Synthesis and Characterization of LRRK2 Modulators

GSK3357679A [25 (link)]was synthesized at GlaxoSmithKline. MLi-2 was synthesized by Natalia Shpiro (University of Dundee) as described previously [16 (link)]. GZD-824 (#21508) and Rebastinib (#21465) were purchased from Cambridge Bioscience and Ponatinib (#4274) from Tocris. Microcystin-LR was purchased from Enzo Life Sciences (#ALX-350-012-M001). Human recombinant full length wild-type Flag-LRRK2 (#A15198) and Flag-LRRK2[G2019S] (#A15201) were from ThermoFisher Scientific. Diisopropylfluorophosphate was from Sigma (#D0879).

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Tasegian A., Singh F., Ganley I.G., Reith A.D, & Alessi D.R. (2021). Impact of Type II LRRK2 inhibitors on signaling and mitophagy. Biochemical Journal, 478(19), 3555-3573.

Publication 2021

Ponatinib Microcystin-LR Flag-LRRK2[G2019S] Diisopropylfluorophosphate

Diisopropylfluorophosphate Gzd 824 Human Lrrk2 Microcystin lr Ponatinib Rebastinib

Corresponding Organization :

Other organizations : MRC Protein Phosphorylation and Ubiquitylation Unit, University of Dundee, Medical Research Council, GlaxoSmithKline (United Kingdom)

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Variable analysis

independent variables

GSK3357679A [25 (link)]
MLi-2
GZD-824 (#21508)
Rebastinib (#21465)
Ponatinib (#4274)
Microcystin-LR
Human recombinant full length wild-type Flag-LRRK2 (#A15198)
Human recombinant Flag-LRRK2[G2019S] (#A15201)
Diisopropylfluorophosphate

dependent variables

Not explicitly mentioned

control variables

Not explicitly mentioned

controls

Human recombinant full length wild-type Flag-LRRK2 (#A15198)
Human recombinant Flag-LRRK2[G2019S] (#A15201)

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