KDS2010, a Newly Developed Reversible MAO?B Inhibitor, as an Effective Therapeutic Candidate for Parkinson’s Disease

Title
KDS2010, a Newly Developed Reversible MAO?B Inhibitor, as an Effective Therapeutic Candidate for Parkinson’s Disease
Authors
오수진박기덕박종현남민호김현정이효원최지원김시원박선준송효정장보고윤형호허준영안희영Doo?Wan Cho양영수한수철김상욱전상용이창준
Issue Date
2021-10
Publisher
Neurotherapeutics
Citation
VOL 온라인게재, 온라인게재
Abstract
Monoamine oxidase-B (MAO-B) is a well-established therapeutic target for Parkinson's disease (PD); however, previous clinical studies on currently available irreversible MAO-B inhibitors have yielded disappointing neuroprotective effects. Here, we tested the therapeutic potential of KDS2010, a recently synthesized potent, selective, and reversible MAO-B inhibitor in multiple animal models of PD. We designed and synthesized a series of α-aminoamide derivatives and found that derivative KDS2010 exhibited the highest potency, specificity, reversibility, and bioavailability (> 100%). In addition, KDS2010 demonstrated significant neuroprotective and anti-neuroinflammatory efficacy against nigrostriatal pathway destruction in the mouse MPTP model of parkinsonism. Treatment with KDS2010 also alleviated parkinsonian motor dysfunction in 6-hydroxydopamine-induced and A53T mutant α-synuclein overexpression rat models of PD. Moreover, KDS2010 showed virtually no toxicity or side effects in non-human primates. KDS2010 could be a next-generation therapeutic candidate for PD.
URI
http://pubs.kist.re.kr/handle/201004/74009
ISSN
1933-7213
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KIST Publication > Article
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