利用磁珠加速的基于细胞的筛选快速鉴定食欲素受体结合配体。
Rapid identification of orexin receptor binding ligands using cell-based screening accelerated with magnetic beads.
作者信息
Qi Xin, Astle John, Kodadek Thomas
机构信息
Department of Chemistry, The Scripps Research Institute, Scripps Florida, 130 Scripps Way, #3A2, Jupiter, FL 33458, USA.
出版信息
Mol Biosyst. 2010 Jan;6(1):102-7. doi: 10.1039/b915611a. Epub 2009 Sep 29.
Abstract
We report here a simple and rapid method by which to screen one bead one compound libraries for highly specific ligands to cell surface proteins such as G protein-coupled receptors. This protocol, which harvests "hits" in a cell-based binding screen magnetically, eliminates the most tedious aspects of previously published bead screening techniques and allows millions of different compounds to be screened rapidly and cheaply. The method is demonstrated using the orexin receptor 1, which resulted in the isolation of moderate potency antagonists.
摘要
我们在此报告一种简单快速的方法，可用于从一珠一化合物文库中筛选针对细胞表面蛋白（如G蛋白偶联受体）的高特异性配体。该方案通过磁性方式在基于细胞的结合筛选中获取“命中”化合物，消除了先前公布的珠筛选技术中最繁琐的环节，并能快速且低成本地筛选数百万种不同化合物。我们使用食欲素受体1对该方法进行了验证，结果分离出了中等效力的拮抗剂。
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本文引用的文献
1
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.
J Med Chem. 2009 Feb 26;52(4):891-903. doi: 10.1021/jm801296d.
2
Enhanced orexin receptor-2 signaling prevents diet-induced obesity and improves leptin sensitivity.
Cell Metab. 2009 Jan 7;9(1):64-76. doi: 10.1016/j.cmet.2008.10.010.
3
Insular hypocretin transmission regulates nicotine reward.
Proc Natl Acad Sci U S A. 2008 Dec 9;105(49):19480-5. doi: 10.1073/pnas.0808023105. Epub 2008 Nov 24.
4
A peptoid "antibody surrogate" that antagonizes VEGF receptor 2 activity.
J Am Chem Soc. 2008 Apr 30;130(17):5744-52. doi: 10.1021/ja711193x. Epub 2008 Apr 2.
5
The neurohormone orexin stimulates hypoxia-inducible factor-1 activity.
Genes Dev. 2007 Nov 15;21(22):2995-3005. doi: 10.1101/gad.1584307.
6
Method for screening and MALDI-TOF MS sequencing of encoded combinatorial libraries.
Anal Chem. 2007 Oct 1;79(19):7275-85. doi: 10.1021/ac070418g. Epub 2007 Aug 23.
7
Promotion of sleep by targeting the orexin system in rats, dogs and humans.
Nat Med. 2007 Feb;13(2):150-5. doi: 10.1038/nm1544. Epub 2007 Jan 28.
8
Combinatorial chemistry identifies high-affinity peptidomimetics against alpha4beta1 integrin for in vivo tumor imaging.
Nat Chem Biol. 2006 Jul;2(7):381-9. doi: 10.1038/nchembio798. Epub 2006 Jun 11.
9
Design and synthesis of an optimized positional scanning library of peptoids: identification of novel multidrug resistance reversal agents.
Bioorg Med Chem. 2005 Mar 15;13(6):1923-9. doi: 10.1016/j.bmc.2005.01.024.
10
Isolation of protein ligands from large peptoid libraries.
J Am Chem Soc. 2003 Nov 19;125(46):13995-4004. doi: 10.1021/ja036417x.
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