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

Authors:   Shunsuke Kikuchi,Daisuke Kanoh,Shinichi Sato,Yoshinori Sakurai,Minoru Suzuki,Hiroyuki Nakamura,
Journal: Journal of Controlled Release
https://doi.org/10.1016/j.jconrel.2016.07.017
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.