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Application of vitamin K in preparation of pyruvate kinase inhibitor

A pyruvate kinase and vitamin technology, which can be used in drug combinations, antitumor drugs, etc., can solve the problem of no vitamin K compounds inhibiting pyruvate kinase and the like

Inactive Publication Date: 2013-09-18
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, no vitamin K compounds have been reported to inhibit the activity of pyruvate kinase

Method used

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  • Application of vitamin K in preparation of pyruvate kinase inhibitor
  • Application of vitamin K in preparation of pyruvate kinase inhibitor
  • Application of vitamin K in preparation of pyruvate kinase inhibitor

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Experimental program
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Embodiment Construction

[0013] The present invention is further described below in conjunction with specific embodiment, but protection scope of the present invention is not limited thereto:

[0014] Experimental Materials:

[0015] Vitamin K3 was purchased from Sigma, and vitamin K5 was purchased from Wako.

[0016] Recombinant PKM2: the gene was cloned from breast cancer cell MCF-7, the gene was integrated into plasmid pQE-30 (purchased from Qiagen), transformed into Escherichia coli XL1 Blue (purchased from Qiagen), sequenced by Invitrogen, NCBI database In comparison, the cloned gene was indeed the PKM2 gene (SEQ ID NO.1), and the PKM2 protein was induced and expressed by IPTG (purchased from Gibco), and PKM2 was purified by Ni-Sepharose chromatography column (purchased from GE). protein (SEQ ID NO. 2).

[0017] β-NADH, ADP and phosphoenolpyruvate (PEP) were purchased from Roche;

[0018] Tris, HCl, KCl, and MgCl were purchased from Haotian Company.

[0019] Dimethylsulfoxide (DMSO) and lacta...

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Abstract

The invention provides two inhibitors of M2 type pyruvate kinase (PKM2)-vitamin K type compounds (vitamin K3 and vitamin K5). The currently reported PKM2 inhibitor which belongs to small molecular compounds is Compound 3 only. The effect of the vitamin K on inhabitation of the PKM2 is found to be higher than that of the Compound 3. Therefore, as an inhibitor of pyruvic acid, the vitamin K has important application value. Two new pyruvate kinase inhibitors-vitamin K3 and vitamin K5 are provided, provide basis for selection of new medicaments and have important application prospect.

Description

(1) Technical field [0001] The present invention mainly relates to the application of vitamin K compounds (vitamin K3, K5) in the preparation of pyruvate kinase inhibitors. (2) Background technology [0002] Two kinds of vitamin K compounds (vitamin K3, K5) that the present invention mainly relates to are synthetic naphthoquinone compounds, and its structural formula is as follows: [0003] [0004] Pyruvate kinase is a key rate-limiting enzyme in glycolysis and plays a key role in energy metabolism. The M2-type pyruvate kinase (PKM2 for short) involved in the present invention mainly exists in the early development of individuals and tumor tissues. There are very few PKM2 inhibitors reported so far, among which small molecule compound inhibitors are only one case of compound 3 (Vander Heiden MG, Christofk HR, Schuman E, Subtelny AO, Sharfi H, Harlow EE et al. Biochem Pharmacol2010, 79, 1118. ), the amount that inhibits 50% of the enzyme activity (i.e. IC50) is 50 μM. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/136A61K31/122A61P35/00
Inventor 胡汛陈晶
Owner ZHEJIANG UNIV