том 56 издание 18 страницы 7222-7231

Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity

Тип публикацииJournal Article
Дата публикации2013-09-05
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR1.726
CiteScore11.5
Impact factor6.8
ISSN00222623, 15204804
Drug Discovery
Molecular Medicine
Краткое описание
Histone N(ε)-methyl lysine demethylases KDM2/7 have been identified as potential targets for cancer therapies. On the basis of the crystal structure of KDM7B, we designed and prepared a series of hydroxamate analogues bearing an alkyl chain. Enzyme assays revealed that compound 9 potently inhibits KDM2A, KDM7A, and KDM7B, with IC50s of 6.8, 0.2, and 1.2 μM, respectively. While inhibitors of KDM4s did not show any effect on cancer cells tested, the KDM2/7-subfamily inhibitor 9 exerted antiproliferative activity, indicating the potential for KDM2/7 inhibitors as anticancer agents.
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ГОСТ |
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Suzuki T. et al. Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity // Journal of Medicinal Chemistry. 2013. Vol. 56. No. 18. pp. 7222-7231.
ГОСТ со всеми авторами (до 50) Скопировать
Suzuki T., Ozasa H., Itoh Y., Zhan P., Sawada H., Mino K., Walport L. J., Ohkubo R., Kawamura A., Yonezawa M., Tsukada Y., Tumber A., NAKAGAWA H., Hasegawa M., SASAKI R., MIZUKAMI T., Schofield C. J., Miyata N. Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity // Journal of Medicinal Chemistry. 2013. Vol. 56. No. 18. pp. 7222-7231.
RIS |
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TY - JOUR
DO - 10.1021/jm400624b
UR - https://doi.org/10.1021/jm400624b
TI - Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity
T2 - Journal of Medicinal Chemistry
AU - Suzuki, Takayoshi
AU - Ozasa, Hiroki
AU - Itoh, Yukihiro
AU - Zhan, Peng
AU - Sawada, Hideyuki
AU - Mino, Koshiki
AU - Walport, Louise J
AU - Ohkubo, Rei
AU - Kawamura, Akane
AU - Yonezawa, Masato
AU - Tsukada, Yuichi
AU - Tumber, Anthony
AU - NAKAGAWA, HIDEHIKO
AU - Hasegawa, Makoto
AU - SASAKI, RYUZO
AU - MIZUKAMI, TAMIO
AU - Schofield, Christopher J.
AU - Miyata, N.
PY - 2013
DA - 2013/09/05
PB - American Chemical Society (ACS)
SP - 7222-7231
IS - 18
VL - 56
PMID - 23964788
SN - 0022-2623
SN - 1520-4804
ER -
BibTex |
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BibTex (до 50 авторов) Скопировать
@article{2013_Suzuki,
author = {Takayoshi Suzuki and Hiroki Ozasa and Yukihiro Itoh and Peng Zhan and Hideyuki Sawada and Koshiki Mino and Louise J Walport and Rei Ohkubo and Akane Kawamura and Masato Yonezawa and Yuichi Tsukada and Anthony Tumber and HIDEHIKO NAKAGAWA and Makoto Hasegawa and RYUZO SASAKI and TAMIO MIZUKAMI and Christopher J. Schofield and N. Miyata},
title = {Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity},
journal = {Journal of Medicinal Chemistry},
year = {2013},
volume = {56},
publisher = {American Chemical Society (ACS)},
month = {sep},
url = {https://doi.org/10.1021/jm400624b},
number = {18},
pages = {7222--7231},
doi = {10.1021/jm400624b}
}
MLA
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Suzuki, Takayoshi, et al. “Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity.” Journal of Medicinal Chemistry, vol. 56, no. 18, Sep. 2013, pp. 7222-7231. https://doi.org/10.1021/jm400624b.
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