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基于四氢氮杂环壬酮支架的新型构象偏向整合素配体的合成与生物学评价

Synthesis and biological evaluation of new conformationally biased integrin ligands based on a tetrahydroazoninone scaffold.

作者信息

Banfi Luca, Basso Andrea, Damonte Gianluca, De Pellegrini Federico, Galatini Andrea, Guanti Giuseppe, Monfardini Ilaria, Riva Renata, Scapolla Carlo

机构信息

Department of Chemistry and Industrial Chemistry, via Dodecaneso 31, 16146 Genova, Italy.

出版信息

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1341-5. doi: 10.1016/j.bmcl.2006.11.085. Epub 2006 Dec 2.

DOI:10.1016/j.bmcl.2006.11.085
PMID:17169558
Abstract

The synthesis of new conformationally biased cyclic pentapeptides, incorporating the RGD sequence, and built around a tetrahydroazoninone scaffold, is reported. They exhibit interesting activity towards integrin alphaVbeta3 and a remarkable selectivity in comparison with integrin alphaVbeta5.

摘要

报道了一种新的构象偏向性环状五肽的合成,该五肽包含RGD序列,并以四氢氮杂环壬酮支架为基础构建。它们对整合素αVβ3表现出有趣的活性,并且与整合素αVβ5相比具有显著的选择性。

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