Abstract
Maleimide-conjugating closo-dodecaborate sodium form 5c (MID) synthesized by the nucleophilic ring-opening reaction of closo-dodecaborate-1,4-dioxane complex 2 with tetrabutylammonium (TBA) azide was found to conjugate to free SH of cysteine and lysine residues in BSA under physiological conditions, forming highly boronated BSA that showed high and selective accumulation in tumor and significant tumor growth inhibition in colon 26 tumor-bearing mice subjected to thermal neutron irradiation.
| Original language | English |
|---|---|
| Pages (from-to) | 160-167 |
| Number of pages | 8 |
| Journal | Journal of Controlled Release |
| Volume | 237 |
| DOIs | |
| Publication status | Published - 2016 Sep 10 |
| Externally published | Yes |
Keywords
- Albumin modification
- Boron delivery system
- Boron neutron capture therapy (BNCT)
- Closo-dodecaborate
- Maleimide
ASJC Scopus subject areas
- Pharmaceutical Science
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Cite this
Kikuchi, S., Kanoh, D., Sato, S., Sakurai, Y., Suzuki, M., & Nakamura, H. (2016). Maleimide-functionalized closo-dodecaborate albumin conjugates (MID-AC): Unique ligation at cysteine and lysine residues enables efficient boron delivery to tumor for neutron capture therapy. Journal of Controlled Release, 237, 160-167. https://doi.org/10.1016/j.jconrel.2016.07.017