International Journal of Molecular Sciences

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Dear Colleagues,

Cancer remains one of the leading causes of death worldwide. Despite the extensive research efforts, cancer drug research remains a remarkably challenging field, and therapeutic innovations are needed to achieve expected clinical results. Several molecular targets and the exposome implicated in disease development and progressions, thus these complex factors have to be taken under for drug design and delivery in cancers. The new era of mRNA-based therapeutics and nanomedicine opens new horizons in the drug design and therapeutics area. This Special Issue aims to include recent advances and challenges in the field of cancer molecular targeting, innovative ways for drug design and drug repurposing based on molecular profiles, nanomedicine and effective targeted drug delivery system.

Dr. Maria Gazouli
Guest Editor

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Keywords

molecular targeting
nanomedicine
drug delivery
targeting therapy
molecular imaging
theranostics

Published Papers (1 paper)

Research

17 pages, 2649 KiB

Open AccessArticle

Aptamers for Addressed Boron Delivery in BNCT: Effect of Boron Cluster Attachment Site on Functional Activity

by Darya S. Novopashina, Maya A. Dymova, Anna S. Davydova, Mariya I. Meschaninova, Daria O. Malysheva, Elena V. Kuligina, Vladimir A. Richter, Iaroslav A. Kolesnikov, Sergey Yu. Taskaev and Mariya A. Vorobyeva

Int. J. Mol. Sci. 2023, 24(1), 306; https://doi.org/10.3390/ijms24010306 - 24 Dec 2022

Cited by 1 | Viewed by 1692

Abstract

Among the great variety of anti-cancer therapeutic strategies, boron neutron capture therapy (BNCT) represents a unique approach that doubles the targeting accuracy due to the precise positioning of a neutron beam and the addressed delivery of boron compounds. We have recently demonstrated the principal possibility of using a cell-specific 2′-F-RNA aptamer for the targeted delivery of boron clusters for BNCT. In the present study, we evaluated the amount of boron-loaded aptamer inside the cell via two independent methods: quantitative real-time polymerase chain reaction and inductive coupled plasma–atomic emission spectrometry. Both assays showed that the internalized boron level inside the cell exceeds 1 × 10⁹ atoms/cell. We have synthesized closo-dodecaborate conjugates of 2′-F-RNA aptamers GL44 and Waz, with boron clusters attached either at the 3′- or at the 5′-end. The influence of cluster localization was evaluated in BNCT experiments on U-87 MG human glioblastoma cells and normal fibroblasts and subsequent analyses of cell viability via real-time cell monitoring and clonogenic assay. Both conjugates of GL44 aptamer provided a specific decrease in cell viability, while only the 3′-conjugate of the Waz aptamer showed the same effect. Thus, an individual adjustment of boron cluster localization is required for each aptamer. The efficacy of boron-loaded 2′-F-RNA conjugates was comparable to that of ¹⁰B-boronophenylalanine, so this type of boron delivery agent has good potential for BNCT due to such benefits as precise targeting, low toxicity and the possibility to use boron clusters made of natural, unenriched boron. Full article

(This article belongs to the Special Issue Recent Advances in Targeted Drug Discovery and Delivery in Cancer)

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