LRRK2 Degrader Discovery: A High-Throughput Direct-to-Biology Screening Platform

LRRK2 Degrader Discovery: A High-Throughput Direct-to-Biology Screening Platform

Accelerating CNS Drug Discovery with a Direct-to-Biology Platform

Parkinson’s Disease (PD) is a growing global concern, with LRRK2 emerging as a key therapeutic target. In this study, we showcase a novel high-throughput Direct-to-Biology platform to discover potent degraders against LRRK2 kinase, offering a valuable alternative to traditional kinase inhibition.

Our flexible and scalable approach enabled rapid synthesis and evaluation of bifunctional LRRK2 degraders, identifying several compounds with nanomolar potency, ready for validation in neurologically relevant systems.

Download the free poster to explore how our Direct-to-Biology platform can be applied to neurodegenerative drug discovery beyond LRRK2.

References:

  1. Liu, X., et al., Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2. J. Am. Chem. Soc. 2022, 144, 16930–16952.
  2. Araujo, E., et al., Indazole Based Compounds and Associated Methods of Use. U.S. Patent No. WO2022198112A1, 22 September 2022
  3. Araujo, E., et al., Selective Modulators of Mutant LRRK2 Proteolysis and Associated Methods of Use. U.S. Patent No. US11858940B2, 2 January 2024.

 

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