Spermidine/spermine n1-acetyltransferase substrates as anti-cancer drug compounds

A technology of acetyltransferase and anticancer drugs, which is applied in the field of spermidine/spermine N1-acetyltransferase substrates used as anticancer drug compounds, and can solve problems such as increased enzyme activity

Inactive Publication Date: 2015-09-16
BIOMARK TECH
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  • Abstract
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  • Claims
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Problems solved by technology

[0004] It has also been reported that the expression of SSAT and its enzyme activity may be increased after chemotherapy or treatment with spermidine analogues

Method used

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  • Spermidine/spermine n1-acetyltransferase substrates as anti-cancer drug compounds
  • Spermidine/spermine n1-acetyltransferase substrates as anti-cancer drug compounds
  • Spermidine/spermine n1-acetyltransferase substrates as anti-cancer drug compounds

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Embodiment Construction

[0026] The invention discloses a method of combining spermidine / spermine N 1 - Methods of acetyltransferase (SSAT) substrates as anticancer drug compounds.

[0027] Relative expression levels of SSAT in human tumor cell lines HEK-293, Malme-3M, HeLa, PC-3 and US-02 were determined by reverse transcription-quantitative polymerase chain reaction analysis (RT-qPCR analysis), and Such as figure 1 with figure 2 As shown, it was observed that the relative expression of SSAT in Malme-3M was the highest. When normalized by GAPDH, the relative expression of SSAT in Malme-3M was 11 times higher than that of the control HEK-293 cell line. When normalized by HPRT1, The relative expression of SSAT in Malme-3M was 58 times higher than that in the control HEK-293 cell line. The relative expression level of SSAT in PC-3 was the second highest, and when normalized by GAPDH and HPRT1, the relative expression level of SSAT in PC-3 was about 3-fold and 7-fold different from HEK-293, respectiv...

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Abstract

ABSTRACT OF THE DISCLOSURE An anti-cancer drug compound comprises an spermidine / spermine N -acetyltransferase substrate. The spermidine / spermine N -acetyltransferase substrate may be a monoamine. The spermidine / spermine N -acetyltransferase substrate may be amantadine, rimantadine, dopamine or L-DOPA. A method of treating cancer comprises the use of an spermidine / spermine N -acetyltransferase substrate to treat cancer. The spermidine / spermine N -acetyltransferase substrate may be a monoamine. The spermidine / spermine N -acetyltransferase substrate may be amantadine, rimantadine, dopamine or L-DOPA.

Description

technical field [0001] The present invention relates to a method for analyzing spermidine / spermine N in cancer cells upregulated by mRNA (messenger ribonucleic acid). 1 - Methods of acetyltransferase (SSAT) activity, in particular the use of SSAT substrates as anticancer drug compounds and in anticancer therapy. Background technique [0002] U.S. Patent No. 6,811,967, issued November 4, 2004 to Sitar et al., the entire disclosure of which is hereby incorporated by reference, discloses the use of SSAT substrates for A method for the analysis of SSAT enzyme activity. SSAT substrates may include amantadine, wherein amantadine is metabolized in part by the action of the inducible enzyme SSAT to produce the acetylated metabolite N-acetylamantadine. Correlation of SSAT activity with pathological conditions is also disclosed. [0003] SSAT is an important enzyme in polyamine metabolism. Polyamines, including spermidine and spermine, are essential for cell survival, and SSAT is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/137A61K31/13A61P35/00
CPCA61K31/13A61K31/137A61K31/198A61P35/00
Inventor 布莱恩·郑拉希德·卜克思德瑞克·郑
Owner BIOMARK TECH
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