کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8633868 | 1569062 | 2016 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Ala5-galanin (2-11) is a GAL2R specific galanin analogue
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کلمات کلیدی
GPCRsGalanin receptor 2p-methylbenzhydrylamineMBHA9-FluorenylmethyloxycarbonylHKRFMOCGIPforskolinGPCRPBSFskSARFBSG-protein coupled receptors - G-پروتئین گیرنده های متصل شدهinositol phosphate - inositol فسفاتAgonist - آگونیستEDTA - اتیلن دی آمین تترا استیک اسید Ethylenediaminetetraacetic acid - اتیلینیدامین تتراستیک اسیدImpedance - امپدانسdynamic mass redistribution - توزیع مجدد جرم پویاCNS - دستگاه عصبی مرکزیSarcosine - سارکوزینBBB - سد خونی مغزیfetal bovine serum - سرم جنین گاوCHO cells - سلول های CHOChinese hamster ovary cells - سلول های تخمدان هامستر چینیcentral nervous system - سیستم عصبی مرکزیperipheral nervous system - سیستم عصبی پیرامونیBlood-brain barrier - مانع خون مغزیPhosphate-buffered saline - محلول نمک فسفات با خاصیت بافریNeuropeptide - نوروپپتیدPNS - کارمندان دولتhigh performance liquid chromatography - کروماتوگرافی مایع با کارایی بالاHPLC - کروماتوگرافی مایعی کاراGalanin - گالانینGalanin receptor 1 - گیرنده گالانین 1
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
علوم غدد
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
It is over 30Â years since the regulatory peptide galanin was discovered by Professor Mutt and co-workers. Galanin exerts its effects by binding to three galanin G-protein coupled receptors, namely GAL1R, GAL2R and GAL3R. Each galanin receptor has a different distribution in the central nervous system and the peripheral nervous system as well as distinctive signaling pathways, which implicates that the receptors are involved in different biological- and pathological effects. The delineation of the galaninergic system is however difficult due to a lack of stable, specific galanin receptor ligands. Herein, a new short GAL2R specific ligand, Ala5-galanin (2-11), is presented. The galanin (2-11) modified analogue Ala5-galanin (2-11) was tested in 125I-galanin competitive binding studies for the three galanin receptors and the G-protein coupled receptor signaling properties was tested by the ability to influence second-messenger molecules like inositol phosphate and cyclic adenosine monophosphate. In addition, two different label-free real-time assays, namely EnSpire® based on an optical biosensor and xCELLigence® based on an electric biosensor, were used for evaluating the signaling properties using cell lines with different levels of receptor expression. Ala5-galanin (2-11) was subsequently found to be a full agonist for GAL2R with more than 375-fold preference for GAL2R compared to both GAL1R and GAL3R. The single amino acid substitution of serine to alanine at position 5 in the short ligand galanin (2-11) resulted in a ligand subsequently unable to bind neither GAL3R nor GAL1R, even at concentrations as high as 0.1Â mM.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Neuropeptides - Volume 60, December 2016, Pages 75-82
Journal: Neuropeptides - Volume 60, December 2016, Pages 75-82
نویسندگان
Kristin Webling, Johan Runesson, Andreas Lang, Indrek Saar, Barbara Kofler, Ãlo Langel,