Search Results - "Kilpeläinen, Tommi"
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5‑Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein–Protein Interaction-Derived Functions
Published in Journal of medicinal chemistry (11-04-2024)“…A series of novel 5-aminothiazole-based ligands for prolyl oligopeptidase (PREP) comprise selective, potent modulators of the protein–protein interaction…”
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2
Nonpeptidic Oxazole-Based Prolyl Oligopeptidase Ligands with Disease-Modifying Effects on α‑Synuclein Mouse Models of Parkinson’s Disease
Published in Journal of medicinal chemistry (08-06-2023)“…Prolyl oligopeptidase (PREP) is a widely distributed serine protease in the human body cleaving proline-containing peptides; however, recent studies suggest…”
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3
New tricks of prolyl oligopeptidase inhibitors – A common drug therapy for several neurodegenerative diseases
Published in Biochemical pharmacology (01-03-2019)“…[Display omitted] Changes in prolyl oligopeptidase (PREP) expression levels, protein distribution, and activity correlate with aging and are reported in many…”
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4
Removal of proteinase K resistant αSyn species does not correlate with cell survival in a virus vector-based Parkinson's disease mouse model
Published in Neuropharmacology (01-11-2022)“…Parkinson's disease (PD) is characterized by degeneration of nigrostriatal dopaminergic neurons and accumulation of α-synuclein (αSyn) as Lewy bodies…”
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The effect of prolyl oligopeptidase inhibitors on alpha-synuclein aggregation and autophagy cannot be predicted by their inhibitory efficacy
Published in Biomedicine & pharmacotherapy (01-08-2020)“…•Prolyl oligopeptidase (PREP) inhibition decreases α-synuclein aggregation and induce autophagy in cells and in vivo.•These effects are related to…”
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Prolyl oligopeptidase inhibition activates autophagy via protein phosphatase 2A
Published in Pharmacological research (01-01-2020)“…[Display omitted] Prolyl oligopeptidase (PREP) is a serine protease that has been studied particularly in the context of neurodegenerative diseases for decades…”
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Behavioural and dopaminergic changes in double mutated human A30PA53T alpha-synuclein transgenic mouse model of Parkinson´s disease
Published in Scientific reports (22-11-2019)“…Alpha-synuclein (aSyn) is the main component of Lewy bodies, the histopathological marker in Parkinson’s disease (PD), and point mutations and multiplications…”
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2‑Imidazole as a Substitute for the Electrophilic Group Gives Highly Potent Prolyl Oligopeptidase Inhibitors
Published in ACS medicinal chemistry letters (14-10-2021)“…Different five-membered nitrogen-containing heteroaromatics in the position of the typical electrophilic group in prolyl oligopeptidase (PREP) inhibitors were…”
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Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors
Published in ACS medicinal chemistry letters (12-12-2019)“…4-Phenylbutanoyl-aminoacyl-2(S)-tetrazolylpyrrolidines were studied as prolyl oligopeptidase inhibitors. The compounds were more potent than expected from the…”
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10
Prolyl oligopeptidase inhibition reduces alpha‐synuclein aggregation in a cellular model of multiple system atrophy
Published in Journal of cellular and molecular medicine (01-10-2021)“…Multiple system atrophy (MSA) is a fatal neurodegenerative disease where the histopathological hallmark is glial cytoplasmic inclusions in oligodendrocytes,…”
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A prolyl oligopeptidase inhibitor reduces tau pathology in cellular models and in mice with tauopathy
Published in Science translational medicine (12-04-2023)“…Tauopathies are neurodegenerative diseases that are characterized by accumulation of hyperphosphorylated tau protein, higher-order aggregates, and tau…”
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Novel Small‐Molecular Ligands for Prolyl Oligopeptidase to Combat Tauopathies
Published in Alzheimer's & dementia (01-12-2023)“…Background Tauopathies that include e.g. frontotemporal dementia and Alzheimer’s disease, are neurodegenerative diseases characterized by accumulation of…”
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