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Title 

A novel γ-lactam-based histone deacetylase inhibitor potently inhibits the growth of human breast and renal cancer cells

Authors 

H K KwonS H AhnS H ParkJ H ParkJ W ParkHwan Mook KimSong Kyu ParkKiho LeeChag Woo LeeE ChoiG HanJ W Han

Publisher 

Pharmaceutical Society of Japan

Issue Date 

2009

Citation 

Biological & Pharmaceutical Bulletin, vol. 32, no. 10, pp. 1723-1727

Keywords 

γ-lactam hydroxamic acidAntiproliferationApoptosisHistone deacetylasep21WAF1/Cip1

Abstract 

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 suberoylanilide 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.

ISSN 

0918-6158

Link 

http://dx.doi.org/10.1248/bpb.32.1723

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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