A Conformationally Frozen Peptoid Boosts CXCR4 Affinity and Anti-HIV Activity

被引：47

作者：

Demmer, Oliver ^{[1
,2
]}

Frank, Andreas O. ^{[1
,2
]}

Hagn, Franz ^{[1
,2
]}

Schottelius, Margret ^{[3
]}

Marinelli, Luciana ^{[4
]}

Cosconati, Sandro ^{[5
]}

Brack-Werner, Ruth ^{[6
]}

Kremb, Stephan ^{[6
]}

Wester, Hans-Juergen ^{[3
]}

Kessler, Horst ^{[1
,2
]}

机构：

[1] Tech Univ Munich, Inst Adv Study, Dept Chem, D-85748 Garching, Germany

[2] King Abdulaziz Univ, Dept Chem, Fac Sci, Jeddah 21589, Saudi Arabia

[3] Lehrstuhl Pharmazeut Radiochem, Garching, Germany

[4] Univ Naples Federico II, Dipartimento Chim Farmaceut & Tossicol, Naples, Italy

[5] Univ Naples 2, Dipartimento Sci Ambientali, Caserta, Italy

[6] Helmholtz Zentrum Munchen, Inst Virol Neuherberg, Neuherberg, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2012年 / 51卷 / 32期

关键词：

biological activity; drug design; medicinal chemistry; peptides; peptidomimetics; CHEMOKINE RECEPTOR CXCR4; PEPTIDES; AMD3100; ANTAGONISTS; DISCOVERY; INFECTION; LIGAND; CELLS; LESTR/FUSIN; INHIBITORS;

D O I：

10.1002/anie.201202090

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

There can be only one: Using a peptoid motif obtained by shifting the arginine side chain of a pentapeptide previously developed by Fujii et al. to the neighboring nitrogen atom restricts the conformational freedom and yields a conformationally homogeneous peptide (see picture) with a 100-fold higher binding affinity to the chemokine receptor CXCR4 in the picomolar range. Its efficiency to inhibit HIV-1 infections is also demonstrated. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：8110 / 8113

页数：4

共 38 条

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