Journal article
Development of a FLIPR Assay for the Simultaneous Identification of MrgD Agonists and Antagonists from a Single Screen
Journal of biomedicine & biotechnology, v 2010
2010
PMID: 20936132
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
MrgD, a member of the Mas-related gene family, is expressed exclusively in small diameter neurons in the dorsal root ganglion. This unique expression pattern, the presence of a single copy of MrgD in rodents and humans, and the identification of a putative ligand, beta-alanine, make it an experimentally attractive therapeutic target for pain with limited likelihood of side effects. We have devised a high throughput calcium mobilization assay that enables identification of both agonists and antagonists from a single screen for MrgD. Screening of the Library of Pharmacologically Active Compounds (LOPAC) validated this assay approach, and we identified both agonists and antagonists active at micromolar concentrations in MrgD expressing but not in parental CHO-DUKX cell line. Further characterization was performed using a subset of these screening hits. Our results demonstrated that the dual agonist/antagonist assay format is feasible and likely can be extended to most GPCRs with known agonist.
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Details
- Title
- Development of a FLIPR Assay for the Simultaneous Identification of MrgD Agonists and Antagonists from a Single Screen
- Creators
- Seena K Ajit - Department of Pharmacology and Physiology, Drexel University College of Medicine, 245 North 15th Street, MS number 488, Philadelphia, PA 19102, USA, Neuroscience Discovery, Pfizer Global Research and Development, CN 8000, Princeton, NJ 08543, USAMark H Pausch - Neuroscience Discovery, Pfizer Global Research and Development, CN 8000, Princeton, NJ 08543, USAJeffrey D Kennedy - Neuroscience Discovery, Pfizer Global Research and Development, CN 8000, Princeton, NJ 08543, USAEdward J Kaftan - Neuroscience Discovery, Pfizer Global Research and Development, CN 8000, Princeton, NJ 08543, USA
- Publication Details
- Journal of biomedicine & biotechnology, v 2010
- Publisher
- Wiley
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000283170200001
- Scopus ID
- 2-s2.0-77957836233
- Other Identifier
- 991014877899904721
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- Collaboration types
- Industry collaboration
- Domestic collaboration
- Web of Science research areas
- Biotechnology & Applied Microbiology
- Medicine, Research & Experimental