486449-62-1Relevant academic research and scientific papers
SAR-Guided Scoring Function and Mutational Validation Reveal the Binding Mode of CGS-8216 at the α1+/γ2- Benzodiazepine Site
Siebert, David C. B.,Wieder, Marcus,Schlener, Lydia,Scholze, Petra,Boresch, Stefan,Langer, Thierry,Schnürch, Michael,Mihovilovic, Marko D.,Richter, Lars,Ernst, Margot,Ecker, Gerhard F.
, p. 1682 - 1696 (2018)
The structural resolution of a bound ligand-receptor complex is a key asset to efficiently drive lead optimization in drug design. However, structural resolution of many drug targets still remains a challenging endeavor. In the absence of structural knowl
Novel immunomodulating compounds
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, (2008/06/13)
The present invention relates to a novel heterocyclic compound, a pharmaceutical composition comprisining said compound, a method and use of said compound for clinical treatment of medical conditions which may benefit from immunomodulation, e.g. rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28. A method of screening compounds for their ability of inhibiting ligand-induced co-stimulatory receptor internalisation pathways in immune competent human cells is described. Said immune competent human cells are incubated at conditions capable of inducing co-stimulatory receptor internalisation in the presence of at least one test compound and the suppression of the ligand-induced co-stimulatory receptor internalisation determined. There is also described a kit for use in such a method, as well as an immunoregulatory drug capable of blocking down-modulation of a ligand-induced receptor.
