Hybrid Bombesin Analogues: Combining an Agonist and an Antagonist in Defined Distances for Optimized Tumor Targeting

被引：60

作者：

Kroll, Carsten ^{[1
]}

Mansi, Rosalba ^{[2
]}

Braun, Friederike ^{[2
]}

Dobitz, Stefanie ^{[1
]}

Maecke, Helmut R. ^{[2
]}

Wennemers, Helma ^{[1
]}

机构：

[1] ETH, Organ Chem Lab, CH-8092 Zurich, Switzerland

[2] Univ Hosp Freiburg, Dept Nucl Med, Freiburg, Germany

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2013年 / 135卷 / 45期

基金：

瑞士国家科学基金会;

关键词：

CELL-SURFACE RECEPTORS; SOLID-PHASE; IN-VIVO; LIGANDS; PROSTATE; SELECTIVITY; PEPTIDES; BINDING;

D O I：

10.1021/ja4087648

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Radiolabeled hybrid ligands with defined distances between an agonist and an antagonist for the gastrin-releasing peptide receptor were found to have excellent tumor-targeting properties. Oligoprolines served as rigid scaffolds that allowed for tailoring distances of 10, 20, and 30 angstrom between the recognition elements. In vitro and in vivo studies revealed that the hybrid ligand with a distance of 20 angstrom between the recognition elements exhibits the highest yet observed tumor cell uptake and retention time in prostate cancer cells.

引用

页码：16793 / 16796

页数：4

共 51 条

[1] Novel DOTA-based prochelator for divalent peptide vectorization: synthesis of dimeric bombesin analogues for multimodality tumor imaging and therapy [J].

Abiraj, Keelara ;

Jaccard, Hugues ;

Kretzschmar, Martin ;

Helm, Lothar ;

Maecke, Helmut R. .

CHEMICAL COMMUNICATIONS, 2008, (28) :3248-3250

[2] Radiopeptide Imaging and Therapy in Europe [J].

Ambrosini, Valentina ;

Fani, Melpomeni ;

Fanti, Stefano ;

Forrer, Flavio ;

Maecke, Helmut R. .

JOURNAL OF NUCLEAR MEDICINE, 2011, 52 :42S-55S

[3]

American Cancer Society, 2011, GLOB CANC FACTS FIGU

[4]

[Anonymous], 2006, ANGEW CHEM, V118, P2408

[5]

[Anonymous], 2008, ANGEW CHEM, V120, P1709

[6]

Bodei L, 2007, EUR J NUCL MED MOL I, V34, pS221

[7]

Breeman WAP, 1999, INT J CANCER, V81, P658, DOI 10.1002/(SICI)1097-0215(19990517)81:4<658::AID-IJC24>3.0.CO

[8]

2-P

[9] Synthesis and characterization of bivalent peptide ligands targeted to G-protein-coupled receptors [J].

Carrithers, MD ;

Lerner, MR .

CHEMISTRY & BIOLOGY, 1996, 3 (07) :537-542

[10] Bombesin receptor antagonists may be preferable to agonists for tumor targeting [J].

Cescato, Renzo ;

Maina, Theodosia ;

Nock, Berthold ;

Nikolopoulou, Anastasia ;

Charalambidis, David ;

Piccand, Veronique ;

Reubi, Jean Claude .

JOURNAL OF NUCLEAR MEDICINE, 2008, 49 (02) :318-326

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