論文

査読有り 国際誌
2020年5月14日

Cancer cell selective probe by mimicking EGCG.

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

525
4
開始ページ
974
終了ページ
981
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/j.bbrc.2020.03.021

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.

リンク情報
DOI
https://doi.org/10.1016/j.bbrc.2020.03.021
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/32173528

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