April 2017
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4 Reads
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Publications (3)
April 2017
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7 Reads
March 2017
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115 Reads
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83 Citations
Journal of Medicinal Chemistry
Since loss of function mutations of PINK1 lead to early-onset Parkinson's disease, there has been growing interest in the discovery of small molecules that amplify the kinase activity of PINK1. We herein report the design, synthesis, serum stability and hydrolysis of four kinetin riboside ProTides. These ProTides, along with kinetin riboside, activated PINK1 in cells independent of mitochondrial depolarization. This highlights the potential of modified nucleosides and their phosphate prodrugs as treatments for neurodegenerative diseases.
Citations (1)
... An initial approach to activate PINK1 with neosubstrates 272 led to the discovery that kinetin, a cellpermeable precursor of kinetin triphos phate (KTP) that has a furfuryl group at the N 6 position of its adenine ring, can activate PINK1 in cells and relieves mitochondrial mutations in flies and mice in a PINK1dependent manner 273,274 . Kinetin exhibited low potency and poor pharmacokinetics and brain penetrance, pre cluding effective use in PD models in vivo 275 . ...
- Citing Article
March 2017
Journal of Medicinal Chemistry