α‐Emitting cancer therapy using 211At‐AAMT targeting LAT1

• DOI: 10.1111/cas.14761
• Publication Date: 2020-12-05T08:15:06Z
• Authors: Kazuko Kaneda‐Nak...; ZiJian Zhang; Yoshiyuki Manabe; Atsushi Shimoyama; Kazuya Kabayama; Tadashi Watabe; Yoshikatsu Kanai; Kazuhiro Ooe; Atsushi Toyoshima; Yoshifumi Shirakami; Takashi Yoshimura; Mitsuhiro Fukuda; Jun Hatazawa; Takashi Nakano; Koichi Fukase; Atsushi Shinohara
• Keywords: Radionuclide therapy; Cancer Therapy; Amino acid transporter

Abstract α‐Methyl‐ l ‐tyrosine (AMT) has a high affinity for the cancer‐specific ‐type amino acid transporter 1 (LAT1). Therefore, we established an anti‐cancer therapy, with 211 At‐labeled α‐methyl‐ ( At‐AAMT) as carrier of At into tumors. At‐AAMT had LAT1, inhibited tumor cell growth, and induced DNA double‐stranded breaks in vitro . We evaluated accumulation vivo role LAT1. Treatment 0.4 MBq/mouse growth PANC‐1 model metastasis lung B16F10 model. Our results suggested that would be useful therapy LAT1 is suitable target radionuclide therapy.