Conformational Control of Integrin-Subtype Selectivity in isoDGR Peptide Motifs: A Biological Switch

被引：63

作者：

Frank, Andreas O. ^{[1
]}

Otto, Elke ^{[1
]}

Mas-Moruno, Carlos ^{[1
]}

Schiller, Herbert B. ^{[3
]}

Marinelli, Luciana ^{[2
]}

Cosconati, Sandro ^{[2
]}

Bochen, Alexander ^{[1
]}

Vossmeyer, Doerte ^{[4
]}

Zahn, Grit ^{[4
]}

Stragies, Roland ^{[4
]}

Novellino, Ettore ^{[2
]}

Kessler, Horst ^{[1
]}

机构：

[1] Tech Univ Munich, Dept Chem, Inst Adv Study, D-85747 Garching, Germany

[2] Univ Naples Federico II, Dipartimento Chim Farmaceut & Tossicolog, I-80131 Naples, Italy

[3] Max Planck Inst Biochem, Dept Mol Med, D-82152 Martinsried, Germany

[4] Jerini AG, D-10115 Berlin, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2010年 / 49卷 / 48期

关键词：

cyclic pentapeptides; integrin ligands; isoDGR sequence; NMR spectroscopy; peptides; CYCLIC PENTAPEPTIDES; FIBRONECTIN; RESIDUES; LIGANDS; BINDING; ALPHA(5)BETA(1); ALPHA-V-BETA-3; DEAMIDATION; SEQUENCES; DESIGN;

D O I：

10.1002/anie.201004363

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The rearrangement of asparagine to isoaspartate (isoD) is responsible for the deactivation of many functional proteins. However, the isoDGR motif, which is optimally presented as a conformationally controlled cyclic pentapeptide, binds selectively to α5β 1 integrin (see the docking model) with an affinity comparable to that of the peptidic antitumor agent Cilengitide. Copyright © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：9278 / 9281

页数：4

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