Published May 2018 | Version v1
Journal article

One-step labelling of a novel small-molecule peptide with astatine-211. Preliminary evaluation in vitro and in vivo

  • 1. Sichuan University, Chengdu (China). Key Laboratory of Radiation Physics and Technology, Ministry of Education, Institute of Nuclear Science and Technology
  • 2. Sichuan Academy of Medical Sciences and Sichuan Provincial People's Hospital, Chengdu, Sichuan (China). Department of Respiration
  • 3. Third Military Medical University, Chongqing (China). Department of Nuclear Medicine, Southwest Hospital

Description

In this paper, VP2, a novel small molecule fusion peptide, was labelled with 211At through a one-step method (coupled with bifunctional intermediate SPC first and then labelled) with a radiochemical yield of about 45%. The radiochemical purity was still > 95% after 24 h at room temperature. Specificity studies in vitro indicated that 211At-SPC-VP2 has a high affinity for several tumour cells. Additionally, biodistribution in KM mice showed that 211At-SPC-VP2 has sufficient stability in vivo. This research suggested that 211At-SPC-VP2 produced by the convenient method has the potential to be a novel targeted drug for cancer radiotherapy. (author)

Additional details

Publishing Information

Journal Title
Journal of Radioanalytical and Nuclear Chemistry
Journal Volume
316
Journal Issue
2
Journal Page Range
p. 451-456
ISSN
0236-5731
CODEN
JRNCDM

Optional Information

Notes
28 refs.