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A prolyl oligopeptidase inhibitor reduces tau pathology in cellular models and in mice with tauopathy.
Eteläinen TS, Silva MC, Uhari-Väänänen JK, De Lorenzo F, Jäntti MH, Cui H, Chavero-Pieres M, Kilpeläinen T, Mechtler C, Svarcbahs R, Seppälä E, Savinainen JR, Puris E, Fricker G, Gynther M, Julku UH, Huttunen HJ, Haggarty SJ, Myöhänen TT. Eteläinen TS, et al. Among authors: savinainen jr. Sci Transl Med. 2023 Apr 12;15(691):eabq2915. doi: 10.1126/scitranslmed.abq2915. Epub 2023 Apr 12. Sci Transl Med. 2023. PMID: 37043557
In Vivo Characterization of the Ultrapotent Monoacylglycerol Lipase Inhibitor {4-[bis-(benzo[d][1,3]dioxol-5-yl)methyl]-piperidin-1-yl}(1H-1,2,4-triazol-1-yl)methanone (JJKK-048).
Aaltonen N, Kedzierska E, Orzelska-Górka J, Lehtonen M, Navia-Paldanius D, Jakupovic H, Savinainen JR, Nevalainen T, Laitinen JT, Parkkari T, Gynther M. Aaltonen N, et al. Among authors: savinainen jr. J Pharmacol Exp Ther. 2016 Oct;359(1):62-72. doi: 10.1124/jpet.116.233114. Epub 2016 Jul 22. J Pharmacol Exp Ther. 2016. PMID: 27451409
5-Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein-Protein Interaction-Derived Functions.
Pätsi HT, Kilpeläinen TP, Jumppanen M, Uhari-Väänänen J, Wielendaele PV, De Lorenzo F, Cui H, Auno S, Saharinen J, Seppälä E, Sipari N, Savinainen J, De Meester I, Lambeir AM, Lahtela-Kakkonen M, Myöhänen TT, Wallén EAA. Pätsi HT, et al. J Med Chem. 2024 Apr 11;67(7):5421-5436. doi: 10.1021/acs.jmedchem.3c01993. Epub 2024 Mar 28. J Med Chem. 2024. PMID: 38546708
Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitors.
Patel JZ, Nevalainen TJ, Savinainen JR, Adams Y, Laitinen T, Runyon RS, Vaara M, Ahenkorah S, Kaczor AA, Navia-Paldanius D, Gynther M, Aaltonen N, Joharapurkar AA, Jain MR, Haka AS, Maxfield FR, Laitinen JT, Parkkari T. Patel JZ, et al. Among authors: savinainen jr. ChemMedChem. 2015 Feb;10(2):253-65. doi: 10.1002/cmdc.201402453. Epub 2014 Dec 11. ChemMedChem. 2015. PMID: 25504894 Free PMC article.
Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase.
Aaltonen N, Savinainen JR, Ribas CR, Rönkkö J, Kuusisto A, Korhonen J, Navia-Paldanius D, Häyrinen J, Takabe P, Käsnänen H, Pantsar T, Laitinen T, Lehtonen M, Pasonen-Seppänen S, Poso A, Nevalainen T, Laitinen JT. Aaltonen N, et al. Among authors: savinainen jr. Chem Biol. 2013 Mar 21;20(3):379-90. doi: 10.1016/j.chembiol.2013.01.012. Chem Biol. 2013. PMID: 23521796
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