<sup>99m</sup>Tc-Labeled RGD-BBN Peptide for Small-Animal SPECT/CT of Lung Carcinoma

Liu, Zhaofei; Huang, Jinming; Dong, Chengyan; Cui, Liyang; Jin, Xiaona; Jia, Bing; Zhu, Zhaohui; Li, Fang; Wang, Fan

doi:10.1021/mp200661t

Cited by 56 publications

(45 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…57,59) As imaging agents, RGD-modified probes were reported, such as [ Tc-labeled HYNIC-3PEG4-E[c(RGDfK) 2 ] was also synthesized as a SPECT/CT probe, shows high binding affinity to integrin α v β 3 , and is used as a pretreatment screening tool in breast cancer. 63,64) 64 Cu-DOTA-QD-RGD is a dual-modality imaging probe, and the quantum dot (QD) surface was modified with about 90 RGD peptides and DOTA chelators for integrin α v β 3 -targeted PET/near-infrared (NIR) fluorescence imaging. In the U87MG tumor model, 64 Cu-DOTA-QD-RGD exhibited specific binding to integrin α v β 3 and provided sufficiently clear tumor images in both PET and optical NIR imaging.…”

Section: Integrin-targeted Peptidesmentioning

confidence: 99%

“…63,64) 64 Cu-DOTA-QD-RGD is a dual-modality imaging probe, and the quantum dot (QD) surface was modified with about 90 RGD peptides and DOTA chelators for integrin α v β 3 -targeted PET/near-infrared (NIR) fluorescence imaging. In the U87MG tumor model, 64 Cu-DOTA-QD-RGD exhibited specific binding to integrin α v β 3 and provided sufficiently clear tumor images in both PET and optical NIR imaging. 65) ATN-161 (Ac-Pro-His-Ser-Cys-Asn-NH 2 ) is a non-RGD peptide that specifically recognizes integrin α 5 β 1 , with potent antitumor and antimetastatic activity.…”

Section: Integrin-targeted Peptidesmentioning

confidence: 99%

See 1 more Smart Citation

Peptide-Based Cancer-Targeted DDS and Molecular Imaging

Hagimori

Fuchigami

Kawakami

2017

CHEMICAL & PHARMACEUTICAL BULLETIN

View full text Add to dashboard Cite

Targeting cancer cell-surface receptors is an attractive approach for cancer treatment and diagnosis. Peptides having high binding affinities to receptors overexpressed in cancer cells are useful because of their simple structure, low immunogenicity, and easy, cost-effective chemical synthesis. A number of peptide ligands have been developed for cancer cell-surface receptors and applied to nanoparticles with anticancer drugs, genes, small interfering RNAs (siRNAs), and molecular imaging agents. In particular, recent findings have revealed that peptide-modified PEGylated liposome-encapsulated drugs are effective in cancer-targeted therapy and cancer cell-specific imaging. This review discusses peptide-modified nanoparticles for drug delivery systems (DDS) and molecular imaging, focusing on peptide ligands for somatostatin receptors, integrin, transferrin receptor, human epidermal growth factor 2 (HER2), etc. In addition, methods to improve binding affinity or endosomal escape with spacer peptides and stimuli (internal and external) are discussed.

show abstract

Section: Integrin-targeted Peptidesmentioning

confidence: 99%

Section: Integrin-targeted Peptidesmentioning

confidence: 99%

Peptide-Based Cancer-Targeted DDS and Molecular Imaging

Hagimori

Fuchigami

Kawakami

2017

CHEMICAL & PHARMACEUTICAL BULLETIN

View full text Add to dashboard Cite

show abstract

“…99m Tc-RGD-Bombesin SPECT Radiolabeling and quality control of the 99m Tc-RGD-bombesin were performed as described previously (14,15). Specifically, a single 11.1 MBq/kg intravenous bolus of 99m Tc-RGD-bombesin was injected and then followed by a 10-mL saline flush (14).…”

Section: Subjectsmentioning

confidence: 99%

^99mTc-Glu-c(RGDyK)-Bombesin SPECT Can Reduce Unnecessary Biopsy of Masses That Are BI-RADS Category 4 on Ultrasonography

Gao

Liu

et al. 2016

J Nucl Med

Self Cite

View full text Add to dashboard Cite

Masses that, on ultrasonography, are category 4 according to the Breast Imaging Reporting and Data System (BI-RADS) represent possible malignancy, and a biopsy is recommended. This study explored the value of 99m Tc-Glu-c(RGDyK)-bombesin ( 99m Tc-RGD-bombesin) in reducing unnecessary biopsy of these masses. Methods: Ninety women with a BI-RADS 4 mass on ultrasonography were enrolled in this study to undergo breast SPECT using 99m Tc-RGD-bombesin. The images were independently interpreted using qualitative visual and semiquantitative analyses. The final diagnosis was based on histopathologic examination of surgically excised or percutaneous biopsy specimens. Fractions of the samples were immunohistochemically analyzed to evaluate expression of integrin α v β 3 and gastrinreleasing peptide receptor (GRPR). The receptor-positive group was further divided into 3 subgroups (GRPR 1 /α v β 3 1 , GRPR 1 /α v β 3 − , and α v β 3 1 /GRPR − ). Results: Ninety-four masses (22 malignant and 72 benign) were confirmed by histopathologic examination. On qualitative analysis, 20 of the malignant masses showed high 99m Tc-RGDbombesin accumulation and 48 of the benign masses showed no 99m Tc-RGD-bombesin accumulation. The optimal cutoff for qualitative analysis was a score of 2. Semiquantitative analysis revealed that 20 of the malignant masses and 16 of the benign masses had a relatively high tumor-to-normal-tissue ratio (T/N). The optimal cutoff was a T/N of 2.26. The mean T/N was higher for malignant masses than for benign masses (3.17 ± 0.86 vs. 1.89 ± 0.71, P , 0.05). T/Ns did not differ among the 3 subgroups (P . 0.05). The areas under the receiver-operating-characteristic curves for the qualitative and semiquantitative analyses were 0.788 and 0.865, respectively, and the overall diagnostic performance did not significantly differ between these analyses (P . 0.05). Conclusion: 99m Tc-RGD-bombesin SPECT can differentiate benign from malignant BI-RADS 4 masses with high specificity. Further study of the application of this test to clinical breast cancer appears warranted.

show abstract

“…The reversed-phase high-performance liquid chromatography (HPLC) system was the same as previously reported (16,17).…”

Section: Generalmentioning

confidence: 99%

Integrin α_vβ₆–Targeted SPECT Imaging for Pancreatic Cancer Detection

Liu

Líu

et al. 2014

J Nucl Med

Self Cite

View full text Add to dashboard Cite

Integrin α v β 6 , a member of the integrin family, is specifically expressed in many malignancies but not in normal organs. Overexpression of integrin α v β 6 is usually correlated with malignant potential and poor prognosis. In this study, we describe the synthesis and evaluation of a 99m Tc-labeled integrin α v β 6 -targeting peptide as a SPECT radiotracer for the in vivo imaging of integrin α v β 6 expression. Methods: An integrin α v β 6 -targeting peptide (denoted as the HK peptide) was conjugated with 6-hydrazinonicotinyl (HYNIC) and radiolabeled with 99m Tc using tricine and TPPTS (trisodium triphenylphosphine-3,3′,3″-trisulfonate) as coligands. The in vitro and in vivo characteristics of 99m Tc-HYNIC(tricine)(TPPTS)-HK ( 99m Tc-HHK) were investigated in BxPC-3 (integrin α v β 6 -positive) and HEK293 (integrin α v β 6 -negative) models. The ability of 99m Tc-HHK to detect liver metastasis of pancreatic cancer was evaluated using small-animal SPECT/CT. Results: 99m Tc-HHK showed high integrin α v β 6 -binding specificity both in vitro and in vivo. 99m Tc-HHK was cleared rapidly from the blood and normal organs except for the kidneys. The highest uptake (0.88 ± 0.12 percentage injected dose per gram) of 99m Tc-HHK in BxPC-3 tumors was observed at 0.5 h after injection. High-contrast images of integrin α v β 6 -positive tumors were obtained using 99m Tc-HHK. The minimum nonspecific activity accumulation in normal liver tissues rendered high-quality SPECT/CT images of metastatic lesions. Conclusion: 99m Tc-HHK is a promising SPECT radiotracer for the noninvasive imaging of integrin α v β 6 expression in vivo. SPECT/ CT with 99m Tc-HHK could provide an effective approach for the noninvasive detection of primary and metastatic lesions of integrin α v β 6 -positive tumors.

show abstract

^99mTc-Labeled RGD-BBN Peptide for Small-Animal SPECT/CT of Lung Carcinoma

Cited by 56 publications

References 28 publications

Peptide-Based Cancer-Targeted DDS and Molecular Imaging

Peptide-Based Cancer-Targeted DDS and Molecular Imaging

^99mTc-Glu-c(RGDyK)-Bombesin SPECT Can Reduce Unnecessary Biopsy of Masses That Are BI-RADS Category 4 on Ultrasonography

Integrin α_vβ₆–Targeted SPECT Imaging for Pancreatic Cancer Detection

Contact Info

Product

Resources

About

99mTc-Labeled RGD-BBN Peptide for Small-Animal SPECT/CT of Lung Carcinoma

Cited by 56 publications

References 28 publications

Peptide-Based Cancer-Targeted DDS and Molecular Imaging

Peptide-Based Cancer-Targeted DDS and Molecular Imaging

99mTc-Glu-c(RGDyK)-Bombesin SPECT Can Reduce Unnecessary Biopsy of Masses That Are BI-RADS Category 4 on Ultrasonography

Integrin αvβ6–Targeted SPECT Imaging for Pancreatic Cancer Detection

Contact Info

Product

Resources

About

^99mTc-Labeled RGD-BBN Peptide for Small-Animal SPECT/CT of Lung Carcinoma

^99mTc-Glu-c(RGDyK)-Bombesin SPECT Can Reduce Unnecessary Biopsy of Masses That Are BI-RADS Category 4 on Ultrasonography

Integrin α_vβ₆–Targeted SPECT Imaging for Pancreatic Cancer Detection