It has been reported that proteolysis targeting chimera (Protein Degraders) technology has the potential to induce protein proteasomal degradation which can be used for inhibiting many disease progressions. Creative Biolabs has accumulated a lot of experience in ligand design studies for different protein kinases by using Protein Degraders technology. Our scientists specialized in Protein Degraders studies will work with you to develop a most appropriate strategy that will offer the most meaningful data for your research.

Introduction to Protein Kinases

Previous studies have indicated that protein kinases play a critical role in regulating cell differentiation, cell metabolism, and cell apoptosis. The dysregulation of these protein kinases, such as Abl, BTK, CDK9, and DAPK1, can accelerate the progression of various diseases. As a result, protein kinases have been considered as attractive targets for many diseases, and drugs targeting protein kinases have also been extensively studied. Meanwhile, a novel and effective Protein Degraders technology has been developed and widely used for protein kinase-based drug discovery research. Protein Degraders is a multifunctional molecule that consists of a ligand for binding the protein of interest, a ligand for binding E3 ligase system, as well as a chemical linker for connecting these two ligands. Currently, Protein Degraders has been successfully used for degrading a number of protein kinases, including BCR-ABL, Akt, RIPK2, PSD-95, by using functional degraders that bind specific E3 ubiquitin ligases.

Fig.1 Synthesis of a Protein Degraders that selectively degrades cyclin-dependent kinase 9 (CDK9). (Robb, 2017)

Our Ligand Design Platform for Protein Kinases

The significant role of protein kinases in regulating cell signaling and the cell-cycle process has aroused much attention in the past few years. Moreover, different kinds of Protein Degraders molecules, such as small molecules, antibodies, and peptides, have been generated for mediating the degradation of protein kinases in the drug discovery area. Following this trend, Creative Biolabs can provide state-of-art ligand design services for any protein kinases. Nowadays, we have developed efficient protocols for designing and assessing potential ligands. And we can also conduct ligand optimization studies in various kind of protein kinases, including but not limited to:

As a specialist in a molecule discovery study, Creative Biolabs is confident in providing a wide range of ligand design services for various target proteins. We have established a comprehensive Protein Degraders technology platform that enables for ligand design, ligand synthesis, ligand evaluation, as well as ligand optimization. Our professional scientists will customize a detailed protocol according to your special purpose. If you have any problems, please don’t hesitate to contact us for more details.

Reference

1. Robb, C. M.; et al. Chemically induced degradation of CDK9 by proteolysis targeting chimera (Protein Degraders). Chemical Communications. 2017, 53(54): 7577-7580.