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

Shunsuke Kikuchi, Daisuke Kanoh, Shinichi Sato, Yoshinori Sakurai, Minoru Suzuki, Hiroyuki Nakamura

Research output: Contribution to journalArticle

21 Citations (Scopus)

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 languageEnglish
Pages (from-to)160-167
Number of pages8
JournalJournal of Controlled Release
Volume237
DOIs
Publication statusPublished - 2016 Sep 10
Externally publishedYes

Keywords

  • Albumin modification
  • Boron delivery system
  • Boron neutron capture therapy (BNCT)
  • Closo-dodecaborate
  • Maleimide

ASJC Scopus subject areas

  • Pharmaceutical Science

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