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Small molecule drug screening in Drosophila identifies the 5HT2A receptor as a feeding modulation target
Gasque, Gabriel ; Conway, Stephen ; Huang, Juan ; Rao, Yi ; Vosshall, Leslie B.
刊名scientific reports
2013
关键词CAENORHABDITIS-ELEGANS SEROTONIN RECEPTOR FOOD-INTAKE FAT-BODY DIETARY RESTRICTION BRAIN REGULATION LIFE-SPAN MELANOGASTER GENETICS NEURONS
DOI10.1038/srep02120
英文摘要Dysregulation of eating behavior can lead to obesity, which affects 10% of the adult population worldwide and accounts for nearly 3 million deaths every year. Despite this burden on society, we currently lack effective pharmacological treatment options to regulate appetite. We used Drosophila melanogaster larvae to develop a high-throughput whole organism screen for drugs that modulate food intake. In a screen of 3630 small molecules, we identified the serotonin (5-hydroxytryptamine or 5-HT) receptor antagonist metitepine as a potent anorectic drug. Using cell-based assays we show that metitepine is an antagonist of all five Drosophila 5-HT receptors. We screened fly mutants for each of these receptors and found that serotonin receptor 5-HT2A is the sole molecular target for feeding inhibition by metitepine. These results highlight the conservation of molecular mechanisms controlling appetite and provide a method for unbiased whole-organism drug screens to identify novel drugs and molecular pathways modulating food intake.; Multidisciplinary Sciences; SCI(E); 5; ARTICLE; 3
语种英语
内容类型期刊论文
源URL[http://ir.pku.edu.cn/handle/20.500.11897/391338]  
专题生命科学学院
推荐引用方式
GB/T 7714
Gasque, Gabriel,Conway, Stephen,Huang, Juan,et al. Small molecule drug screening in Drosophila identifies the 5HT2A receptor as a feeding modulation target[J]. scientific reports,2013.
APA Gasque, Gabriel,Conway, Stephen,Huang, Juan,Rao, Yi,&Vosshall, Leslie B..(2013).Small molecule drug screening in Drosophila identifies the 5HT2A receptor as a feeding modulation target.scientific reports.
MLA Gasque, Gabriel,et al."Small molecule drug screening in Drosophila identifies the 5HT2A receptor as a feeding modulation target".scientific reports (2013).
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