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

Liu, Weihao; Ma, Hongxia; Tang, Yu; Chen, Qing; Peng, Shuqun; Yang, Jijun; Liao, Jiali; Yang, Yuanyou; Li, Qianwei; Liu, Ning

doi:10.1007/s10967-018-5780-x

Cited by 14 publications

(7 citation statements)

References 24 publications

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“… 33 Liu et al radiolabeled a small-molecule peptide with 211 At by using an N-succinimidyl 5-(tributylstannyl)-3-pyridinecarboxylate ester precursor and reported the stomach uptake to be 5.55%ID/g 3 h after intravenous injection. 34 However, in a subsequent therapy study using this molecule, gastric toxicity was observed at higher doses. 35 In summary, although different animal models were used, uptake of 211 At activity in the stomach and thyroid after injection of 211 At-labeled GNS is lower than that observed for most other 211 At-labeled TAT agents, including those that have either been investigated clinically or will soon enter clinical trials.…”

Section: Discussionmentioning

confidence: 98%

Gold Nanostars: A Novel Platform for Developing 211At-Labeled Agents for Targeted Alpha-Particle Therapy

Liu

Zhou

Feng

et al. 2021

IJN

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Section: Discussionmentioning

confidence: 98%

Gold Nanostars: A Novel Platform for Developing 211At-Labeled Agents for Targeted Alpha-Particle Therapy

Liu

Zhou

Feng

et al. 2021

IJN

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“…For instance, Weihao Liu et al. [ 23 ] labeled a novel small molecule fusion peptide, VP2, with 211 At through a one-step method and the TAT conjugate had a high affinity for tumor cells expressing vasoactive intestinal peptide receptors (VIPRs); Charles Zhu et al . [ 30 ] presented a transmission dosimetry design for alpha particles using A549 lung carcinoma cells, an external alpha particle emitting source (radium 223; Ra-223) and a Timepix pixelated semiconductor detector.…”

Section: Discussionmentioning

confidence: 99%

“…211 At was produced by the 209 Bi (α, 2n) 211 At nuclear reaction on the CS-30 cyclotron accelerator in Sichuan University, detailed procedures as reported elsewhere [ 23 ]. 131 I was bought from Chengdu Gaotong Isotope Co., Ltd. (CNNC).…”

Section: Methodsmentioning

confidence: 99%

Construction and Preclinical Evaluation of 211At Labeled Anti-mesothelin Antibodies as Potential Targeted Alpha Therapy Drugs

Wang

Liu

et al. 2020

Journal of Radiation Research

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ABSTRACT Targeted alpha therapy (TAT) is a promising tumor therapy that can specifically transport α particle to the vicinity of tumor cells while the normal cells are only slightly irradiated. Mesothelin is a highly promising molecular signature for many types of solid tumors including malignant mesothelioma, pancreatic cancer, ovarian cancer and lung adenocarcinoma etc., while the expression in normal human tissues are limited, thus making mesothelin a promising antigen for TAT. Previously we developed a theoretical model that could predict and optimize in vitro screening of potential TAT drugs. The aim of the study is construction and preclinical evaluation of 211At labeled anti-mesothelin antibodies as potential TAT drugs. Mesothelin expression of two tumor cell lines were confirmed by flow cytometry, and their radiosensitivities were also evaluated. We used two kinds of anti-mesothelin antibodies, ET210–6 and ET210–28, to construct TAT drugs. Then, radiochemical purity, stability in vitro, affinity of the conjugates and mesothelin expression level were assessed. The specific killing of mesothelin-positive cancer cells treated by 211At-ET210–28 and 211At-ET210–6 were studied via Cell Counting Kit-8 assay and colony formation assay. 211At-ET210–28 and 211At-ET210–6 revealed excellent affinity and stability in both phosphate buffer saline and fetal bovine serum environment. Radiolabeled antibody conjugates bound specifically to mesothelin-positive cells in vitro. Both 211At-ET210–28 and 211At-ET210–6 could specifically kill mesothelin-positive cells with negligible damages to mesothelin-negative cells. Our findings provide initial proof-of-concept for the potential use of 211At labeled ET210–28/ET210–6 anti-mesothelin antibody in specific killings of mesothelin-positive tumor cells.

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“…Based on homemade 211 At, several research works on 211 At-labeled agents have been carried out. Using N-succinimidyl-5-(tributylstannyl)-3-pyridinecarboxylate (SPC) as a bi-functional linker [91], a one-step method was used for the preparation of [ 211 At]At-SPC-VP2 peptide [92]. The following research suggests that [ 211 At]At-SPC-VP2 has good in vivo stability and shows potential for targeted cancer radiotherapy.…”

Section: Therapeutic Radiopharmaceuticalsmentioning

confidence: 99%

Current status and future perspective of radiopharmaceuticals in China

Ji¹,

Li²,

Sui³

et al. 2021

Eur J Nucl Med Mol Imaging

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

Cited by 14 publications

References 24 publications

Gold Nanostars: A Novel Platform for Developing 211At-Labeled Agents for Targeted Alpha-Particle Therapy

Gold Nanostars: A Novel Platform for Developing 211At-Labeled Agents for Targeted Alpha-Particle Therapy

Construction and Preclinical Evaluation of 211At Labeled Anti-mesothelin Antibodies as Potential Targeted Alpha Therapy Drugs

Current status and future perspective of radiopharmaceuticals in China

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