Preparation and SPECT imaging of the novel Anxa 1-targeted probe 99mTc-p-SCN-Bn-DTPA-GGGRDN-IF7

Chen, Fei; Pu, Xiaojia; Xiao, Yichun; Shao, Kejing; Wang, Junchao; Hu, Wei; Zhu, Bao Li; Mengjun, Jiang

doi:10.1007/s10967-019-06500-1

Cited by 4 publications

(1 citation statement)

References 17 publications

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“…Currently, tumors are often diagnosed by positron emission tomography (PET) scans utilizing radioactive 18 F glucose or FDG. Despite the highly specific tumor vasculature targeting activity of IF7, our attempts to conduct PET with IF7 were not successful (data not shown), although others have shown detectable, though limited, tumor imaging with IF7 [29][30][31]. We emphasize, however, that whole body imaging of IRDye-conjugated dTIT7 indicated clear brain tumor targeting (Fig 4).…”

Section: Discussionmentioning

confidence: 83%

Development of an orally-administrable tumor vasculature-targeting therapeutic using annexin A1-binding D-peptides

et al. 2021

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We previously reported that IF7 peptide, which binds to the annexin A1 (ANXA1) N-terminus, functions as a tumor vasculature-targeted drug delivery vehicle after intravenous injection. To enhance IF7 stability in vivo, we undertook mirror-image peptide phage display using a synthetic D-peptide representing the ANXA1 N-terminus as target. We then identified peptide sequences, synthesized them as D-amino acids, and designated the resulting peptide dTIT7, which we showed bound to the ANXA1 N-terminus. Whole body imaging of mouse brain tumor models injected with near infrared fluorescent IRDye-conjugated dTIT7 showed fluorescent signals in brain and kidney. Furthermore, orally-administered dTIT7/geldanamycin (GA) conjugates suppressed brain tumor growth. Ours is a proof-of-concept experiment showing that ANXA1-binding D-peptide can be developed as an orally-administrable tumor vasculature-targeted therapeutic.

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