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Application of 5-LO (lipoxygenase) inhibitor for treatment of malignant tumor in blood system

A 5-LO, blood system technology, applied in the field of application of arachidonic acid 5-lipoxygenase in the treatment of hematological malignancies, can solve problems such as incurable, and achieve the effect of treating leukemia

Inactive Publication Date: 2013-02-06
JIAXING XIUGUANG BIOTECH CONSULTING CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Although there have been some therapeutic drugs for the treatment of malignant hematological diseases in recent years, they are still limited to controlling the development of the disease and relieving the pain of patients, and cannot be cured at all.

Method used

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  • Application of 5-LO (lipoxygenase) inhibitor for treatment of malignant tumor in blood system
  • Application of 5-LO (lipoxygenase) inhibitor for treatment of malignant tumor in blood system
  • Application of 5-LO (lipoxygenase) inhibitor for treatment of malignant tumor in blood system

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Embodiment Construction

[0046] The specific implementation will be described in detail below in conjunction with the accompanying drawings:

[0047] figure 1 showed that, compared with GFP+Lin-c-Kit+Sca-1+ cells that had no expression of BCR-ABL, the expression of Alox5 gene was upregulated by BCR-ABL in chronic myeloid leukemia CML stem cells, and this upregulation could not be detected by ImA Treatment with tinib (imatinib+) prevented.

[0048] figure 2 It is a quantitative RT-PCR analysis of a group of genes upregulated by BCR-ABL in leukemia stem cells. It can be seen that the expression of BCR-ABL changes before and after imatinib treatment. Mate (black box) and normal control group (gray box).

[0049] image 3 Alox5 gene expression is shown to be upregulated by BCR-ABL in leukemic stem cells (BCR-ABL, filled boxes) compared to GFP normal stem cells (vehicle, open boxes) (p<0.001).

[0050] DNA microarray analysis identified genes with altered expression caused by ALOX5 gene deletion in l...

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Abstract

The present invention relates to an application of a 5-LO (lipoxygenase) inhibitor for treatment of malignant tumor in a blood system. The hematological malignancy is confirmed to be leukemia relating to ALOX5 (Arachidonate) gene through test, and the hematologic tumor cancer gene ALOX5 directly causes the occurrence and development of the leukemia. The 5-LO inhibitor is also called zileuton with the formula of 1-[1-(1-Benzothiophen-2-yl)ethyl]-1-Hydroxyurea. The 5-LO inhibitor includes but not limited to N-hydroxyurea derivatives, comprising 1-[(2R-level)-4-[5-[(4-fluorophenyl)methyl]thiophene-2-yl]-N-2-yl]-1-hydroxyurea, also called ABT-761 and 1-[(5)-4-[3-(4-fluorophenyl)phenyl]-N-2-yl]-1-hydroxyurea, also called BW-B 70C.. The 5-LO inhibitor can be used for inhibiting the stem cells of leukemia so as to treat the hematological malignancies, and the inhibiting of the stem cells of leukemia can be used for inhibiting one or more hematological malignancy as well as symptoms at the phase of crisis.

Description

Technical field: [0001] The invention relates to the field of medicinal chemistry, in particular to the application of arachidonic acid 5-lipoxygenase in the treatment of hematological malignancies. Background technique: [0002] Hematological malignancies are a collective term for cancers of the blood, lymph nodes, and bone marrow. The tumors can be divided into the following groups: leukemia, lymphoma, myeloma, myelodysplastic syndrome (MDS) and myeloproliferative disorder (MPD). Common leukemia types are subdivided into five categories: acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML), chronic myeloid leukemia (CML), chronic lymphocytic leukemia (CLL) and hairy cell leukemia (HCL) . [0003] Chronic myelogenous leukemia (CML), also known as chronic myeloid leukemia or CML. CML is a cellular malignancy characterized by genetic abnormalities of hematopoietic stem cells, also known as Philadelphia chromosome positive (Druker, 2008; Faderl et al., 1999a; Fa...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K48/00A61P35/00
Inventor 李少光李东光
Owner JIAXING XIUGUANG BIOTECH CONSULTING CO LTD
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