TY - JOUR
T1 - Maleimide-functionalized closo-dodecaborate albumin conjugates (MID-AC)
T2 - Unique ligation at cysteine and lysine residues enables efficient boron delivery to tumor for neutron capture therapy
AU - Kikuchi, Shunsuke
AU - Kanoh, Daisuke
AU - Sato, Shinichi
AU - Sakurai, Yoshinori
AU - Suzuki, Minoru
AU - Nakamura, Hiroyuki
N1 - Funding Information:
This work was supported by a Grant-in-Aid for Scientific Research (B) (No. 26293007 ) from the Ministry of Education, Culture, Sports, Science and Technology, Japan , Terumo Foundation for Life Sciences and Arts , Terumo Foundation for Life Science and Art , and the Cooperative Research Program of “Network Joint Research Center for Materials and Devices.” We thank Professor Mitsunori Kirihata (Osaka Prefecture University) for the kind donation of anti-BSH antibody and Dr. Hyun Seung Ban (Korea Research Institute of Bioscience and Biotechnology) for statistical analysis.
Publisher Copyright:
© 2016 Elsevier B.V.
PY - 2016/9/10
Y1 - 2016/9/10
N2 - 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.
AB - 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.
KW - Albumin modification
KW - Boron delivery system
KW - Boron neutron capture therapy (BNCT)
KW - Closo-dodecaborate
KW - Maleimide
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U2 - 10.1016/j.jconrel.2016.07.017
DO - 10.1016/j.jconrel.2016.07.017
M3 - Article
C2 - 27422608
AN - SCOPUS:84978387796
VL - 237
SP - 160
EP - 167
JO - Journal of Controlled Release
JF - Journal of Controlled Release
SN - 0168-3659
ER -