Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Linda Öster"'
Autor:
Ola Fjellström, Sibel Akkaya, Hans-Georg Beisel, Per-Olof Eriksson, Karl Erixon, David Gustafsson, Ulrik Jurva, Daiwu Kang, David Karis, Wolfgang Knecht, Viveca Nerme, Ingemar Nilsson, Thomas Olsson, Alma Redzic, Robert Roth, Jenny Sandmark, Anna Tigerström, Linda Öster
Publikováno v:
PLoS ONE, Vol 10, Iss 1, p e0113705 (2015)
Activated factor XI (FXIa) inhibitors are anticipated to combine anticoagulant and profibrinolytic effects with a low bleeding risk. This motivated a structure aided fragment based lead generation campaign to create novel FXIa inhibitor leads. A virt
Externí odkaz:
https://doaj.org/article/1a2cc35337574e84979292e3f9e6ec05
Autor:
Lena Ripa, Josefine Pemberton, Fredrik Edfeldt, Ulf Börjesson, Magnus Nilsson, R. Ian Storer, Paolo Di Fruscia, Gavin W. Collie, Louise Barlind, Anna Aagaard, Linda Öster, Helena Käck, Eva L. Hansson, Igor L. Shamovsky, Richard J. Lewis
Publikováno v:
ACS Med Chem Lett
[Image: see text] The MEK1 kinase plays a critical role in key cellular processes, and as such, its dysfunction is strongly linked to several human diseases, particularly cancer. MEK1 has consequently received considerable attention as a drug target,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32e123e9ce780e990c54c74a7c8c4a07
https://doi.org/10.1021/acsmedchemlett.0c00563
https://doi.org/10.1021/acsmedchemlett.0c00563
Publikováno v:
European journal of medicinal chemistry. 227
Inhibition of mucosa-associated lymphoid tissue lymphoma translocation protein-1 (MALT1) is a promising strategy to modulate NF-κB signaling, with the potential to treat B-cell lymphoma and autoimmune diseases. We describe the discovery and optimiza
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5085d83f97e829c60839c3e4117e20f6
https://pubmed.ncbi.nlm.nih.gov/34742013
https://pubmed.ncbi.nlm.nih.gov/34742013
Autor:
Christian Tyrchan, Anna-Pia Palmgren, Hui-Fang Amy Chang, Yunhua Chen, Victoria Ullah, Karin Björhall, Annika Westin Eriksson, Rebecca Fransson, Mickael Mogemark, Tiiu Wennberg, Shuchun Zhao, Bold Peter, Linda Fredlund, Matthew Thomas, Eva Lamm Bergström, Nils Pemberton, Ulf Börjesson, Reed W. Smith, Mikael Brűlls, Johan Carlsson, Britt-Marie Fihn, Linda Öster, Mio Rodrigo Blomqvist, Hongbin Ge, Antonios Nikitidis, Wenzhen Yang, Anders Eriksson, Haijuan Huang, Sarah Lever, Perry Matthew, Kostas Karabelas, Helena Lindmark, Jens Petersen
Publikováno v:
Journal of medicinal chemistry. 64(12)
Starting from our previously described PI3Kγ inhibitors, we describe the exploration of structure-activity relationships that led to the discovery of highly potent dual PI3Kγδ inhibitors. We explored changes in two positions of the molecules, incl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f1afe7cc480e1edf37ab207774eb9ff
https://pubmed.ncbi.nlm.nih.gov/34080862
https://pubmed.ncbi.nlm.nih.gov/34080862
Autor:
Tomas Akerud, Bingze Xu, Göran Dahl, Robert G. Roth, Patrik Johansson, Anna Aagaard, Maria Sörhede Winzell, Janna M. Bigalke, G. Jonah A. Rainey, Jenny Sandmark, Pia Davidsson, Linda Öster
Publikováno v:
Journal of Biological Chemistry. 293:5492-5508
Neurturin (NRTN) provides trophic support to neurons and is considered a therapeutic agent for neurodegenerative diseases, such as Parkinson's disease. It binds to its co-receptor GFRa2, and the resulting NRTN–GFRa2 complex activates the transmembr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f03dc7b12e7a3f6af84b761a8ee197bd
https://doi.org/10.1074/jbc.ra117.000820
https://doi.org/10.1074/jbc.ra117.000820
Autor:
Linda Öster, Helena Lindmark, Ina Terstiege, Jens Petersen, Perry Matthew, Tor Svensson, Christian Tyrchan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:679-687
A novel class of potent PI3Kδ inhibitors with >1000-fold selectivity against other class I PI3K isoforms is described. Optimization of the substituents on a triazole aminopyrazine scaffold, emerging from an in-house PI3Kα program, turned moderately
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::667d8560a853b5dcb7cb3313026d3553
https://doi.org/10.1016/j.bmcl.2016.11.004
https://doi.org/10.1016/j.bmcl.2016.11.004
Autor:
David Karis, Hans-Georg Beisel, Carina A Johansson, Stefan Bäckström, Tommy Olsson, Mattias Rohman, Linda Öster, Yafeng Xue
Publikováno v:
ChemMedChem. 11:497-508
Soluble epoxide hydrolase (sEH) is involved in the regulation of many biological processes by metabolizing the key bioactive lipid mediator, epoxyeicosatrienoic acids. For the development of sEH inhibitors with improved physicochemical properties, we
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5a58720ee4e95e22a7192dc785d829e
https://doi.org/10.1002/cmdc.201500575
https://doi.org/10.1002/cmdc.201500575
Autor:
Gangadhara Gangadhara, Nils Pemberton, Kostas Karabelas, Rebecca Rae, Mickael Mogemark, Christian Tyrchan, Tineke Papavoine, Göran Dahl, Perry Matthew, Helena Lindmark, Stefan Blaho, Linda Öster, Jenny Gunnarsson, Thomas Bohnacker, Matthias P. Wymann, Jens Petersen, Roger L. Williams
Publikováno v:
Nature chemical biology. 15(4)
We have discovered a class of PI3Kγ inhibitors exhibiting over 1,000-fold selectivity over PI3Kα and PI3Kβ. On the basis of X-ray crystallography, hydrogen-deuterium exchange-mass spectrometry and surface plasmon resonance experiments we propose t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46f86620bb7e981497d01936b9b6e091
https://pubmed.ncbi.nlm.nih.gov/30718815
https://pubmed.ncbi.nlm.nih.gov/30718815
Autor:
Nils Pemberton, Cristina Gardelli, Jens Petersen, Neil S. Holden, Helena Lindmark, Pavol Zlatoidsky, Sandra Rodrigo Blomqvist, Annika Westin Eriksson, Rhona J. Cox, Linda Öster, Christian Tyrchan, Susanne Arlbrandt, Sarah Lever, Perry Matthew, Bold Peter, Mickael Mogemark, Matthew F. Thomas, A. Monica Norberg, Kostas Karabelas, Johan Karlsson, Xueshan Li
Publikováno v:
'Journal of Medicinal Chemistry ', vol: 61, pages: 5435-5441 (2018)
In this paper, we describe the discovery and optimization of a new chemotype of isoform selective PI3Kγ inhibitors. Starting from an HTS hit, potency and physicochemical properties could be improved to give compounds such as 15, which is a potent an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::522cd582a4e8dd33b4cac2f260c043ff
https://pubmed.ncbi.nlm.nih.gov/29852070
https://pubmed.ncbi.nlm.nih.gov/29852070
Publikováno v:
Drug Discovery Today. 20:1104-1111
Fragment-based drug discovery relies upon structural information for efficient compound progression, yet it is often challenging to generate structures with bound fragments. A summary of recent literature reveals that a wide repertoire of experimenta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72adecd32284810a72da8b42c939767c
https://doi.org/10.1016/j.drudis.2015.04.005
https://doi.org/10.1016/j.drudis.2015.04.005