Induction of ADCC by a folic acid-mAb conjugate prepared by tryptophan-selective reaction toward folate-receptor-positive cancer cells

Hiroshi Tagawa; Katsuya Maruyama; Koichi Sasaki; Natsuki Konoue; Akihiro Kishimura; Motomu Kanai; Takeshi Mori; Kounosuke Oisaki; Yoshiki Katayama

doi:10.1039/d0ra03291c

Induction of ADCC by a folic acid-mAb conjugate prepared by tryptophan-selective reaction toward folate-receptor-positive cancer cells

RSC Adv. 2020 Apr 29;10(28):16727-16731. doi: 10.1039/d0ra03291c. eCollection 2020 Apr 23.

Authors

Hiroshi Tagawa¹, Katsuya Maruyama², Koichi Sasaki³, Natsuki Konoue², Akihiro Kishimura^{1

3

4}, Motomu Kanai², Takeshi Mori^{1

3}, Kounosuke Oisaki², Yoshiki Katayama^{1

3

4

5

6}

Affiliations

¹ Graduate School of Systems Life Sciences, Kyushu University Fukuoka Japan.
² Graduate School of Pharmaceutical Sciences, The University of Tokyo Tokyo Japan.
³ Department of Applied Chemistry, Faculty of Engineering, Kyushu University Fukuoka Japan.
⁴ International Research Center for Molecular Systems, Kyushu University Fukuoka Japan.
⁵ Center for Advanced Medical Innovation, Kyushu University Fukuoka Japan.
⁶ Department of Biomedical Engineering, Chung Yuan Christian University Taoyuan Taiwan.

Abstract

We developed conjugates between monoclonal antibody (mAb) and folic acid (FA) by using a tryptophan (Trp)-selective reaction, which yields relatively homogenous products compared to conventional methods. The obtained mAb-FA conjugates showed significant cellular cytotoxicity toward folate receptor-expressing cancer cells, demonstrating that the conjugates retained the Fc region's original function.