title: 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.
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.
authors.affiliation: Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, Yokohama, Japan.
authors.forename: Shunsuke
authors.initials: S
authors.lastname: Kikuchi
authors.affiliation: Department of Chemistry, Faculty of Science, Gakushuin University, Tokyo, Japan.
authors.forename: Daisuke
authors.initials: D
authors.lastname: Kanoh
authors.affiliation: Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, Yokohama, Japan.
authors.forename: Shinichi
authors.initials: S
authors.lastname: Sato
authors.affiliation: Department of Radiation Life Science and Radiation Medical Science, Kyoto University Research Reactor Institute, Osaka, Japan.
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Sakurai
authors.affiliation: Particle Radiation Oncology Research Center, Kyoto University Research Reactor Institute, Osaka, Japan.
authors.forename: Minoru
authors.initials: M
authors.lastname: Suzuki
authors.affiliation: Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, Yokohama, Japan. Electronic address: hiro@res.titech.ac.jp.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Nakamura
mesh_terms: D000818:Animals; D001895:Boron / Q000008:administration & dosage* / Q000627:therapeutic use; D001896:Boron Compounds / Q000737:chemistry*; D016754:Boron Neutron Capture Therapy / Q000379:methods*; D002460:Cell Line; D003545:Cysteine / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D005260:Female; D008239:Lysine / Q000737:chemistry; D008301:Maleimides / Q000737:chemistry*; D051379:Mice; D008807:Mice, Inbred BALB C; D008958:Models, Molecular; D009369:Neoplasms / Q000532:radiotherapy*; D012710:Serum Albumin, Bovine / Q000737:chemistry*
chemical_list: D001896:Boron Compounds; D004337:Drug Carriers; D008301:Maleimides; C119788:dodecaborate; D012710:Serum Albumin, Bovine; D008239:Lysine; D003545:Cysteine; D001895:Boron
keywords: Albumin modification; Boron delivery system; Boron neutron capture therapy (BNCT); Closo-dodecaborate; Maleimide