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

  • Weihao Liu
  • Huan Ma
  • Yu Tang
  • Qing Chen
  • Shuqun Peng
  • Jijun Yang
  • Jiali Liao
  • Yuanyou Yang
  • Qianwei Li
  • Ning Liu


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.


211At VP2 One-step labelling Biodistribution Cell binding 



This work was financially supported by the China National Natural Science Foundation (Grant No. 21371124).


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Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2018

Authors and Affiliations

  • Weihao Liu
    • 1
  • Huan Ma
    • 1
  • Yu Tang
    • 1
  • Qing Chen
    • 2
  • Shuqun Peng
    • 2
  • Jijun Yang
    • 1
  • Jiali Liao
    • 1
  • Yuanyou Yang
    • 1
  • Qianwei Li
    • 3
  • Ning Liu
    • 1
  1. 1.Key Laboratory of Radiation Physics and Technology, Ministry of Education, Institute of Nuclear Science and TechnologySichuan UniversityChengduChina
  2. 2.Department of RespirationSichuan Academy of Medical Sciences & Sichuan Provincial People’s HospitalChengduChina
  3. 3.Department of Nuclear Medicine, Southwest HospitalThird Military Medical UniversityChongqingChina

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