Cyclic RGD β-Lactam Peptidomimetics Induce Differential Gene Expression in Human Endothelial Cells

被引：14

作者：

Aizpurua, Jesus M. ^{[1
]}

Ignacio Ganboa, Jose ^{[1
]}

Palomo, Claudio ^{[1
]}

Loinaz, Iraida ^{[1
]}

Oyarbide, Joseba ^{[1
]}

Fernandez, Xabier ^{[1
]}

Balentova, Eva ^{[1
]}

Fratila, Raluca M. ^{[1
]}

Jimenez, Azucena ^{[1
]}

Ignacio Miranda, Jose ^{[1
]}

Laso, Antonio ^{[2
]}

Avila, Silvia ^{[2
]}

Luis Castrillo, Jose ^{[2
]}

机构：

[1] Univ Basque Country UPV EHU, Dept Quim Organ 1, Ctr Joxe Mari Korta, San Sebastian 20018, Spain

[2] Genetadi Biotech AG, Derio 48160, Spain

来源：

CHEMBIOCHEM | 2011年 / 12卷 / 03期

关键词：

antitumor agents; cell adhesion expression; peptides; peptidomimetics; INTEGRIN LIGANDS; DRUG DESIGN; PEPTIDES; ANGIOGENESIS; ARG; ALPHA(V)BETA(3); CONFORMATION; ANTAGONISTS; INHIBITORS; SCAFFOLDS;

D O I：

10.1002/cbic.201000572

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

RGD peptidomimetics touch DNA: A few RGD cyclic peptidomimetics, each incorporating a densely substituted β-lactam moiety, were prepared, and their effect on extracellular adhesion and intracellular gene regulation through αVβ3 integrin was studied in human endothelial cells (HUVECs). Surprisingly, the cyclic tetrapeptide with a deleted glycine residue and its parent RGD peptidomimetic displayed practically opposite angiogenic gene-regulation activity. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：401 / 405

页数：5

共 35 条

[1]

[Anonymous], 2009, ANGEW CHEM

[2] Conformationally Homogeneous Heterocyclic Pseudotetrapeptides as Three-Dimensional Scaffolds for Rational Drug Design: Receptor-Selective Somatostatin Analogues [J].