Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Stefan M, Noha"'
Autor:
Stefan M. Noha, Chao Wang, Yan Niu, Hongyue Li, Dandan Xi, Fengrong Xu, Ping Xu, Veronika Temml, Daniela Schuster
Publikováno v:
European Journal of Medicinal Chemistry. 178:802-817
We report in this work the discovery of novel allosteric MEK inhibitors by pharmacophore modeling and virtual screening. Two out of 13 virtual hit compounds were identified as MEK kinase inhibitors using a MEK1 binding assay. Structural derivations o
Autor:
Atanas G Atanasov, Martina Blunder, Nanang Fakhrudin, Xin Liu, Stefan M Noha, Clemens Malainer, Matthias P Kramer, Amina Cocic, Olaf Kunert, Andreas Schinkovitz, Elke H Heiss, Daniela Schuster, Verena M Dirsch, Rudolf Bauer
Publikováno v:
PLoS ONE, Vol 8, Iss 4, p e61755 (2013)
Peroxisome proliferator-activated receptor gamma (PPARγ) is a key regulator of glucose and lipid metabolism and therefore an important pharmacological target to combat metabolic diseases. Since the currently used full PPARγ agonists display serious
Externí odkaz:
https://doaj.org/article/b576503ce8344f05a6585e83cfecfe37
Autor:
Maria, Dumitrascuta, Tanila, Ben Haddou, Elena, Guerrieri, Stefan M, Noha, Lea, Schläfer, Helmut, Schmidhammer, Mariana, Spetea
Publikováno v:
Journal of Medicinal Chemistry
Position 6 of the morphinan skeleton plays a key role in the μ-opioid receptor (MOR) activity in vitro and in vivo. We describe the consequence of the 6-carbonyl group deletion in N-methylmorphinan-6-ones 1–4 on ligand–MOR interaction, signaling
Publikováno v:
ACS Chemical Neuroscience
Among opioids, morphinans are of major importance as the most effective analgesic drugs acting primarily via μ-opioid receptor (μ-OR) activation. Our long-standing efforts in the field of opioid analgesics from the class of morphinans led to N-meth
Publikováno v:
Current Pharmaceutical Design. 19:7362-7372
The κ opioid receptor (KOR) plays a significant role in many physiological functions, including pain relief, stress, depression, drug abuse, anxiety and psychotic behaviors. KORs are widely distributed in the central and peripheral nervous systems,
Autor:
Stefan M Noha, Daniela Schuster
Publikováno v:
In SilicoDrug Discovery and Design. :80-93
Autor:
Oliver Werz, Stefan M. Noha, Antonella Peduto, Rosanna Filosa, Dagmar Barz, Daniela Schuster, Christina Weinigel, Heidi Traber, Anja M. Schaible, Veronika Temml
Publikováno v:
Biochemical Pharmacology. 86:476-486
Embelin (2,5-dihydroxy-3-undecyl-1,4-benzoquinone) possesses anti-inflammatory and anti-carcinogenic properties in vivo, and these features have been related to interference with multiple targets including XIAPs, NF kappa B, STAT-3, Akt and mTOR. How
Autor:
Stefan M. Noha, Oliver Werz, Daniela Schuster, Gerhard Wolber, Susanne Kuehnl, Judith M. Rollinger, Hermann Stuppner, Anja M. Schaible, Bianca Jazzar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters
Graphical abstract
The release of arachidonic acid, a precursor in the production of prostaglandins and leukotrienes, is achieved by activity of the cytosolic phospholipase A2α (cPLA2α). Signaling mediated by this class of bioactive lipids, wh
The release of arachidonic acid, a precursor in the production of prostaglandins and leukotrienes, is achieved by activity of the cytosolic phospholipase A2α (cPLA2α). Signaling mediated by this class of bioactive lipids, wh
Pharmacophore-based discovery of FXR agonists. Part I: Model development and experimental validation
Autor:
Hermann Stuppner, Valery N. Bochkov, Judith M. Rollinger, Ulrike Grienke, Patrick Markt, Stefan M. Noha, Daniela Schuster, Gerhard Wolber, Markus Binder, Judit Mihaly-Bison
Publikováno v:
Bioorganic & Medicinal Chemistry
Graphical abstract
The farnesoid X receptor (FXR) is involved in glucose and lipid metabolism regulation, which makes it an attractive target for the metabolic syndrome, dyslipidemia, atherosclerosis, and type 2 diabetes. In order to find novel
The farnesoid X receptor (FXR) is involved in glucose and lipid metabolism regulation, which makes it an attractive target for the metabolic syndrome, dyslipidemia, atherosclerosis, and type 2 diabetes. In order to find novel
Autor:
Hermann Stuppner, Gerhard Wolber, Judith M. Rollinger, Daniela Schuster, Julia Bauer, Oliver Werz, Stefan M. Noha, Patrick Markt, Katja Wiechmann, Birgit Waltenberger
Publikováno v:
Journal of Medicinal Chemistry. 54:3163-3174
Microsomal prostaglandin E2 synthase-1 (mPGES-1) catalyzes prostaglandin E2 formation and is considered as a potential anti-inflammatory pharmacological target. To identify novel chemical scaffolds active on this enzyme, two pharmacophore models for