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Tumor vasculature-targeted 10B delivery by an Annexin A1-binding peptide boosts effects of boron neutron capture therapy.
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ABSTRACT: Background
p-Boronophenylalanine (10BPA) is a powerful 10B drug used in current clinical trials of BNCT. For BNCT to be successful, a high (500?mg/kg) dose of 10BPA must be administered over a few hours. Here, we report BNCT efficacy after rapid, ultralow-dose administration of either tumor vasculature-specific annexin A1-targeting IFLLWQR (IF7)-conjugated 10BPA or borocaptate sodium (10BSH).Methods
(1) IF7 conjugates of either 10B drugs intravenously injected into MBT2 bladder tumor-bearing mice and biodistribution of 10B in tumors and normal organs analyzed by prompt gamma-ray analysis. (2) Therapeutic effect of IF7-10B drug-mediated BNCT was assessed by either MBT2 bladder tumor bearing C3H/He mice and YTS-1 tumor bearing nude mice.Results
Intravenous injection of IF7C conjugates of either 10B drugs into MBT2 bladder tumor-bearing mice promoted rapid 10B accumulation in tumor and suppressed tumor growth. Moreover, multiple treatments at ultralow (10-20?mg/kg) doses of IF7-10B drug-mediated BNCT significantly suppressed tumor growth in a mouse model of human YTS-1 bladder cancer, with increased Anxa1 expression in tumors and infiltration by CD8-positive lymphocytes.Conclusions
We conclude that IF7 serves as an efficient 10B delivery vehicle by targeting tumor tissues via the tumor vasculature and could serve as a relevant vehicle for BNCT drugs.
SUBMITTER: Yoneyama T
PROVIDER: S-EPMC7809749 | biostudies-literature | 2021 Jan
REPOSITORIES: biostudies-literature
Publications
Tumor vasculature-targeted <sup>10</sup>B delivery by an Annexin A1-binding peptide boosts effects of boron neutron capture therapy.
BMC cancer 20210115 1
<h4>Background</h4>p-Boronophenylalanine (<sup>10</sup>BPA) is a powerful <sup>10</sup>B drug used in current clinical trials of BNCT. For BNCT to be successful, a high (500 mg/kg) dose of <sup>10</sup>BPA must be administered over a few hours. Here, we report BNCT efficacy after rapid, ultralow-dose administration of either tumor vasculature-specific annexin A1-targeting IFLLWQR (IF7)-conjugated <sup>10</sup>BPA or borocaptate sodium (<sup>10</sup>BSH).<h4>Methods</h4>(1) IF7 conjugates of eith ...[more]