Acta pharmacologica Sinica, 2015-07, Vol.36 (7), p.874-878
2015
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Details
- Autor(en) / Beteiligte
- Titel
- High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139
- Ist Teil von
- Acta pharmacologica Sinica, 2015-07, Vol.36 (7), p.874-878
- Ort / Verlag
- United States: Nature Publishing Group
- Erscheinungsjahr
- 2015
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Aim： To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules. Methods： Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies. Results： Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds. Conclusion： The findings provide important tools for further study of this orphan G-protein coupled receptor.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1671-4083eISSN: 1745-7254DOI: 10.1038/aps.2015.12Titel-ID: cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_4648122
- Format
- –
- Schlagworte
- Animals, Calcium - metabolism, CHO Cells, Cricetinae, Cricetulus, Dose-Response Relationship, Drug, Drug Evaluation, Preclinical - methods, High-Throughput Screening Assays - methods, Humans, Nerve Tissue Proteins - antagonists & inhibitors, Nerve Tissue Proteins - metabolism, Original, Receptors, G-Protein-Coupled - antagonists & inhibitors, Receptors, G-Protein-Coupled - metabolism, 受体拮抗剂, 合成化合物, 吞吐量, 孤儿G蛋白偶联受体, 小分子, 钙动员, 高通量筛选