Radiosynthesis and micro-SPECT analysis of triazole-based RGD integrin ligands as non-peptide molecular imaging probes for angiogenesis

被引：14

作者：

Bianchini, Francesca ^{[1
]}

Fabbrizzi, Pierangelo ^{[2
]}

Menchi, Gloria ^{[2
,3
]}

Raspanti, Silvia ^{[1
]}

Bottoncetti, Anna ^{[4
]}

Passeri, Alessandro ^{[1
,3
]}

Andreucci, Elena ^{[1
]}

Guarna, Antonio ^{[2
,3
]}

Calorini, Lido ^{[1
]}

Pupi, Alberto ^{[1
,3
,4
]}

Trabocchi, Andrea ^{[2
,3
]}

机构：

[1] Univ Florence, Dept Clin & Expt Biomed Sci Mario Serio, I-50134 Florence, Italy

[2] Univ Florence, Dept Chem Ugo Schiff, I-50019 Florence, Italy

[3] Univ Florence, Interdept Ctr Preclin Dev Mol Imaging CISPIM, I-50134 Florence, Italy

[4] AOUC, I-50134 Florence, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 05期

关键词：

Integrins; Molecular imaging; Cancer; Angiogenesis; Amino acids; CATION-PI INTERACTIONS; IN-VIVO; ALPHA(V)BETA(3) INTEGRIN; DRUG DEVELOPMENT; RECEPTOR; DISCOVERY; BIOLOGY; CANCER; TUMOR; ALPHA-V-BETA-3;

D O I：

10.1016/j.bmc.2014.12.065

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：

Taking advantage of click chemistry, we synthesized triazole-containing RGD peptidomimetics capable of binding to alpha(v)beta(3) integrin with diverse potency, and selected I-125-labeled compounds proved to interact in vitro and in vivo with alpha(v)beta(3) integrin expressed by melanoma cells. Two I-125-compounds containing either 2-aminobenzimidazole or 2-aminopyridine groups as the arginine bioisostere with the capacity to selectively bind cells of highly expressing alpha(v)beta(3) melanoma xenografts were found using micro-SPECT imaging studies. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：1112 / 1122

页数：11

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