Cancer cell selective probe by mimicking EGCG

Motofumi Kumazoe, Shun Hiroi, Yousuke Tanimoto, Jyunichi Miyakawa, Maasa Yamanouchi, Yumi Suemasu, Ren Yoshitomi, Motoki Murata, Yoshinori Fujimura, Takashi Takahashi, Hiroshi Tanaka, Hirofumi Tachibana

研究成果: Contribution to journalArticle

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Targeting proteins that are overexpressed in cancer cells is the major strategy of molecular imaging and drug delivery systems. The 67-kDa laminin receptor (67LR), also known as oncofetal antigen, is overexpressed in several types of cancer, including melanoma, multiple myeloma, cervical cancer and bile duct carcinoma. 67LR is involved in tumour growth, tumour metastasis and drug resistance. Green tea polyphenol (−)-epigallocatechin-3-O-gallate (EGCG) directly binds to cell-surface 67LR and induces apoptosis through the protein kinase B (Akt)/endothelial nitric oxide synthase/nitric oxide/cyclic GMP (cGMP) axis. Here we report the optimum hydroxyl group for the utilization of EGCG as a novel fluorescent EGCG-mimic imaging probe based on 67LR agonist characters, including Akt activation and inhibitory effect on viable cell number in cancer cells. 67LR specific targeting is unambiguously confirmed with the use of a non-labelled EGCG competitive assay and 67LR knockdown. Importantly, this probe strongly binds to multiple myeloma cells compared with its binding to normal cells.

ジャーナルBiochemical and Biophysical Research Communications
出版物ステータス出版済み - 5 14 2020

All Science Journal Classification (ASJC) codes

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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    Kumazoe, M., Hiroi, S., Tanimoto, Y., Miyakawa, J., Yamanouchi, M., Suemasu, Y., Yoshitomi, R., Murata, M., Fujimura, Y., Takahashi, T., Tanaka, H., & Tachibana, H. (2020). Cancer cell selective probe by mimicking EGCG. Biochemical and Biophysical Research Communications, 525(4), 974-981.