Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Per Hillertz"'
Autor:
Göran Dahl, Bernd Kappler, Anna Tigerström, Annette Brodte, Fredrik Edfeldt, Philip B. Rawlins, Anders Egnéus, Geoff Holdgate, Rutger H. A. Folmer, Gareth M. Davies, Stephan Steigele, Eva-Lotta Westberg, Stephan Heyse, Nichole O'Connell, Martin Ginkel, Per Hillertz, Alexander Mehrle
Publikováno v:
Slas Discovery
Surface plasmon resonance (SPR) is a powerful method for obtaining detailed molecular interaction parameters. Modern instrumentation with its increased throughput has enabled routine screening by SPR in hit-to-lead and lead optimization programs, and
Autor:
Anders Jerre, Håkan Bladh, Stefan Bäckström, Karl Edman, Matti Lepistö, Amir Smailagic, Ann Tjörnebo, Jan Dahmén, John D. Taylor, Liz Kinchin, Stinabritt Nilsson, Krister Henriksson, Per Hillertz, Vijakumar Hulikal, Charlotte Kåse, Ragnhild Ahlgren, Malena Bengtsson, Irene Mile, Thomas Hansson, Lisa Wissler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2571-2577
We report the discovery of highly potent and selective non-steroidal glucocorticoid receptor modulators with PK properties suitable for inhalation. A high throughput screen of the AstraZeneca compound collection identified sulfonamide 3 as a potent n
Autor:
Xin Wang, Magdalena Mazurkiewicz, Ellin-Kristina Hillert, Maria Hägg Olofsson, Stefan Pierrou, Per Hillertz, Joachim Gullbo, Karthik Selvaraju, Aneel Paulus, Sharoon Akhtar, Felicitas Bossler, Asher Chanan Khan, Stig Linder, Padraig D’Arcy
Publikováno v:
Scientific Reports
Inhibition of deubiquitinase (DUB) activity is a promising strategy for cancer therapy. VLX1570 is an inhibitor of proteasome DUB activity currently in clinical trials for relapsed multiple myeloma. Here we show that VLX1570 binds to and inhibits the
Publikováno v:
ChemMedChem. 11(17)
The retinoic-acid-related orphan receptor γ t (RORγt), as a master regulator of Th17 cell pathology, has become an attractive target for small-molecule drug discovery for the treatment of Th17-cell-related autoimmune diseases. A crystallographic fr
Autor:
Niek Dekker, Annemarie Beate Wöhri, Johan Meuller, Arjan Snijder, Per Hillertz, Per-Olof Eriksson
Publikováno v:
Molecular Membrane Biology. 30:169-183
In this work, we describe a process for production of a Pichia pastoris strain which overproduces large quantities of the human glycine receptor. Subsequent purification yielded functional, uniform protein with expression yields of up to 5 mg per lit
Publikováno v:
Proceedings of the National Academy of Sciences. 104:14658-14663
Better understanding of the fundamental mechanisms behind metabolic diseases requires methods to monitor lipid stores on single-cell level in vivo . We have used Caenorhabditis elegans as a model organism to demonstrate the limitations of fluorescenc
Autor:
Per Hillertz, Fritz Schweikart, Lisa Wissler, Yanlong Zhao, Paul T. Wan, Niek Dekker, Yafeng Xue
Publikováno v:
ChemMedChem. 8(11)
Tau-tubulin kinase 1 (TTBK1) is a serine/threonine/tyrosine kinase that putatively phosphorylates residues including S422 in tau protein. Hyperphosphorylation of tau protein is the primary cause of tau pathology and neuronal death associated with Alz
Autor:
Tomas Akerud, Henrik Andersson, Shephali Trivedi, Didier Rottici, Kai Sun, Anna Ridderstad Wollberg, Kristian Sandberg, Magdalena Otrocka, Pontus Forsell, Lina Eisele, Per Hillertz, Helena Almqvist, Niek Dekker
Publikováno v:
Journal of biomolecular screening. 18(6)
The TrkA-PathHunter cell-based assay was used in high-throughput screening (HTS) to identify compounds that inhibit nerve growth factor (NGF)/TrkA signaling. The assay was conducted in a 384-well format, and typical Z' values during HTS ranged from 0
Autor:
Per Hillertz, Eric Valeur, Christine Charon, Didier Roche, Serge Christmann-Franck, Djordje Musil, Denis Carniato, Liliane Doare, Sophie Bozec, Fabien Schmidlin, Melanie Schultz, Cravo Daniel, Franck F. Lepifre, Marc Lecomte
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(18)
Indole-pyrrolidines were identified as inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) by high-throughput screening. Optimisation of the initial hit through structure-based design led to 7-azaindole-derivatives, with the best analo
Publikováno v:
SPIE Proceedings.
We introduce near-infrared Coherent Anti-Stokes Raman Scattering (CARS) microscopy as a method for the monitoring of fat deposition in a living organism by directly probing the CH 2 vibration of the lipids without the need for staining or labeling. T