Targeted Protein Degradation (TPD)

Over the last decade, we have rapidly gained experience and expertise in targeted protein degradation (TPD) drug  discovery, synthesizing hundreds of structurally diverse targeted protein degraders, via several of the ubiquitinoylation pathways.

Investment in our scientists’ development ensures they have expertise in this modality that can successfully be applied to your TPD drug discovery and development program. A specific focus is development of:

• Versatile workflows for the design, synthesis and assessment of targeted protein degraders
• Methods to screen targeted protein degraders
• Final purification of these large-small molecules containing two rigid protein binders and a flexible linker
• Quantification of the protein degradation and measurement of the subsequent biological activity

More recently we have:

• Developed a screening cascade for the molecular glue initiated CK1α degradation
• Launched a direct-to-biology service for the rapid synthesis and profiling of PROTACs

The challenges of targeted protein degradation

Targeted protein degradation remains one of the hot topics in drug discovery with PROTACs and molecular glues two of the most common pathways for designing TPD molecules for drug discovery.

This is because scientists across the world have come to understand their potential as large-small molecules offering the benefits of oral bioavailability, combined with a catalytic mechanism of action requiring a low dosage.

The development of this modality is still in its infancy, researchers are only now beginning to understand why these molecules, despite being rule-of-five non-compliant are orally bioavailable; and how to optimize their structure to facilitate ternary complex formation and protein degradation.

Discover how Concept Life Sciences can help you rapidly progress your targeted protein degraded program today. Contact us today for a confidential discussion with our team of expert scientists.