Identification of the first small-molecule ligand of the neuronal receptor sortilin and structure determination of the receptor-ligand complex

AndersenJ.L.; Schr?derT.J.; ChristensenS.Strandbyg?rdD.PallesenL.T.García-AlaiM.M.LindbergS.Langg?rdM.EskildsenJ.C.DavidL.TagmoseL.SimonsenK.B.MaltasP.J.R?nnL.C.B.DeJongI.E.M.MalikI.J.EgebjergJ.KarlssonJ.-J.UppalanchiS.SakumudiD.R.EradiP.WatsonS.P.ThirupS.

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Identification of the first small-molecule ligand of the neuronal receptor sortilin and structure determination of the receptor-ligand complex

机译：第一个小分子配体的识别的神经受体sortilin和结构确定receptor-ligand复杂

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Sortilin is a type I membrane glycoprotein belonging to the vacuolar protein sorting 10 protein (Vps10p) family of sorting receptors and is most abundantly expressed in the central nervous system. Sortilin has emerged as a key player in the regulation of neuronal viability and has been implicated as a possible therapeutic target in a range of disorders. Here, the identification of AF40431, the first reported small-molecule ligand of sortilin, is reported. Crystals of the sortilin-AF40431 complex were obtained by co-crystallization and the structure of the complex was solved to 2.7 ? resolution. AF40431 is bound in the neurotensin-binding site of sortilin, with the leucine moiety of AF40431 mimicking the binding mode of the C-terminal leucine of neurotensin and the 4-methyl-umbelliferone moiety of AF40431 forming π-stacking with a phenylalanine.

机译：Sortilin I型膜糖蛋白属于空泡的蛋白分类10蛋白(Vps10p)受体和排序的家庭最丰富的表达在中央神经系统调节神经元生存能力,作为一个可能的治疗目标的障碍。识别AF40431,第一个报道sortilin小分子配体的报道。晶体的sortilin-AF40431复杂通过co-crystallization和结构解决了复杂的2.7吗?AF40431势必neurotensin-binding网站sortilin,亮氨酸AF40431的一部分模仿的绑定模式c端神经降压素和亮氨酸4-methyl-umbelliferone AF40431形成的一部分苯丙氨酸π堆积。

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《Acta crystallographica.Section D Biological crystallography.》 |2014年第2期|451-460|共10页
作者
AndersenJ.L.; Schr?derT.J.; ChristensenS.Strandbyg?rdD.PallesenL.T.García-AlaiM.M.LindbergS.Langg?rdM.EskildsenJ.C.DavidL.TagmoseL.SimonsenK.B.MaltasP.J.R?nnL.C.B.DeJongI.E.M.MalikI.J.EgebjergJ.KarlssonJ.-J.UppalanchiS.SakumudiD.R.EradiP.WatsonS.P.ThirupS.;
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作者单位

Lundbeck Foundation Research Centre MIND, Department of Biomedicine, Aarhus University, Ole Worms;

Neuroscience Drug Discovery, H. Lundbeck A/S, Ottiliavej 9, 2500 Valby, Denmark;

Medicinal Chemistry, GVK BioScience, IDA Nacharam, Plot No. 28 A, Hyderabad 500 076, IndiaLundbeck Foundation Research Centre MIND, Department of Molecular Biology and Genetics, Aarhus;

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正文语种英语
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关键词
sortilin; small molecule;

机译：sortilin small molecule);

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Identification of the first small-molecule ligand of the neuronal receptor sortilin and structure determination of the receptor-ligand complex

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