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PROTAC Structural Modification

Once the early design of ligands for target protein, E3 ligase and linker are initially proposed, Creative Biolabs will be dedicated to small molecule structural modification to finalize the PROTAC molecule discovery and design. With senior high-level scientists and experienced chemical structural optimization platform, Creative Biolabs is fully competent and committed to high quality and reliable PROTACs to our clients.

Background

In principle, a vast array of PROTACs can be designed for drug discovery because of various combinations of different ligands and linkers, as well as more than 600 E3 ligases. Even though PROTACs owns great potential for practical applications as chimeric molecules, the application of PROTACs is limited caused by poor molecule stability, biodistribution, and cellular permeability in vivo. As a consequence of this problem, there has been increased research in PROTAC structural modification since structure determines the properties of compounds (see Fig. 1). The development of cell-permeable PROTACs is relatively mature now as an exciting breakthrough for PROTAC technology since it offers the possibility of targeting disease-causing proteins in vivo. Also, it results in promising application in drug development.

Drug-like properties of small molecule drug candidates. Fig. 1 Drug-like properties of small molecule drug candidates.

Introduction of PROTAC Structural Modification

Empowered by a wide range of E3 ubiquitin ligases and linkers, Creative Biolabs provides different “mix and match” combination strategies for our clients to screen the optimal PROTAC candidate to maximum the degradation efficiency for target proteins. In the meantime, we will utilize our professional chemical structural modification platform to offer the structural modification service to optimize the pharmacological properties and other drug-like properties. For example, we can modify the peptide ligands or replace peptide ligands with small molecules to improve permeability, or we can add a poly-D-arginine tag in the carboxyl terminus of E3 ligase ligand to improve the cell permeability and prevent nonspecific degradation. The structural modification may focus on hydrogen bonding, polar surface area, lipophilicity, shape, molecular weight, reactivity, pKa, and detailed modification will be designed as per specific properties of PROTACs to fit the specific needs of your projects. With this kind of service, Creative Biolabs aims to provide an ideal PROTAC to our clients for further research or drug discovery. Once the design and modification are completed, Creative Biolabs is capable of providing synthesis service.

Cell-permeable PROTACs with a poly-arginine. Fig. 2 Cell-permeable PROTACs with a poly-arginine. (Gu, 2018)

Highlight Features of Our Services

  • One-stop service from scratch to full development
  • Experienced scientists and technicians
  • Advanced structural modification platform
  • Superior efficiency

To optimize the structural properties of PROTACs and explore the broad application of PROTAC in a variety of diseases, Creative Biolabs is committed to offering a variety of methodologies in PROTAC structural modification to investigate and develop an ideal PROTAC for our worldwide clients. To achieve the best efficacy, we do recommend our one-stop PROTAC design service to maximize the success of projects. For more detailed information, please feel free to contact us.

Reference

  1. Gu, S.; et al. PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery. Bioessays. 2018, 40(4), e1700247.
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