino acid to another, peptides are chemically synthesized. The chemical synthesis normally starts at the C-terminus of the peptide and proceeds toward the N-terminus. Our synthesis service offers a variety of options for synthesis platform, formats, modifications and purity levels to meet various research needs. Creative Biolabs utilizes the current popular FMOC solid-phase technology to synthesis small peptides (see Fig.2), and purify the products by HPLC, in addition, Creative Biolabs offers custom small molecules synthesis service to expand the in-house library of compounds. Empowered by our senior synthetic chemists with unparalleled expertise, we can assist you to develop specific peptide and new chemical compounds in the milligram to gram scale. With the assistance of our microwave and ligation technologies, we are able to increase chemical coupling efficiency and enhance the yield, also we can help you obtain reproducible products and consistent results. Beyond that, the comprehensive suite of analytical services will ensure high purity and structural confirmation.
Fig.2 Solid-phase synthesis of a dipeptide using an amide resin.
Creative Biolabs is committed to offering high-quality peptide/compound synthesis within the agreed timeline. We aim to share our knowledge and passion in the PROTAC field to promote the advances in science and drug discovery and for a healthier world. For any required custom synthesis project, please contact us and we will respond as soon as possible.