An HDAC inhibitor
Chidamide is a novel benzamide-type histone deacetylase (HDAC) inhibitor. People have investigated the effects of CS055 on proliferation, differentiation and apoptosis in human leukaemia cell lines and primary myeloid leukaemia cells.[1]
Histone deacetylases (HDACs) is a series of enzymes functioning to acetylate and deacetylate the amino-terminal lysine residues of histones, which result in the remodeling of the chromatin structures and affect the accessibility of the chromatin to transcription factors to start gene transcription.[2]
Chidamide has effect on cell cycle, it significantly reduced the S phase cell fraction, while inducing a marked increase in the G1 phase cell fraction in BEL-7402 and HCC-9204 cells with different p53 statuses. Chidamide signifiantly altered the number of cells in the phase fractions with an increase in dose.[2]
The results of the present study suggest that Chidamide is a HDACi with potential therapeutic value in several haematological malignancies via the inhibition of cell proliferation, inducing differentiation and apoptosis in human cells. Chidamide is a new HDACi with potential therapeutic values in several haematological malignancies via the inhibition of cell proliferation, inducing differentiation and apoptosis in human leukaemia cells.[1]
参考文献:
[1] Gong K,?Xie J,?Yi H,?Li W.? CS055?(Chidamide/HBI-8000), a?novel?histone?deacetylase?inhibitor,?induces?G1?arrest,?ROS-dependent?apoptosisand?differentiation?in?human?leukaemia?cells. Biochem J.?2012 May 1;443(3):735-46.
[2] Wang H1,?Guo Y,?Fu M,?Liang X, etal.? , Antitumor?activity?of?Chidamide?in?hepatocellular?carcinoma?cell?lines. Mol Med Rep.?2012 Jun;5(6):1503-8.
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