Affiliation: Schering AG
- Insight into the molecular mechanisms of glucocorticoid receptor action promotes identification of novel ligands with an improved therapeutic indexHeike Schäcke
CRBA Inflammation, Corporate Research, Schering AG, Berlin, Germany
Exp Dermatol 15:565-73. 2006..Nevertheless, considerable improvement in the therapeutic action of glucocorticoid receptor ligands is being achieved through the use of key molecular targets for screening novel glucocorticoid receptor ligands...
- Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effectsHeike Schäcke
Corporate Research Business Area Dermatology, Corporate Project Management Strategic Business Unit Specialized Therapeutics, and Medicinal Chemistry, Schering AG, Berlin, D 13342 Berlin, Germany
Proc Natl Acad Sci U S A 101:227-32. 2004..Moreover, they are useful tool compounds for further investigating the mechanisms of GR-mediated effects...
- Dissociated glucocorticoid receptor ligandsHeike Schäcke
Schering AG, Corporate Research, Mullerstrasse 178, 13342 Berlin, Germany
Curr Opin Investig Drugs 5:524-8. 2004..Several pharmaceutical companies are currently pursuing this goal...
- Selective glucocorticoid receptor agonists (SEGRAs): novel ligands with an improved therapeutic indexHeike Schäcke
Bayer Schering Pharma AG, Global Drug Discovery, TRG Inflammation Immunology, Müllerstr 178, 13342 Berlin, Germany
Mol Cell Endocrinol 275:109-17. 2007..Such selective GR agonists (SEGRAs) are likely to enter clinical testing soon...
- Dissociated glucocorticoid receptor ligands: compounds with an improved therapeutic indexHeike Schäcke
Schering AG, RBA Dermatology Europe, 13342 Berlin, Germany
Curr Opin Investig Drugs 6:503-7. 2005..Compounds that preferentially induce transrepression rather than transactivation should be superior to classical glucocorticoids. Indeed, proof of concept has been recently achieved with such selective glucocorticoid receptor agonists...
- Mechanisms involved in the side effects of glucocorticoidsHeike Schäcke
Research Business Area Dermatology, Schering AG, D 13342, Berlin, Germany
Pharmacol Ther 96:23-43. 2002..The focus on the molecular aspects should be helpful in predicting the potential advantages of selective GR agonists in comparison to classical GCs...
- GR ligands: can we improve the established drugs?Hartmut Rehwinkel
Schering AG, Corporate Research, Medicinal Chemistry, 13342 Berlin, Germany
ChemMedChem 1:803-5. 2006
- Discovery of quinolines as selective glucocorticoid receptor agonistsStefan Jaroch
Medicinal Chemistry Berlin, Lead Generation and Optimization, Bayer Schering Pharma AG, Berlin D 13342, Germany
Bioorg Med Chem Lett 20:5835-8. 2010..Compounds were shown to be efficacious in cell assays with respect to inflammation endpoints, along with reduced activity in a transactivation assay, hinting at an improved therapeutic window over corticosteroids...
- Effects of a selective glucocorticoid receptor agonist on experimental keratoplastyUwe Pleyer
Department of Ophthalmology, Institute of Pharmacy, Charite, Humboldt University, Berlin, Germany
Graefes Arch Clin Exp Ophthalmol 243:450-5. 2005..We set out to evaluate the effect of a SEGRA compound following topical application on the course of experimental orthotopic corneal grafts...
- Shortened treatment duration of glucocorticoid-induced skin atrophy in ratsStefanie Schoepe
Exp Dermatol 20:853-5. 2011..We show here that the treatment duration of rat skin atrophy models might be reduced to 5 days for economical and ethical reasons...