Label-free cell phenotypic profiling and pathway deconvolution of neurotensin receptor-1
文献类型：期刊论文
| 作者 | Hou, Tao2; Shi, Liying3; Wang, Jixia2; Wei, Lai2; Qu, Lala2; Zhang, Xiuli1,2; Liang, Xinmiao2 |
| 刊名 | PHARMACOLOGICAL RESEARCH
 |
| 出版日期 | 2016-06-01 |
| 卷号 | 108页码:39-45 |
| 关键词 | Neurotensin Receptor-1 Pathway Label-free Cell Phenotypic Profiling Biased Agonism |
| ISSN号 | 1043-6618 |
| DOI | 10.1016/j.phrs.2016.04.018 |
| 文献子类 | Article |
| 英文摘要 | Neurotensin (NT), an endogenous peptide found in the central nervous system and in peripheral tissues, contributes to the pathophysiology of neurodegenerative and psychiatric diseases, cancer, inflammation, and immunomodulatory disease. NT exerts its physiological effects predominantly through its cognate high-affinity neurotensin receptor-1 (NTS1). NTS1 emerges as a druggable target; however, there are limited numbers of NTS1 active compounds reported to date. Here we reported a label-free cell phenotypic profiling model for screening NTS1 ligands and differentiating their biased agonism. Resonant waveguide grating enabled dynamic mass redistribution (DMR) assay was first optimized against cell confluency and then used to characterize the endogenous NTS1 in HT-29 cell using known agonists and antagonists. Pathway modulators were also used to deconvolute the signaling pathways of endogenous NTS1. Results showed that the NTS1 DMR assay is robust for screening and can differentiate biased agonism; and the activation of NTS1 in HT-29 triggers multiple pathways including G(q) signaling and epidermal growth factor receptor transactivation. This study highlighted the power of label-free DMR assay to characterize receptor signaling and pharmacology of distinct classes of ligands for NTS1, G protein-coupled receptors in general. (C) 2016 Elsevier Ltd. All rights reserved. |
| WOS关键词 | LUNG-CANCER CELLS ; PROTEIN-KINASE-C ; DOWN-REGULATION ; CALCIUM MOBILIZATION ; OPTICAL BIOSENSORS ; N1E-115 CELLS ; DNA-SYNTHESIS ; EGF-RECEPTOR ; GROWTH ; ACTIVATION |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000377729600006 |
| 出版者 | ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/170548]  |
| 专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
| 通讯作者 | Zhang, Xiuli; Liang, Xinmiao |
| 作者单位 | 1.Nantong Univ, Coinnovat Ctr Neuroregenerat, Nantong 226019, Peoples R China 2.Chinese Acad Sci, Dalian Inst Chem Phys, Key Lab Separat Sci Analyt Chem, Dalian 116023, Liaoning, Peoples R China 3.Dalian Univ, Bioengn Coll, Dalian 116622, Liaoning, Peoples R China |
| 推荐引用方式 GB/T 7714 | Hou, Tao,Shi, Liying,Wang, Jixia,et al. Label-free cell phenotypic profiling and pathway deconvolution of neurotensin receptor-1[J]. PHARMACOLOGICAL RESEARCH,2016,108:39-45. |
| APA | Hou, Tao.,Shi, Liying.,Wang, Jixia.,Wei, Lai.,Qu, Lala.,...&Liang, Xinmiao.(2016).Label-free cell phenotypic profiling and pathway deconvolution of neurotensin receptor-1.PHARMACOLOGICAL RESEARCH,108,39-45. |
| MLA | Hou, Tao,et al."Label-free cell phenotypic profiling and pathway deconvolution of neurotensin receptor-1".PHARMACOLOGICAL RESEARCH 108(2016):39-45. |
入库方式： OAI收割
来源：大连化学物理研究所
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