期刊
MOLECULAR PHARMACEUTICS
卷 17, 期 10, 页码 3885-3899出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.0c00630
关键词
boron neutron capture therapy; cancer therapeutics; carbohydrates; glucose transporters; medicinal chemistry; drug delivery
资金
- Jane and Aatos Erkko foundation
- Cancer foundation
- Swedish Cultural foundation
- Ruth and Nils-Erik Stenback foundation
- Finnish Academy of Science and Letters
- University of Helsinki research funds
- Academy of Finland [308329, 318422, 289179, 319453]
- Waldemar von Frenckell foundation
- Academy of Finland (AKA) [308329, 318422, 319453, 318422, 319453, 308329, 289179, 289179] Funding Source: Academy of Finland (AKA)
Boron neutron capture therapy (BNCT) for cancer is on the rise worldwide due to recent developments of in-hospital neutron accelerators which are expected to revolutionize patient treatments. There is an urgent need for improved boron delivery agents, and herein we have focused on studying the biochemical foundations upon which a successful GLUT1-targeting strategy to BNCT could be based. By combining synthesis and molecular modeling with affinity and cytotoxicity studies, we unravel the mechanisms behind the considerable potential of appropriately designed glucoconjugates as boron delivery agents for BNCT. In addition to addressing the biochemical premises of the approach in detail, we report on a hit glucoconjugate which displays good cytocompatibility, aqueous solubility, high transporter affinity, and, crucially, an exceptional boron delivery capacity in the in vitro assessment thereby pointing toward the significant potential embedded in this approach.
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