2018
DOI: 10.7150/thno.24395
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Radionuclide imaging of VEGFR2 in glioma vasculature using biparatopic affibody conjugate: proof-of-principle in a murine model

Abstract: Vascular endothelial growth factor receptor-2 (VEGFR2) is a key mediator of angiogenesis and therefore a promising therapeutic target in malignancies including glioblastoma multiforme (GBM). Molecular imaging of VEGFR2 expression may enable patient stratification for antiangiogenic therapy. The goal of the current study was to evaluate the capacity of the novel anti-VEGFR2 biparatopic affibody conjugate (ZVEGFR2-Bp2) for in vivo visualization of VEGFR2 expression in GBM.Methods: ZVEGFR2-Bp2 coupled to a NODAGA… Show more

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Cited by 26 publications
(40 citation statements)
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“…Another feature of affibody molecules is the very efficient reabsorption in the proximal tubules of kidneys. This feature has been observed for all binders, independent of the molecular target [23][24][25][26][27]29,37]. Therefore, it is reasonable to suppose that the reabsorption is determined by the scaffold rather than by a binding site.…”
Section: Biodistribution and Targeting Features Of Radiolabeled Affibmentioning
confidence: 73%
See 1 more Smart Citation
“…Another feature of affibody molecules is the very efficient reabsorption in the proximal tubules of kidneys. This feature has been observed for all binders, independent of the molecular target [23][24][25][26][27]29,37]. Therefore, it is reasonable to suppose that the reabsorption is determined by the scaffold rather than by a binding site.…”
Section: Biodistribution and Targeting Features Of Radiolabeled Affibmentioning
confidence: 73%
“…Affinity maturation permits a further increase of the affinity from a few nM to a few pM. High-affinity affibody binders have been selected for potential cancer-associated molecular targets such as human epidermal growth factor receptor type 2 (HER2) [22], epidermal growth factor receptor (EGFR or HER1) [23], human epidermal growth factor receptor type 3 (HER3) [24], insulinlike growth factor-1 receptor (IGF-1R) [25], platelet-derived growth factor receptor β (PDGFRβ) [26], vascular endothelial growth factor receptor 2 (VEGFR2) [27], programmed death-ligand 1 (PD-L1) [28], and carbonic anhydrase IX (CAIX) [29]. Several features of affibody molecules make them potentially attractive as targeting vectors for imaging probes:…”
Section: Engineered Scaffold Protein-based Imaging Probes: Affibody Mmentioning
confidence: 99%
“…Expression and purification of 3VGR19-3 (3,4). Expression and purification of bispecific nanobody (5,6). L is (G4S)3 (GGCGGCGGTGGTAGCGGCGGCGGCGGTTCCGGCGGTGGTGGTTCT) linker, M is size standards.…”
Section: Discussionmentioning
confidence: 99%
“…Vascular endothelial growth factor receptor 2 (VEGFR2) is involved in the regulation of angiogenesis, therefore, inhibiting VEGFR2 activity, and the downstream signaling pathway has become an important approach in cancer treatment. [3][4][5] Overexpression of HER2 can upregulate VEGF through the PI3K signaling pathway, so blocking HER2 significantly decreases VEGF expression and helps killing the tumor cells. 3,6 In addition, based on the synergetic effect and cross-talk between the signaling pathways, targeting both receptors simultaneously may more effectively inhibit tumor cell proliferation and promote apoptosis.…”
Section: Introductionmentioning
confidence: 99%
“…Besides, several research efforts have been put toward affibody and peptide-based radiotracers. 35,36 These molecules showed satisfactory PK and image contrast, but their imaging mode is based on SPECT, which significantly limits signal sensitivity and image quality. Compared to SPECT, PET exhibits several advantages, including improved image quality, greater interpretive certainty, higher diagnostic accuracy, and lower patient dosimetry.…”
Section: ■ Introductionmentioning
confidence: 99%