کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10586727 | 981395 | 2011 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A sucrose-derived scaffold for multimerization of bioactive peptides
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کلمات کلیدی
TLCMSH4BOCFMOCMC4RHOBtCCK2RDTPACuAACHRMStert-butoxycarbonyltert-butylEC50TFACCK4Cl-HOBttris[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]amineDMFdiisopropyl carbodiimideDMEMESIDCMTBTATRFTHFDICCopper(I)-catalyzed azide-alkyne cycloaddition1-hydroxybenzotriazole - 1-هیدروکسی بنزوتریازول6-chloro-1-hydroxybenzotriazole - 6-کلرو-1-هیدروکسی بنزوتریازولBSA - BSAMALDI–TOF - MALDI-TOFDulbecco’s modified Eagle medium - Modified Eagle اصلاح شده DulbeccoN,N-dimethylformamide - N، N-dimethylformamidebovine serum albumin - آلبومین سرم گاوTrifluoroacetic acid - اسید TrifluoroaceticTetrahydrofuran - تتراهیدروفورانt-Bu - تی بوminimum essential medium - حداقل حداقل مورد نیازDiethylenetriaminepentaacetic acid - دی اتیلنتریمین پنتا اسیدهای اسیدDichloromethane - دیکلورمتانHigh resolution mass spectroscopy - طیف سنجی جرمی با وضوح بالاTime-resolved fluorescence - فلورسانس حل شده در زمانMEM - مامانthin-layer chromatography - کروماتوگرافی نازک لایهcholecystokinin 2 receptor - کولسیستوکینین 2 گیرندهmelanocortin 4 receptor - گیرنده ملانوکورتین 4electrospray ionization - یونیزاسیون الکترو اسپری
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A spherical molecular scaffold bearing eight terminal alkyne groups was synthesized in one step from sucrose. One or more copies of a tetrapeptide azide, either N3(CH2)5(CO)-His-DPhe-Arg-Trp-NH2 (MSH4) or N3(CH2)5(CO)-Trp-Met-Asp-Phe-NH2 (CCK4), were attached to the scaffold via the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. Competitive binding assays using Eu-labeled probes based on the superpotent ligands Ser-Tyr-Ser-Nle-Glu-His-DPhe-Arg-Trp-Gly-Lys-Pro-Val-NH2 (NDP-α-MSH) and Asp-Tyr-Met-Gly-Trp-Met-Asp-Phe-NH2 (CCK8) were used to study the interactions of monovalent and multivalent MSH4 and CCK4 constructs with Hek293 cells engineered to overexpress MC4R and CCK2R. All of the monovalent and multivalent MSH4 constructs exhibited binding comparable to that of the parental ligand, suggesting that either the ligand spacing was inappropriate for multivalent binding, or MSH4 is too weak a binder for a second 'anchoring' binding event to occur before the monovalently-bound construct is released from the cell surface. In contrast with this behavior, monovalent CCK4 constructs were significantly less potent than the parental ligand, while multivalent CCK4 constructs were as or more potent than the parental ligand. These results are suggestive of multivalent binding, which may be due to increased residence times for monovalently bound CCK4 constructs on the cell surface relative to MSH4 constructs, the greater residence time being necessary for the establishment of multivalent binding.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 21, 1 November 2011, Pages 6474-6482
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 21, 1 November 2011, Pages 6474-6482
نویسندگان
Venkataramanarao Rao, Ramesh Alleti, Liping Xu, Narges K. Tafreshi, David L. Morse, Robert J. Gillies, Eugene A. Mash,