chelating agents such as isothiocyanatobenzyl-1,4,7-triazacyclononane-triacetic
acid (SCN–NOTA) can be simply conjugated on the carboxylate group of the
surface of GOs which will be used later to label radionuclides such as
68 Ga or
64 Cu
[82, 83]. It also has the ability to chelate other radionuclide,
177 Lu for cancer
theranostic approach exploiting its emission of gamma ray and beta ray.
As another labeling method, click chemistry has been successfully adopted for a
simple and rapid labeling of GOs or GQDs in mild condition, showing that the
reaction between clickable moieties of esop and its corresponding azadibenzocyclooctyne group occurs within several minutes at room temperature [84–86].
Through this simple reaction, the well-defined and simple click reaction for modification of GOs shall aid in the development of a variety of radionuclide-labeled
graphene nanosheets capable of decorating multifunctional theranostic
biomolecules.
To date, researchers have attempted to develop graphene-based in vivo active
tumor targeting by incorporating specific ligands together with radioisotope labeling [87, 88]. Cai and his group used the
64 Cu-labeled GOs on PET imaging and
achieved successful cancer targeting [87].
64 Cu–GOs labeled with monoclonal
antibody against proliferating endothelial marker, TRC105 (
64 Cu–NOTA–GO–
TRC105), showed specific targeting to the 4T1 breast cancers inoculated in the
mouse. A parallel study of tumor targeting used
66 Ga-labeled nano GO (nGO)-PEG
for PET imaging [88]. Other reports followed to show again efficient tumor targeting of GOs conjugated with monoclonal antibody (mAb) against follicle stimulating hormone receptor (FSHR), which is ubiquitously expressed in tumor
vasculature.
64 Cu–NOTA–GO–FSHR–mAb accumulated persistently in metastatic
breast cancer nodules in the lungs on PET imaging [89]. In addition, vascular
endothelial growth factor 121 (VEGF 121 ) was conjugated with GOs by Shi et al. for
targeting VEGF receptor and could enhance the targeting efficiency of GOs to the
tumor [90]. Serial whole body PET images of
64 Cu–GO–VEGF 121 showed rapid
accumulation of graphene in U87MG tumor-bearing mice within 30 min. The same
group also used
64 Cu–NOTA–RGO–IONP–PEG, finding that radiolabeled-GOs
cumulated passively in peripheral ischemic area. A reinjection of
64 Cu–RGO–
IONP–PEG revealed accelerated blood clearance, and IgM against PEG was the
cause of this shortening of circulation [91, 92].
SPECT is approximately ten times less sensitive than PET. However, concurrent
imaging of multiple radionuclides of different energies is an advantage of SPECT.
Additionally, SPECT is widely available in clinics unlike PET’s dependence on the
availability of cyclotron, and SPECT radionuclides are simpler to prepare and usually
have a longer half-life than PET radionuclides. Cornelissen et al. explored feasibility
of targeting the HER2-overproducing breast cancer using anti-HER2 antibodyconjugated nGO, radiolabeled with
111 In-benzyl-diethylenetriaminepentaacetic acid
via p–p stacking on SPECT [93]. The pharmacokinetics of radiolabeled
nGO-trastuzumab conjugates were better when compared to radiolabeled trastuzumab without NGO, clearing from circulation at a faster rate. Fazaeli et al. investigated
in vivo targeting and SPECT imaging of tumors with
198,199 AU@AF–GO
96
J. M. Yoo et al.
acid (SCN–NOTA) can be simply conjugated on the carboxylate group of the
surface of GOs which will be used later to label radionuclides such as
68 Ga or
64 Cu
[82, 83]. It also has the ability to chelate other radionuclide,
177 Lu for cancer
theranostic approach exploiting its emission of gamma ray and beta ray.
As another labeling method, click chemistry has been successfully adopted for a
simple and rapid labeling of GOs or GQDs in mild condition, showing that the
reaction between clickable moieties of esop and its corresponding azadibenzocyclooctyne group occurs within several minutes at room temperature [84–86].
Through this simple reaction, the well-defined and simple click reaction for modification of GOs shall aid in the development of a variety of radionuclide-labeled
graphene nanosheets capable of decorating multifunctional theranostic
biomolecules.
To date, researchers have attempted to develop graphene-based in vivo active
tumor targeting by incorporating specific ligands together with radioisotope labeling [87, 88]. Cai and his group used the
64 Cu-labeled GOs on PET imaging and
achieved successful cancer targeting [87].
64 Cu–GOs labeled with monoclonal
antibody against proliferating endothelial marker, TRC105 (
64 Cu–NOTA–GO–
TRC105), showed specific targeting to the 4T1 breast cancers inoculated in the
mouse. A parallel study of tumor targeting used
66 Ga-labeled nano GO (nGO)-PEG
for PET imaging [88]. Other reports followed to show again efficient tumor targeting of GOs conjugated with monoclonal antibody (mAb) against follicle stimulating hormone receptor (FSHR), which is ubiquitously expressed in tumor
vasculature.
64 Cu–NOTA–GO–FSHR–mAb accumulated persistently in metastatic
breast cancer nodules in the lungs on PET imaging [89]. In addition, vascular
endothelial growth factor 121 (VEGF 121 ) was conjugated with GOs by Shi et al. for
targeting VEGF receptor and could enhance the targeting efficiency of GOs to the
tumor [90]. Serial whole body PET images of
64 Cu–GO–VEGF 121 showed rapid
accumulation of graphene in U87MG tumor-bearing mice within 30 min. The same
group also used
64 Cu–NOTA–RGO–IONP–PEG, finding that radiolabeled-GOs
cumulated passively in peripheral ischemic area. A reinjection of
64 Cu–RGO–
IONP–PEG revealed accelerated blood clearance, and IgM against PEG was the
cause of this shortening of circulation [91, 92].
SPECT is approximately ten times less sensitive than PET. However, concurrent
imaging of multiple radionuclides of different energies is an advantage of SPECT.
Additionally, SPECT is widely available in clinics unlike PET’s dependence on the
availability of cyclotron, and SPECT radionuclides are simpler to prepare and usually
have a longer half-life than PET radionuclides. Cornelissen et al. explored feasibility
of targeting the HER2-overproducing breast cancer using anti-HER2 antibodyconjugated nGO, radiolabeled with
111 In-benzyl-diethylenetriaminepentaacetic acid
via p–p stacking on SPECT [93]. The pharmacokinetics of radiolabeled
nGO-trastuzumab conjugates were better when compared to radiolabeled trastuzumab without NGO, clearing from circulation at a faster rate. Fazaeli et al. investigated
in vivo targeting and SPECT imaging of tumors with
198,199 AU@AF–GO
96
J. M. Yoo et al.