Targeted radionuclide therapy, which is based on the selective delivery of a sufficient radiation dose to tumors without significantly affecting normal tissues, is a promising therapeutic approach for the treatment of a wide variety of malignancies. Integrins, a family of cell adhesion molecules, play key roles during tumor angiogenesis and metastasis. Among all the integrins, αvβ3 seems to be ...

RGD tripeptide is a specific, high-affinity ligand for integrin, which is highly expressed in cancer cells. We previously reported that cRGD chemically modified AAV2 (AAV2(N587+1/azido+RGD)) showed significantly enhanced infectivity compared to RGD genetically inserted AAV2 (AAV2(N587+RGD)) (10.1016/j.biomaterials.2015.11.066) [1]. Herein we provide the binding ability analysis of RGD modified ...

RATIONALE The dramatic upregulation of αvβ3-integrin that occurs in the vasculature during tumor growth has long suggested that the endothelial expression of this molecule is an ideal target for antiangiogenic therapy to treat cancer. This discovery led to the development of small-molecule inhibitors directed against αvβ3-integrin that are currently in clinical trials. In 2002, we reported that...

We have developed a small-molecular probe, consisting of cyclic RGD pentapeptides bearing a nitrobenzoxadiazole fluorophore at the 4'-residue, which detects integrin αVβ3 activity in terms of fluorescence intensity decrease due to quenching of the fluorophore by interaction with tyrosine-122 at the binding site of the protein. This probe appears to be suitable for a practical, high-throughput f...

We have synthesized a new and stable MR contrast agent, SPIO-mPEG-cRGD, that exhibits superior binding to the biologic target αvβ3 integrins. Selective targeting of αvβ3 integrins was achieved by conjugating cyclic RGD peptides to the superparamagnetic iron oxide nanoparticles (SPIO) surface, while poly(ethylene glycol) (PEG) were used for nonimmunogenic, nonantigenic and protein resistant. The...

Fibroblast growth factor-1 (FGF1) and FGF2 play a critical role in angiogenesis, a formation of new blood vessels from existing blood vessels. Integrins are critically involved in FGF signaling through crosstalk. We previously reported that FGF1 directly binds to integrin αvβ3 and induces FGF receptor-1 (FGFR1)-FGF1-integrin αvβ3 ternary complex. We previously generated an integrin binding defe...

BACKGROUND Expression of αvβ3 integrin is increased after myocardial infarction as part of the repair process. Increased expression of αvβ3 has been shown by molecular imaging with 18F-galacto-RGD in a rat model. The 68Ga-labelled RGD compounds 68Ga-NODAGA-RGD and 68Ga-TRAP(RGD)3 have high specificity and affinity, and may therefore serve as alternatives of 18F-galacto-RGD for integrin imaging....

The deployment of endovascular implants such as stents in the treatment of cardiovascular disease damages the vascular endothelium, increasing the risk of thrombosis and promoting neointimal hyperplasia. The rapid restoration of a functional endothelium is known to reduce these complications. Circulating endothelial progenitor cells (EPCs) are increasingly recognized as important contributors t...

The connective tissue formed by extracellular matrix (ECM) rich in fibronectin and collagen consists a barrier that cancer cells have to overpass to reach blood vessels and then a metastatic site. Cell adhesion to fibronectin is mediated by αvβ3 and α5β1 integrins through an RGD motif present in this ECM protein, thus making these receptors key targets for cell migration studies. Here we invest...

Cancer stem cells (CSCs) have recently emerged as key contributors to drug resistance based on their enhanced abilities to evade apoptosis and survive unfavorable microenvironments. CSCs represent a subpopulation of cells that can self-renew, propagate, reconstitute the tumor heterogeneity, and resist many types of cancer therapies. Determining the specific pathways involved in regulating the d...