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
2016; Elsevier BV; Volume: 237; Linguagem: Inglês
10.1016/j.jconrel.2016.07.017
ISSN1873-4995
AutoresShunsuke Kikuchi, Daisuke Kanoh, Shinichi Sato, Yoshinori Sakurai, Minoru Suzuki, Hiroyuki Nakamura,
Tópico(s)Medical Imaging Techniques and Applications
ResumoMaleimide-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.
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