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Literature DB >> 22871580

Near-infrared fluorescent divalent RGD ligand for integrin αvβ₃-targeted optical imaging.

Yunpeng Ye¹, Walter Akers, Baogang Xu, Sharon Bloch, Charles Odonkor, Samuel Achilefu.

Abstract

A new near-infrared fluorescent compound containing two cyclic RGD motifs, cypate-[c(RGDfK)](2) (1), was synthesized based on a carbocyanine fluorophore bearing two carboxylic acid groups (cypate) for integrin α(v)β(3)-targeting. Compared with its monovalent counterpart cypate-c(RGDfK) (2), 1 exhibited remarkable improvements in integrin α(v)β(3) binding affinity and tumor uptake in nude mice of A549. The results suggest that cypate-linked divalent ligands can serve as an important molecular platform for exploring receptor-targeted optical imaging and treatment of various diseases.

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Year: 2012 PMID： 22871580 PMCID： PMC3423536 DOI： 10.1016/j.bmcl.2012.07.044

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

38 in total

1. Crystal structure of the extracellular segment of integrin alpha Vbeta3.

Authors: J P Xiong; T Stehle; B Diefenbach; R Zhang; R Dunker; D L Scott; A Joachimiak; S L Goodman; M A Arnaout
Journal: Science Date: 2001-09-06 Impact factor: 47.728

2. Multimodal silica nanoparticles are effective cancer-targeted probes in a model of human melanoma.

Authors: Miriam Benezra; Oula Penate-Medina; Pat B Zanzonico; David Schaer; Hooisweng Ow; Andrew Burns; Elisa DeStanchina; Valerie Longo; Erik Herz; Srikant Iyer; Jedd Wolchok; Steven M Larson; Ulrich Wiesner; Michelle S Bradbury
Journal: J Clin Invest Date: 2011-06-13 Impact factor: 14.808

3. Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.

Authors: Yunpeng Ye; Sharon Bloch; Baogang Xu; Samuel Achilefu
Journal: J Med Chem Date: 2006-04-06 Impact factor: 7.446

Review 4. Radiolabeled multimeric cyclic RGD peptides as integrin alphavbeta3 targeted radiotracers for tumor imaging.

Authors: Shuang Liu
Journal: Mol Pharm Date: 2006 Sep-Oct Impact factor: 4.939

5. Synthesis and characterization of a Eu-DTPA-PEGO-MSH(4) derivative for evaluation of binding of multivalent molecules to melanocortin receptors.

Authors: Liping Xu; Josef Vagner; Ramesh Alleti; Venkataramanarao Rao; Bhumasamudram Jagadish; David L Morse; Victor J Hruby; Robert J Gillies; Eugene A Mash
Journal: Bioorg Med Chem Lett Date: 2010-03-04 Impact factor: 2.823

6. In vitro and in vivo evaluation of a paclitaxel conjugate with the divalent peptide E-[c(RGDfK)2] that targets integrin alpha v beta 3.

Authors: Claudia Ryppa; Hagit Mann-Steinberg; Martin L Biniossek; Ronit Satchi-Fainaro; Felix Kratz
Journal: Int J Pharm Date: 2008-10-17 Impact factor: 5.875

7. Development and evaluation of peptidic ligands targeting tumour-associated urokinase plasminogen activator receptor (uPAR) for use in alpha-emitter therapy for disseminated ovarian cancer.

Authors: Sebastian Knör; Sumito Sato; Timo Huber; Alfred Morgenstern; Frank Bruchertseifer; Manfred Schmitt; Horst Kessler; Reingard Senekowitsch-Schmidtke; Viktor Magdolen; Christof Seidl
Journal: Eur J Nucl Med Mol Imaging Date: 2007-09-22 Impact factor: 9.236

8. Improving tumor uptake and pharmacokinetics of (64)Cu-labeled cyclic RGD peptide dimers with Gly(3) and PEG(4) linkers.

Authors: Jiyun Shi; Young-Seung Kim; Shizhen Zhai; Zhaofei Liu; Xiaoyuan Chen; Shuang Liu
Journal: Bioconjug Chem Date: 2009-04 Impact factor: 4.774