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The main focus of my group is development of state-of-the-art molecular pharmacological assays for G protein-coupled receptors and ionotropic glutamate receptors. These assays are being used to characterize ligands primarly synthesized at the Department of Drug Design and Pharmacology with special focus on subtype selectivity of the ligands and development of ligands with novel pharmacological profiles (e.g. pathway biased ligands and allosteric modulators). In this way several subtype specific/selective ligands have been identified. Another interest is ligand-receptor interactions, subtype selectivity and the activation mechanisms of receptors. These aspects have been investigated by integrated use of point-mutations, random saturation mutagenesis, chimeric receptors, engineered zinc-sites and molecular modelling.
Orphan receptors, for which the endogenous ligands remains to be identified, are also a focus area of my group. Using bioinformatics and molecular biological tools, we screen focused compound libraries for endogenous and surrogate ligands. Recently, we were the first to report the endogenous agonists for the human GPRC6A and GPR139 G-protein coupled receptors. We are currently using a GPRC6A and GPR139 knockout mouse to unravel the physiological function and therapeutic prospect of these new exciting receptors.
Most recently, my group has engaged in the use of chemogenomics and virtual screening for identification of novel pharmacological tool compounds as for example our recent discovery of the most selective GPRC6A receptor and GluN3 antagonists and GPR132 agonist reported to date.
The majority of projects are run in close collaboration with computational and medicinal chemists.
Possible conflicts of interest
Member of the board of the Alfred Benzon Foundation.
Research interests
The main focus of my group is development of state-of-the-art molecular pharmacological assays for G protein-coupled receptors and ionotropic glutamate receptors. These assays are being used to characterize ligands primarly synthesized at the Department of Drug Design and Pharmacology with special focus on subtype selectivity of the ligands and development of ligands with novel pharmacological profiles (e.g. pathway biased ligands and allosteric modulators). In this way several subtype specific/selective ligands have been identified. Another interest is ligand-receptor interactions, subtype selectivity and the activation mechanisms of receptors. These aspects have been investigated by integrated use of point-mutations, random saturation mutagenesis, chimeric receptors, engineered zinc-sites and molecular modelling.
Orphan receptors, for which the endogenous ligands remains to be identified, are also a focus area of my group. Using bioinformatics and molecular biological tools, we screen focused compound libraries for endogenous and surrogate ligands. Recently, we were the first to report the endogenous agonists for the human GPRC6A and GPR139 G-protein coupled receptors. We are currently using a GPRC6A and GPR139 knockout mouse to unravel the physiological function and therapeutic prospect of these new exciting receptors.
Most recently, my group has engaged in the use of chemogenomics and virtual screening for identification of novel pharmacological tool compounds as for example our recent discovery of the most selective GPRC6A receptor and GluN3 antagonists and GPR132 agonist reported to date.
The majority of projects are run in close collaboration with computational and medicinal chemists.
Possible conflicts of interest
Member of the board of the Alfred Benzon Foundation.
研究兴趣
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FEBS lettersno. 11 (2023): 1528-1540
Basic & clinical pharmacology & toxicologyno. 6 (2023): 459-471
IUPHAR/BPS guide to pharmacology CITEno. 1 (2023)
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IUPHAR/BPS guide to pharmacology CITEno. 1 (2023)
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bioRxiv (Cold Spring Harbor Laboratory)no. 12 (2022): eabk1410-eabk1410
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