A Novel γ-Lactam-Based Histone Deacetylase Inhibitor Potently Inhibits the Growth of Human Breast and Renal Cancer Cells
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概要
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We evaluated the novel γ-lactam-based analogue, KBH-A145, for its anticancer activities. KBH-A145 markedly inhibited histone deacetylase (HDAC) activity in vitro and in vivo to an extent comparable to suberoyl-anilide hydroxamic acid (SAHA). The proliferation of various types of cancers was significantly suppressed by KBH-A145, among which MDA-MB-231 and MCF, human breast cancer cells and ACHN human renal cancer cells, were most sensitive. This was accompanied by induction of p21WAF1/Cip1 through compromised recruitment of HDAC1, which leads to hyperacetylation of its promoter region and thus arrested both cells in the G2/M phase. Interestingly, this compound induced apoptosis of MDA-MB-231 cells, but not ACHN cells, through cleavage of poly(ADP-ribose) polymerase (PARP). Taken together, these results show that this novel γ-lactam-based HDAC inhibitor potently inhibits the growth of human breast and renal cancer cells. Thus KBH-A145 is a potential therapeutic agent for the treatment of these types of cancer.
著者
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HAN Jeung-Whan
College of Pharmacy, Sungkyunkwan University
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Han Jeung-whan
College Of Pharmacy Sungkyunkwan University
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Ahn Seong
Division of Molecular & Life Science, Hanyang University
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Park Jong
College Of Pharmacy Pusan National University
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LEE Kiho
Bioevaluation Center, Korea Research Institute of Bioscience and Biotechnology
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PARK Song-Kyu
Bioevaluation Center, Korea Research Institute of Bioscience and Biotechnology
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KIM Hwan
Bioevaluation Center, Korea Research Institute of Bioscience and Biotechnology
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Park Song-kyu
Bioevaluation Center Korea Research Institute Of Bioscience And Biotechnology
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Kim Hwan
Bioevaluation Center Korea Research Institute Of Bioscience And Biotechnology
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PARK Se
College of Veterinary Medicine, Seoul National University
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Kwon Hyoung
College of Pharmacy, Sungkyunkwan University
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Park Jae
College of Pharmacy, Sungkyunkwan University
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Lee Chang-Woo
Bioevaluation Center, KRIBB
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Choi Eunhyun
Department of Biotechnology, Yonsei University
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Han Gyoonhee
Department of Biotechnology, Yonsei University
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Park Se
College Of Applied Life Science Jeju National University
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Kim Hwan
Bioevaluation Center, KRIBB
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Park Se
College of Pharmacy, Sungkyunkwan University
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Park Song-Kyu
Bioevaluation Center, KRIBB
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Park Jong
College of Pharmacy, Sungkyunkwan University
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Lee Kiho
Bioevaluation Center, KRIBB
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