%0 Journal Article %1 doi:10.1021/bc100551s %A Morales-Avila, Enrique %A Ferro-Flores, Guillermina %A Ocampo-García, Blanca E. %A De León-Rodríguez, Luis M. %A Santos-Cuevas, Clara L. %A García-Becerra, Rocío %A Medina, Luis A. %A Gómez-Oliván, Leobardo %D 2011 %J Bioconjugate Chemistry %K gold %N 5 %P 913-922 %R 10.1021/bc100551s %T Multimeric System of 99mTc-Labeled Gold Nanoparticles Conjugated to cRGDfK(C) for Molecular Imaging of Tumor α(v)β(3) Expression %U http://pubs.acs.org/doi/abs/10.1021/bc100551s %V 22 %X Integrin αVβ3 plays a critical role in tumor angiogenesis and metastasis. Suitably radiolabeled cyclic RGD peptides can be used for noninvasive imaging of αVβ3 expression. The aim of this research was to prepare a multimeric system of technetium-99m-labeled gold nanoparticles conjugated to cRGDfK(C) and to evaluate its biological behavior as a potential radiopharmaceutical for molecular imaging of tumor angiogenesis. Hydrazinonicotinamide-GGC (HYNIC-GGC) and cRGDfK(C) peptides were synthesized and conjugated to gold nanoparticles (AuNP, 20 nm) by means of spontaneous reaction of the thiol groups of cysteine. The nanoconjugate was characterized by TEM, FT-IR, UV–vis, XPS, and Raman spectroscopy. To obtain 99mTc-HYNIC-GGC-AuNP-cRGDfK(C) (99mTc-AuNP-RGD), the 99mTc-HYNIC-GGC radiopeptide was first prepared and added to 1.5 mL of AuNP solution (1 nM) followed by cRGDfK(C) (10 μL, 50 μM) at 18 °C with stirring for 15 min. Radiochemical purity (RP) was determined by size-exclusion HPLC and ITLC-SG analyses. In vitro binding studies were carried out in αVβ3 receptor-positive C6 glioma cancer cells. Biodistribution studies were accomplished in athymic mice with C6-induced tumors with blocked and nonblocked receptors, and images were obtained using a micro-SPECT/CT. TEM and spectroscopy techniques demonstrated that AuNPs were functionalized with peptides. RP was 96 ± 2% without postlabeling purification. 99mTc-AuNP-RGD showed specific recognition for αVβ3 integrins expressed in C6 cells, and 3 h after i.p. administration in mice, the tumor uptake was 8.18 ± 0.57% ID/g. Micro-SPECT/CT images showed evident tumor uptake. 99mTc-AuNP-RGD demonstrates properties suitable for use as a target-specific agent for molecular imaging of tumor αVβ3 expression.

@article{doi:10.1021/bc100551s, abstract = { Integrin αVβ3 plays a critical role in tumor angiogenesis and metastasis. Suitably radiolabeled cyclic RGD peptides can be used for noninvasive imaging of αVβ3 expression. The aim of this research was to prepare a multimeric system of technetium-99m-labeled gold nanoparticles conjugated to c[RGDfK(C)] and to evaluate its biological behavior as a potential radiopharmaceutical for molecular imaging of tumor angiogenesis. Hydrazinonicotinamide-GGC (HYNIC-GGC) and c[RGDfK(C)] peptides were synthesized and conjugated to gold nanoparticles (AuNP, 20 nm) by means of spontaneous reaction of the thiol groups of cysteine. The nanoconjugate was characterized by TEM, FT-IR, UV–vis, XPS, and Raman spectroscopy. To obtain 99mTc-HYNIC-GGC-AuNP-c[RGDfK(C)] (99mTc-AuNP-RGD), the 99mTc-HYNIC-GGC radiopeptide was first prepared and added to 1.5 mL of AuNP solution (1 nM) followed by c[RGDfK(C)] (10 μL, 50 μM) at 18 °C with stirring for 15 min. Radiochemical purity (RP) was determined by size-exclusion HPLC and ITLC-SG analyses. In vitro binding studies were carried out in αVβ3 receptor-positive C6 glioma cancer cells. Biodistribution studies were accomplished in athymic mice with C6-induced tumors with blocked and nonblocked receptors, and images were obtained using a micro-SPECT/CT. TEM and spectroscopy techniques demonstrated that AuNPs were functionalized with peptides. RP was 96 ± 2% without postlabeling purification. 99mTc-AuNP-RGD showed specific recognition for αVβ3 integrins expressed in C6 cells, and 3 h after i.p. administration in mice, the tumor uptake was 8.18 ± 0.57% ID/g. Micro-SPECT/CT images showed evident tumor uptake. 99mTc-AuNP-RGD demonstrates properties suitable for use as a target-specific agent for molecular imaging of tumor αVβ3 expression. }, added-at = {2012-04-21T03:05:46.000+0200}, author = {Morales-Avila, Enrique and Ferro-Flores, Guillermina and Ocampo-García, Blanca E. and De León-Rodríguez, Luis M. and Santos-Cuevas, Clara L. and García-Becerra, Rocío and Medina, Luis A. and Gómez-Oliván, Leobardo}, biburl = {https://www.bibsonomy.org/bibtex/292b483f9d5744b5d5ea907ab53e125aa/rodrimauricio}, description = {Multimeric System of 99mTc-Labeled Gold Nanoparticles Conjugated to c[RGDfK(C)] for Molecular Imaging of Tumor α(v)β(3) Expression - Bioconjugate Chemistry (ACS Publications)}, doi = {10.1021/bc100551s}, eprint = {http://pubs.acs.org/doi/pdf/10.1021/bc100551s}, interhash = {0a76eb709527a7fb58b90716ab6daf40}, intrahash = {92b483f9d5744b5d5ea907ab53e125aa}, journal = {Bioconjugate Chemistry}, keywords = {gold}, number = 5, pages = {913-922}, timestamp = {2012-04-21T03:05:46.000+0200}, title = {Multimeric System of 99mTc-Labeled Gold Nanoparticles Conjugated to c[RGDfK(C)] for Molecular Imaging of Tumor α(v)β(3) Expression}, url = {http://pubs.acs.org/doi/abs/10.1021/bc100551s}, volume = 22, year = 2011 }