المؤلفون: Leino, Teppo O., Noutsias, Dimitris, Helttunen, Kaisa, Moilanen, Jani O., Tarkkonen, Eeki, Kalenius, Elina, Kiesilä, Anniina, Pihko, Petri M.

المصدر: European Journal of Organic Chemistry ; ISSN 1434-193X 1099-0690

الإتاحة: https://doi.org/10.1002/ejoc.202400321Test

المؤلفون: Leino, Teppo O., Turku, Ainoleena, Urvas, Lauri, Adhikari, Karuna, Oksanen, Jouni, Steynen, Yana, Yli-Kauhaluoma, Jari, Xhaard, Henri, Kukkonen, Jyrki P., Wallén, Erik A. A.

المساهمون: Divisions of Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, Drug Research Program, Pharmaceutical Design and Discovery group, Veterinary Biosciences, Faculty of Veterinary Medicine, Faculty of Pharmacy, Department of Pharmacology, Jari Yli-Kauhaluoma / Principal Investigator, Computational Adme, Henri Xhaard / Principal Investigator, Division of Pharmaceutical Biosciences, Erik Wallen / Principal Investigator, Medicinal Chemistry research group

مصطلحات موضوعية: Agonist, Azulene, Medicinal chemistry, Orexin receptor, Sulfonamides, 3111 Biomedicine, 1182 Biochemistry, cell and molecular biology, 317 Pharmacy

وصف الملف: application/pdf

العلاقة: Leino , T O , Turku , A , Urvas , L , Adhikari , K , Oksanen , J , Steynen , Y , Yli-Kauhaluoma , J , Xhaard , H , Kukkonen , J P & Wallén , E A A 2023 , ' Azulene as a biphenyl mimetic in orexin/hypocretin receptor agonists ' , Bioorganic & Medicinal Chemistry , vol. 88-89 , 117325 . https://doi.org/10.1016/j.bmc.2023.117325Test; ORCID: /0000-0002-6989-1564/work/137437590; ORCID: /0000-0003-0370-7653/work/137437764; ORCID: /0000-0003-0959-7221/work/137438818; ORCID: /0000-0003-2582-7971/work/137440251; http://hdl.handle.net/10138/359559Test; c9572f10-7a1b-42fd-9f32-fe162591a425; 001001557400001

الإتاحة: http://hdl.handle.net/10138/359559Test

المؤلفون: Kilpelainen, Tommi P., Patsi, Henri T., Svarcbahs, Reinis, Julku, Ulrika H., Eteläinen, Tony S., Cui, Hengjing, Auno, Samuli, Sipari, Nina, Norrbacka, Susanna, Leino, Teppo O., Jäntti, Maria, Myöhänen, Timo T., Wallen, Erik A. A.

المساهمون: Divisions of Faculty of Pharmacy, PREP in neurodegenerative disorders, Division of Pharmaceutical Chemistry and Technology, Division of Pharmacology and Pharmacotherapy, Organismal and Evolutionary Biology Research Programme, Faculty of Pharmacy, Pharmaceutical Design and Discovery group, Drug Research Program, Erik Wallen / Principal Investigator, Medicinal Chemistry research group

مصطلحات موضوعية: Endopeptidase inhibitor, Efficient synthesis, Overexpression, Autophagy, Kyp-2047, Drug, Pharmacokinetics, Phosphorylation, Aggregation, Activation, 317 Pharmacy

وصف الملف: application/pdf

العلاقة: Kilpelainen , T P , Patsi , H T , Svarcbahs , R , Julku , U H , Eteläinen , T S , Cui , H , Auno , S , Sipari , N , Norrbacka , S , Leino , T O , Jäntti , M , Myöhänen , T T & Wallen , E A A 2023 , ' Nonpeptidic Oxazole-Based Prolyl Oligopeptidase Ligands with Disease-Modifying Effects on alpha-Synuclein Mouse Models of Parkinson's Disease ' , Journal of Medicinal Chemistry , vol. 66 , no. 11 , pp. 7475-7496 . https://doi.org/10.1021/acs.jmedchem.3c00235Test; ORCID: /0000-0002-0786-2493/work/137858078; ORCID: /0000-0002-9277-6687/work/137863336; ORCID: /0000-0003-2582-7971/work/137863726; ORCID: /0000-0002-1312-9837/work/137864347; ORCID: /0000-0003-2931-6853/work/137864976; ORCID: /0000-0003-0802-2557/work/137865122; http://hdl.handle.net/10138/563197Test; 16a1b13f-44d5-4dbb-b1f4-a84fa0485c6f; 001005897700001

الإتاحة: http://hdl.handle.net/10138/563197Test

المؤلفون: Kilpeläinen, Tommi P., Pätsi, Henri T., Svarcbahs, Reinis, Julku, Ulrika H., Eteläinen, Tony S., Cui, Hengjing, Auno, Samuli, Sipari, Nina, Norrbacka, Susanna, Leino, Teppo O., Jäntti, Maria, Myöhänen, Timo T., Wallén, Erik A. A.

المساهمون: Terveyden Tutkimuksen Toimikunta, Helsinki Institute of Life Science, Helsingin Yliopisto, Business Finland, Sigrid Juselius Foundation

المصدر: Journal of Medicinal Chemistry ; volume 66, issue 11, page 7475-7496 ; ISSN 0022-2623 1520-4804

الإتاحة: https://doi.org/10.1021/acs.jmedchem.3c00235Test

المؤلفون: Leino, Teppo O., Sieger, Peter, Yli-Kauhaluoma, Jari, Wallén, Erik A.A., Kley, Jörg T.

مصطلحات موضوعية: Indole, Naphthalene, Photostability, Scaffold hopping, atsuleeni, lääkesuunnittelu, aromaattiset yhdisteet, lääkekemia, biologinen aktiivisuus

وصف الملف: application/pdf; fulltext

العلاقة: European Journal of Medicinal Chemistry; 237; 330800; Research Council of Finland; Suomen Akatemia; Leino, T. O., Sieger, P., Yli-Kauhaluoma, J., Wallén, E. A., & Kley, J. T. (2022). The azulene scaffold from a medicinal chemist's perspective : Physicochemical and in vitro parameters relevant for drug discovery. European Journal of Medicinal Chemistry , 237 , Article 114374. https://doi.org/10.1016/j.ejmech.2022.114374Test; CONVID_118852176; URN:NBN:fi:jyu-202204262374; http://urn.fi/URN:NBN:fi:jyu-202204262374Test

الإتاحة: http://urn.fi/URN:NBN:fi:jyu-202204262374Test

المؤلفون: Leino, Teppo O., Turku, Ainoleena, Yli-Kauhaluoma, Jari Tapani, Kukkonen, Jyrki P., Xhaard, Henri, Wallén, Erik A. A.

المساهمون: Faculty of Pharmacy, Pharmaceutical Design and Discovery group, Division of Pharmaceutical Chemistry and Technology, Drug Research Program, Jari Yli-Kauhaluoma / Principal Investigator, Jyrki Kukkonen / Principal Investigator, Veterinary Biochemistry and Cell Biology, Veterinary Biosciences, Departments of Faculty of Veterinary Medicine, Faculty of Veterinary Medicine, Department of Physiology, Medicum, Henri Xhaard / Principal Investigator, Erik Wallen / Principal Investigator, Medicinal Chemistry research group

مصطلحات موضوعية: 317 Pharmacy, 116 Chemical sciences, Azulene, Orexin receptor, Potentiator, Agonist, Antagonist, Sleep-wake regulation, PROTEIN-COUPLED RECEPTORS, HAMSTER OVARY CELLS, SIGNAL-TRANSDUCTION, CA2+ INFLUX, OX1, DERIVATIVES, INHIBITORS, PEPTIDES, LIGANDS, KINASE

وصف الملف: application/pdf

العلاقة: Leino , T O , Turku , A , Yli-Kauhaluoma , J T , Kukkonen , J P , Xhaard , H & Wallén , E A A 2018 , ' Azulene-based compounds for targeting orexin receptors ' , European Journal of Medicinal Chemistry , vol. 157 , pp. 88-100 . https://doi.org/10.1016/j.ejmech.2018.07.040Test; ORCID: /0000-0003-0370-7653/work/50286680; ORCID: /0000-0003-0959-7221/work/50289879; ORCID: /0000-0003-2582-7971/work/50290708; ORCID: /0000-0002-6989-1564/work/63349244; http://hdl.handle.net/10138/319069Test; be64b9c4-f27c-4b99-9902-88569234386b; 85050849346; 000447480000008

الإتاحة: http://hdl.handle.net/10138/319069Test

المؤلفون: Rinne, Maiju K., Leino, Teppo O., Turku, Ainoleena, Turunen, Pauli M., Steynen, Yana, Xhaard, Henri, Wallen, Erik A. A., Kukkonen, Jyrki P.

المساهمون: Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, Veterinary Biosciences, Departments of Faculty of Veterinary Medicine, Pharmaceutical Design and Discovery group, Medicum, Department of Physiology, Veterinary Biochemistry and Cell Biology, Henri Xhaard / Principal Investigator, Computational Adme, Drug Research Program, Erik Wallen / Principal Investigator, Jyrki Kukkonen / Principal Investigator, Medicinal Chemistry research group

مصطلحات موضوعية: Orexin, Calcium, Phospholipase C, cAMP, Cell death, ERK, ACTIVATED PROTEIN-KINASE, OREXIN TYPE-2 RECEPTOR, HAMSTER OVARY CELLS, OX1 RECEPTOR, NARCOLEPSY, SLEEP, MICE, WAKEFULNESS, APOPTOSIS, GENE, 317 Pharmacy

وصف الملف: application/pdf

العلاقة: Santeri Suokas, Marja Peltola and Jouni Oksanen (Biochemistry and Cell Biology, Department of Veterinary Biosciences, University of Helsinki) are gratefully acknowledged for technical assistance with the experiments, and Kaj-Roger Hurme (Instrument Centre of Faculty of Agriculture and Forestry, University of Helsinki) and Raija Savolainen (Institute of Biotechnology, University of Helsinki) for all help with the liquid scintillation counting and luminescence measurements, respectively. This work was supported by the European Union (FP7-HEALTHproject GLORIA [# 602919]), the Magnus Ehrnrooth Foundation, the Finnish Cultural Foundation, the Orion Research Foundation, the Liv & Halsa Foundation, and the Doctoral Program in Drug Research of the University of Helsinki.; Rinne , M K , Leino , T O , Turku , A , Turunen , P M , Steynen , Y , Xhaard , H , Wallen , E A A & Kukkonen , J P 2018 , ' Pharmacological characterization of the orexin/hypocretin receptor agonist Nag 26 ' , European Journal of Pharmacology , vol. 837 , pp. 137-144 . https://doi.org/10.1016/j.ejphar.2018.09.003Test; ORCID: /0000-0003-0959-7221/work/49162309; ORCID: /0000-0003-2582-7971/work/49162603; ORCID: /0000-0002-3129-1678/work/49160715; ORCID: /0000-0002-6989-1564/work/63349243; ORCID: /0000-0003-3218-2841/work/68616121; http://hdl.handle.net/10138/305214Test; aff2e1b3-c4b3-4caf-a9e3-98c8277aa516; 85053081769; 000444963400016

الإتاحة: http://hdl.handle.net/10138/305214Test

المؤلفون: Vidilaseris, Keni, Kiriazis, Alexandros, Turku, Ainoleena, Khattab, Ayman, Johansson, Niklas G., Leino, Teppo O., Kiuru, Paula S., Boije af Gennäs, Gustav, Meri, Seppo, Yli-Kauhaluoma, Jari, Xhaard, Henri, Goldman, Adrian

المساهمون: BBSRC, Academy of Finland, The Jane and Aatos Erkko Foundation, University of Helsinki funds

المصدر: Science Advances ; volume 5, issue 5 ; ISSN 2375-2548

الإتاحة: https://doi.org/10.1126/sciadv.aav7574Test

المؤلفون: Karhu, Lasse, Weisell, Janne, Turunen, Pauli M., Leino, Teppo O., Pätsi, Henri, Xhaard, Henri, Kukkonen, Jyrki P., Wallén, Erik A.A.

المساهمون: Faculty of Pharmacy, Pharmaceutical Design and Discovery group, Medicum, Veterinary Biosciences, Departments of Faculty of Veterinary Medicine, Faculty of Veterinary Medicine, Division of Pharmaceutical Chemistry and Technology, Henri Xhaard / Principal Investigator, Drug Research Program, Jyrki Kukkonen / Principal Investigator, Veterinary Biochemistry and Cell Biology, Department of Physiology, Erik Wallen / Principal Investigator, Medicinal Chemistry research group

مصطلحات موضوعية: peptide stapling, pseudopeptide, orexin, G protein-coupled receptor, OX1, BINDING, RECOGNITION, APPETITE, LIGANDS, ANALOGS, SYSTEM, ACID, 3111 Biomedicine, 317 Pharmacy, 1182 Biochemistry, cell and molecular biology

وصف الملف: application/pdf

العلاقة: Karhu , L , Weisell , J , Turunen , P M , Leino , T O , Pätsi , H , Xhaard , H , Kukkonen , J P & Wallén , E A A 2018 , ' Stapled truncated orexin peptides as orexin receptor agonists ' , Peptides , vol. 102 , pp. 54-60 . https://doi.org/10.1016/j.peptides.2018.02.004Test; RIS: urn:47A3C83D5A70294343EAE7F9322ED5A3; ORCID: /0000-0003-2582-7971/work/44189377; ORCID: /0000-0001-6432-8580/work/44189445; ORCID: /0000-0002-3129-1678/work/44189234; ORCID: /0000-0002-6989-1564/work/63349261; http://hdl.handle.net/10138/234577Test; 342c7d94-0f56-473a-9ae0-178e813e1e17; 85042934582; 000427917500008

الإتاحة: http://hdl.handle.net/10138/234577Test

المؤلفون: Keurulainen, Leena, Heiskari, Mikko, Nenonen, Satu, Nasereddin, Abedelmajeed, Kopelyanskiy, Dmitry, Leino, Teppo O., Yli-Kauhaluoma, Jari, Jaffe, Charles L., Kiuru, Paula

المساهمون: Faculty of Pharmacy, Division of Pharmaceutical Chemistry and Technology, Jari Yli-Kauhaluoma / Principal Investigator, Drug Discovery, Pharmaceutical Design and Discovery group, Drug Research Program, Medicinal Chemistry research group

مصطلحات موضوعية: IN-VITRO ACTIVITY, INHIBITORS, DESIGN, DRUGS, AMASTIGOTES, DERIVATIVES, CYANATION, ASSAY, 1182 Biochemistry, cell and molecular biology, 317 Pharmacy

وصف الملف: application/pdf

العلاقة: We thank Ms. Anna Keltikangas nee Takala for the synthesis assistance. This study was supported by the Academy of Finland (projects 264020 and 265481 to JYK). CLJ holds the Michael and Penny Feiwel Professorial Chair of Dermatology.; Keurulainen , L , Heiskari , M , Nenonen , S , Nasereddin , A , Kopelyanskiy , D , Leino , T O , Yli-Kauhaluoma , J , Jaffe , C L & Kiuru , P 2015 , ' Synthesis of carboxyimidamide-substituted benzo[c][1,2,5]oxadiazoles and their analogs, and evaluation of biological activity against Leishmania donovani ' , MedChemComm , vol. 6 , no. 9 , pp. 1673-1678 . https://doi.org/10.1039/c5md00119fTest; ORCID: /0000-0001-8528-7757/work/30218069; ORCID: /0000-0003-0370-7653/work/28760601; ORCID: /0000-0003-2582-7971/work/29942451; ORCID: /0000-0001-6084-684X/work/41128118; http://hdl.handle.net/10138/224652Test; 73e21bf2-65fd-4006-8e14-3f82da4f00a5; 84940939353; 000360639300012

الإتاحة: http://hdl.handle.net/10138/224652Test