Poster
20

LRRK2 Inhibitor Evaluation and Profiling in Both Biochemical and Cellular HTS Formats by SelectScreen® Screening Services

Discussion

Parkinson's Disease (PD) is a progressive neurological disorder that results from degeneration of neurons in a region of the brain that controls movement, impacting an estimated 6.3 million people worldwide. To date, mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are the most common genetic cause of PD. LRRK2 is a protein kinase now being aggressively pursued as a target for PD therapeutics. However, studies of LRRK2 function and inhibition have been hampered by a lack of tools to express LRRK2 in diverse cell types as well as high-throughput biochemical and cell based assays. To address these needs, we have developed BacMam particles to express both untagged and green fluorescent protein (GFP) tagged full-length LRRK2 (WT and disease relevant mutants). BacMam technology has enabled higher levels of expression of LRRK2 in both workhorse cell lines (e.g. U-2 OS, HEK293T) and cells more physiologically relevant to neuroscience such as neuroblastoma SH-SY5Y and primary astrocytes compared to standard lipid transfection. Furthermore, the ability to express high levels of LRRK2 in these systems has enabled modular high-throughput assays for full-length LRRK2. Utilizing BacMam expression and LanthaScreen® technology, biochemical assays to measure inhibitor binding and cellular assays to measure inhibitor effects on kinase activity were developed and implemented by SelectScreen® Screening Services. Together these technologies will advance the field of PD research and therapeutics by addressing the currently unmet need for modular over expression, inhibitor binding assays and cellular kinase assays for full-length LRRK2.

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