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Application of TRPC in screening antitumour medicine and medical use of its inhibitor

A technology of inhibitors and uses, applied in the field of cell biology, can solve the problems of complex tumor growth and proliferation

Inactive Publication Date: 2007-04-18
SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the growth and proliferation of tumors is still a complex problem without a complete answer. Therefore, there is an urgent need in this field to study ion channels and related pathways related to tumor growth and proliferation, and to develop drugs targeting related pathways or targets to inhibit tumor cells. proliferating compound

Method used

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  • Application of TRPC in screening antitumour medicine and medical use of its inhibitor
  • Application of TRPC in screening antitumour medicine and medical use of its inhibitor
  • Application of TRPC in screening antitumour medicine and medical use of its inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 High expression of TRPC3 and TRPC6 in several tumor samples

[0045] The expression levels of TRPC channel subtypes in some tumors were detected by conventional RT-PCR method. The tumor cell lines used are: glioblastoma (GBM, glioblastoma), breast cancer, endometrial cancer, and ovarian cancer cell lines.

[0046] The test results are shown in Figure 1, human glioblastoma U251 (purchased from the Cell Bank of the Chinese Academy of Sciences), A172 (ATTC No.: CRL-1620) cell line and rat glioma cell line C6 (ATTC No.: CCL -107), mainly expressed TRPC1, TRPC3 and TRPC6 channels (Fig. 1A). Breast cancer cell line MCF-7 (ATTC No.: HTB-22), ovarian cancer cell line SKOV3 (ATTC No.: HTB-77), and liver cancer cell line 7721 (purchased from the Cell Bank of the Chinese Academy of Sciences) and glioblasts Tumor cell lines similarly mainly expressed TRPC1, TRPC3 and TRPC6 channels, and endometrial cancer cell line HEC-1A (ATTC No.: HTB-112) mainly expressed TRPC1 and T...

Embodiment 2

[0053] Example 2 Growth factors BDNF and EGF can induce TRPC-specific inward current in tumor cell SKOV3

[0054] Growth factors, as extracellular stimuli, are crucial to the proliferation of tumor cells. Whether growth factors cause extracellular calcium to enter the cell through TRPC channels, increase the intracellular calcium concentration, and achieve the purpose of promoting its proliferation is still unclear. The present inventors applied BDNF (purchased from Sigma) and EGF (purchased from Sigma) to the culture medium of ovarian cancer cell lines. As shown in FIG. 5 , both BDNF and EGF can induce a slow inward current on SKOV3. Through the analysis of the IV curve of its current, this inward current is similar to the bidirectional rectification characteristic of TRPC (Fig. 6A, 6B). And found, this electric current can be blocked by TRPC channel agent SK&F96365 (1-[β-[3-(4-methoxyphenyl) propoxy]-4-p-methoxyphenol]-1-hydrogen-imidazole Hydrochloride, C 22 h 26 N 2 o...

Embodiment 3

[0056] Example 3 TRPC channel blockers inhibit the proliferation of glioma cells U251 and C6

[0057] Example 2 proves that the TRPC channel blocker SK&F96365 blocks the TRPC-like inward current induced by growth factors on tumor cells. This example further confirms that SK&F96365 inhibits the proliferation of tumor cells by blocking TRPC channels.

[0058] The specific test method is as follows: 10 μM SK&F96365 was added to the cultured glioblastoma C6 cells and U251 cells respectively. Compared with the solvent control, SK&F96365 could significantly inhibit the proliferation of the two tumor cells. The activation of phospholipase C (PLC) and inositol triphosphate (InsP3) acting on the receptor (IP3R) on its endoplasmic reticulum can activate TRPC channels [Montell, C. et al., Mol.Cell.9, 229-231. ]. The inventors used 9 μM PLC inhibitor U73122 (1-[6-[((17β)-3-methoxyestr-1,3,5[10]-triethylenetetramine-17-yl)amino]hexyl ]-1H-pyrrole-2,5-dione, C 29 h 40 N 2 o 3 , purch...

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Abstract

The invention discloses a method to screen compounds which can suppress tumor cells multiplication by suppressing TRPC ion channel. Use of TRPC inhibitor in preparing medicine for curing tumor is also disclosed. The invention firstly testifies the correlation on cells of TRPC ion channel and tumor cells multiplication, which offers a new path to suppress tumor cells multiplication by suppressing TRPC ion channel.

Description

technical field [0001] The present invention belongs to the field of cell biology and relates to a cell ion channel. More specifically, the present invention relates to the application of TRPC ion channel in the screening of anti-tumor drugs and the use of TRPC antagonists in the preparation of drugs for treating tumors. Background technique [0002] Intracellular calcium homeostasis is crucial to the normal physiological activities of cells. The entry of extracellular calcium ions into the cell and the increase of intracellular calcium ion concentration will promote cell proliferation and affect the cell cycle [Kahl CR, Means AR.Endocr Rev.2003 Dec ;24(6):719-36.]. [0003] TRP (transient receptor potential, transient receptor potential channel) ion channel is a large family of ion channels discovered recently. Montell et al. divided this family into three categories according to the sequence homology of each member of the TRP ion channel family: TRPC, TRPM and TRPV [Monte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12Q1/04A61K31/4164A61P35/00
CPCG01N33/6872A61K31/4174G01N2500/00A61P35/00
Inventor 王以政贾怡昌
Owner SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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