Ligand Design for Retinoic Acid Receptors (RAR)-targeting PROTAC

Creative Biolabs offers customized ligand design services for RAR-targeting PROTAC. With a variety of mature platforms and state-of-art technologies, we can evaluate and improve the efficacy of candidate ligands in clinical use. We are dedicated to providing the best solutions and customized services to our worldwide customers.

Introduction of Retinoic Acid Receptors (RAR)

Retinoic acid (RA), a type of vitamin A, is essential for mediating many biological activities, such as cell differentiation, embryonic development, and immune responses. Retinoic acid receptors (RARs), belonging to the steroid/thyroid hormone receptor superfamily, play an important role in regulating the activation and expression of retinoic acid. Three subtypes of RARs, RARα, RARβ, and RARγ, have been identified and studied in the past few years. Previous studies have demonstrated that the expression level of RARs can be reduced or absent in many cell types, especially for cancer cells. As a consequence, RARs have been considered as effective targets for discovering novel drugs in human disease treatments.

Nowadays, a new technology named PROTAC, proteolysis-targeting chimera, has been broadly used for inducing protein degradation by using a targeting molecule. The PROTAC system is based on two ligands and a linker. One ligand is designed to recruit E3 ligase, another ligand is used to bind with target proteins, and they are connected by a chemical linker. Currently, PROTAC has been widely used to link inhibitors to RARs for therapeutic intervention.

A schematic diagram of peptide-based proteolysis targeting chimera (PROTAC). Fig.1 A schematic diagram of peptide-based proteolysis targeting chimera (PROTAC). (Zou, 2019)

Our Ligand Design Platform for RAR-targeting PROTAC

Pilot studies have shown that RARs are key trans-regulators that regulate the expression of a variety of disease cells based on various ligands. In many human cancers, the transcription level of RARs is associated with the interaction between RARs and several transcriptional complexes. Furthermore, recent researchers have revealed that RAR-targeting PROTAC can be an attractive strategy for modulating the function of RARs in both biological studies and potential drug discovery.

Creative Biolabs has developed a one-stop solution ligand design platform to help our clients design and synthesize RAR-targeting PROTAC degradation inducers. The studies conducted by our labs have suggested that this platform is useful for inducing RAR degradation and reducing its expression in several cancer cells. Up to now, many PROTAC systems, such as peptide-based, antibody-based, as well as small molecule-based PROTAC, have been designed to target RARs, which pioneered the field. Additionally, we also offer a panel of assays to optimize ligands of your interest, and our service chain covers all stages of the ligand design process, ranging from the linker length optimization to ligand composition evaluation.

With experienced experts and advanced platforms, Creative Biolabs can provide excellent RAR-targeting PROTAC ligand design services. We will work with you to develop the most appropriate strategy that will offer the most meaningful data for your research. If you have any special needs in our services or be interested in learning more about our company, please feel free to contact us for more details.

Reference

  1. Zou, Y.; et al. The PROTAC technology in drug development. Cell Biochem Funct. 2019, 37(1): 21-30.
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