Synthesis of guanidinium-Derived Receptor Libraries and Screening for Selective Peptide Receptors in Water

Kim B. Jensen; Tobias M. Braxmeier; Mariangela Demarcus; Jeremy G. Frey; Jeremy D. Kilburn

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Synthesis of guanidinium-Derived Receptor Libraries and Screening for Selective Peptide Receptors in Water

机译：胍基受体文库的合成及水中选择性肽受体的筛选

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A library of "tweezer" receptors, incorporating a guanidinium "head group" and two peptide derived side arms has been prepared on the solidphase using an orthogonally protected guanidinium scaffold 12. The library wasscreened with various tripeptide derivatives in an aqueous solvent system. A tweezer receptor 25 for the side chain protected tripeptide 19 was identified from the screening experiments. Receptor 25 was resynthesised and solution binding studies were carried out, which revealed that 25 binds to tripeptide 19 with K_a=8.2X10~4+-2.5X10~4 (15% DMSO/H_2O, pH8.75) and with appreciable selectivity over the tripeptide enantiomer 22 and the side chain deprotected tripeptide 20.

机译：已经使用正交保护的胍支架12在固相上制备了包含镊子“头部基团”和两个肽衍生的侧臂的“镊子”受体文库。该文库在水性溶剂系统中用各种三肽衍生物筛选。从筛选实验中鉴定出用于侧链保护的三肽19的镊子受体25。重新合成了受体25，并进行了溶液结合研究，结果表明25与三肽19结合，K_a = 8.2X10〜4 + -2.5X10〜4（15％DMSO / H_2O，pH8.75），并且在三肽对映体22和侧链去保护三肽20。

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《Chemistry: A European journal》 |2002年第6期|共10页
作者
Kim B. Jensen; Tobias M. Braxmeier; Mariangela Demarcus; Jeremy G. Frey; Jeremy D. Kilburn;
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正文语种 eng
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combinatorial chemistry; guanidinium; peptides; receptors; screening;

机译：组合化学胍盐肽受体筛选;

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1. Synthesis of guanidinium-Derived Receptor Libraries and Screening for Selective Peptide Receptors in Water [J] . Kim B. Jensen, Tobias M. Braxmeier, Mariangela Demarcus, Chemistry: A European journal . 2002,第6期

机译：胍基受体文库的合成及水中选择性肽受体的筛选
2. Design, Synthesis, and Screening of a Library of Peptidyl Bis(Boroxoles) as Oligosaccharide Receptors in Water: Identification of a Receptor for the Tumor Marker TF-Antigen Disaccharide† [J] . li id=au1Arnab Pal li id=au2Marie Bérubé Dr. li id=au3Dennis#x2005, G. Hall Prof. Angewandte Chemie International Edition . 2010,第8期

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3. Design, Synthesis, and Screening of a Library of Peptidyl Bis(BoroxoIes) as Oligosaccharide Receptors in Water: Identification of a Receptor for the Tumor Marker TF-Antigen Disaccharide [J] . Arnab Pal, Marie Berube, Dennis G. Hall Angewandte Chemie . 2010,第8期

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机译：设计，合成和筛选作为中性水中复杂寡糖的低分子量受体的肽基双硼氧烷库：鉴定肿瘤标记物TF-抗原的选择性受体
6. Synthesis and Screening of a Cyclic Peptide Library: Discovery of Small-Molecule Ligands against Human Prolactin Receptor [O] . Tao Liu, Sang Hoon Joo, Jeffrey L. Voorhees, -1

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7. Synthesis and screening of a cyclic peptide library: Discovery of small-molecule ligands against human prolactin receptor [O] . Tao Liu, Sang Hoon Joo, Jeffrey L. Voorhees, 2009

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Synthesis of guanidinium-Derived Receptor Libraries and Screening for Selective Peptide Receptors in Water

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