TY - JOUR
T1 - Cancer cell selective probe by mimicking EGCG
AU - Kumazoe, Motofumi
AU - Hiroi, Shun
AU - Tanimoto, Yousuke
AU - Miyakawa, Jyunichi
AU - Yamanouchi, Maasa
AU - Suemasu, Yumi
AU - Yoshitomi, Ren
AU - Murata, Motoki
AU - Fujimura, Yoshinori
AU - Takahashi, Takashi
AU - Tanaka, Hiroshi
AU - Tachibana, Hirofumi
N1 - Funding Information:
This work was supported in part by JSPS KAKENHI grant 22228002 and JP15H02448 to H. Tachibana and JST H. Tanaka. This work was also supported in part by a Grant-in-Aid for JSPS Fellows to M. K umazoe (PD) and JSPS KAKENHI grant JP15K18821, Kowa Life Science Foundation. We appreciate the technical assistance from The Research Support Center, Research Center for Human Disease Modeling, Kyushu University Graduate School of Medical Sciences.
Funding Information:
This work was supported in part by JSPS KAKENHI grant 22228002 and JP15H02448 to H. Tachibana and JST H. Tanaka. This work was also supported in part by a Grant-in-Aid for JSPS Fellows to M. K umazoe (PD) and JSPS KAKENHI grant JP15K18821 , Kowa Life Science Foundation . We appreciate the technical assistance from The Research Support Center, Research Center for Human Disease Modeling, Kyushu University Graduate School of Medical Sciences.
Publisher Copyright:
© 2020 Elsevier Inc.
PY - 2020/5/14
Y1 - 2020/5/14
N2 - 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.
AB - 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.
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U2 - 10.1016/j.bbrc.2020.03.021
DO - 10.1016/j.bbrc.2020.03.021
M3 - Article
C2 - 32173528
AN - SCOPUS:85081574798
SN - 0006-291X
VL - 525
SP - 974
EP - 981
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
IS - 4
ER -
