Zobrazeno 1 - 10
of 41
pro vyhledávání: '"Erik A.A. Wallén"'
Autor:
Teppo O. Leino, Ainoleena Turku, Lauri Urvas, Karuna Adhikari, Jouni Oksanen, Yana Steynen, Jari Yli-Kauhaluoma, Henri Xhaard, Jyrki P. Kukkonen, Erik A.A. Wallén
Azulene is a rare ring structure in drugs, and we investigated whether it could be used as a biphenyl mimetic in known orexin receptor agonist Nag 26, which is binding to both orexin receptors OX1 and OX2 with preference towards OX2. The most potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7df09711b7611d8344b9ac76de0bc4c
http://hdl.handle.net/10138/359559
http://hdl.handle.net/10138/359559
Publikováno v:
European journal of medicinal chemistry. 237
Azulene is a bicyclic scaffold rarely applied in medicinal chemistry. Here we report physicochemical and in vitro parameters relevant for drug discovery for a series of diversely substituted azulenes. We synthesized and characterized several scaffold
Autor:
Pyry M. J. Dillemuth, Timo T. Myöhänen, Maija Lahtela-Kakkonen, Henri T. Pätsi, Samuli Auno, Erik A.A. Wallén, Khaled Arja, Tommi Kilpeläinen
Publikováno v:
ACS Medicinal Chemistry Letters
Different five-membered nitrogen-containing heteroaromatics in the position of the typical electrophilic group in prolyl oligopeptidase (PREP) inhibitors were investigated and compared to tetrazole. The 2-imidazoles were highly potent inhibitors of t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d2b18fee964d75dc4dbbf9ec8da5bbf
http://hdl.handle.net/10138/336056
http://hdl.handle.net/10138/336056
Autor:
Henri Xhaard, Erik A.A. Wallén, Jari Yli-Kauhaluoma, Jyrki P. Kukkonen, Teppo O. Leino, Lasse Karhu, Ainoleena Turku
Publikováno v:
ChemMedChem. 14:965-981
We previously demonstrated the potential of di- or trisubstituted azulenes as ligands (potentiators, weak agonists, and antagonists) of the orexin receptors. In this study we investigated 27 1-benzoylazulene derivatives, uncovering seven potentiators
Autor:
Kati-Sisko Vellonen, Laura Hellinen, Johannes Vrijdag, Henri J. Huttunen, Arto Urtti, Xu Yan, Tommi Kilpeläinen, Reinis Svarcbahs, Timo T. Myöhänen, Anne-Marie Lambeir, Erik A.A. Wallén
Publikováno v:
Biomedicine and pharmacotherapy
Biomedicine & Pharmacotherapy, Vol 128, Iss, Pp 110253-(2020)
Biomedicine & Pharmacotherapy, Vol 128, Iss, Pp 110253-(2020)
Previous studies have shown that prolyl oligopeptidase (PREP) negatively regulates autophagy and increases the aggregation of alpha-synuclein (alpha Syn), linking it to the pathophysiology of Parkinson's disease. Our earlier results have revealed tha
Autor:
Ainoleena Turku, Henri Xhaard, Erik A.A. Wallén, Jyrki P. Kukkonen, Jari Yli-Kauhaluoma, Teppo O. Leino
Publikováno v:
European Journal of Medicinal Chemistry. 157:88-100
A library of 70 000 synthetically accessible azulene-based compounds was virtually screened at the OX2 receptor. Based on the results, a series of azulene derivatives was synthesized and the binding to and activation of both orexin receptor subtypes
Autor:
Jonna Tyni, Maija Lahtela-Kakkonen, Timo T. Myöhänen, Erik A.A. Wallén, Tommi Kilpeläinen, Tony Eteläinen
Publikováno v:
ACS Med Chem Lett
[Image: see text] 4-Phenylbutanoyl-aminoacyl-2(S)-tetrazolylpyrrolidines were studied as prolyl oligopeptidase inhibitors. The compounds were more potent than expected from the assumption that the tetrazole would also here be a bioisostere of the car
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73545c046ba9a0c2e7d7a0042e7946f3
http://hdl.handle.net/10138/325038
http://hdl.handle.net/10138/325038
Autor:
Niklas G. Johansson, Teppo O. Leino, Lars Devisscher, Erik A.A. Wallén, Jari Yli-Kauhaluoma, Nina Sipari
Publikováno v:
European Journal of Organic Chemistry. 2016:5539-5544
An efficient synthetic route to 1,3,6-trisubstituted azulenes based on the 1-acyloxyazulene scaffold was developed. The 1-position in azulene was substituted in the ring-formation step with a functionalized acyloxy group. Additionally, the 3- and 6-p
Autor:
Maija Lahtela-Kakkonen, Kristian Meinander, Henna Ylikangas, Ale Närvänen, Hannu Koistinen, Erik A.A. Wallén, Ulf-Håkan Stenman
Publikováno v:
Biological Chemistry. 397:1229-1235
Kallikrein-related peptidase-3 (KLK3, known also as prostate-specific antigen, PSA) is highly expressed in the prostate. KLK3 possess antiangiogenic activity, which we have found to be related to its proteolytic activity. Thus, it may be possible to
Autor:
Pauli M. Turunen, Teppo O. Leino, Maiju K. Rinne, Yana Steynen, Erik A.A. Wallén, Jyrki P. Kukkonen, Ainoleena Turku, Henri Xhaard
One promising series of small-molecule orexin receptor agonists has been described, but the molecular pharmacological properties, i.e. ability and potency to activate the different orexin receptor-regulated signal pathways have not been reported for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9bb422f466296214348c1b5aa6d1038f
http://hdl.handle.net/10138/305214
http://hdl.handle.net/10138/305214