A screening method for identifying new drugs

A screening method and drug technology, applied in the field of screening for identifying new drugs, can solve problems such as poor bioavailability, lack of inhibitory activity, and poor specificity

Inactive Publication Date: 2009-07-08
INSTITUCIO CATALANA DE RECERCA I ESTUDIS AVANCATS +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Pseudomonic acid is approximately 8000-fold more selective for pathogens than mammalian IleRS, but the lack of systemic bioavailability of the drug limits its use for topical administration
[0008] Although there are other known natural product inhibitors against synthetases (e.g., borrelidin, furamycin, duricin, etc.), due to lack of inhibitory activity, poor specificity, or poor bioavailability, these None developed into commercial antibiotics

Method used

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  • A screening method for identifying new drugs
  • A screening method for identifying new drugs
  • A screening method for identifying new drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0058] Example: Expression of Helicobacter pylori glutamyl-tRNA synthetase in HeLa cells

[0059] import :

[0060] The pathogen H. pylori utilizes two essential glutamyl-tRNA synthetases (GluRS1 and GluRS2). GluRS1 is a typical recognition GluRS (discriminating GluRS), and GluRS2 is atypical because it only corrects misacylated Glu-tRNA Gln It is necessary for the production.

[0061] To investigate whether expression of H. pylori atypical GRS2 in mammalian systems has toxic effects and leads to cell death, H. pylori GFPGRS2 was expressed in HeLa cells, human cell lines and their putative toxic effects were examined.

[0062] get expression vector

[0063] The plasmid vector GRS2#1 (SEQ ID NO: 1)

[0064] 5'-GTCACCACCATGCTTCGTTTTGCGCCTTCGCCTACAG

[0065] and GRS2#2 (SEQ ID NO: 2)

[0066] 5'-GACTCAATGGTGATGGTGATGATGTGCTTTGAGCCTTAAAACTT

[0067] It is used to amplify GRS2 from genomic DNA from Helicobacter pylori (ATCC 700392D), and add kozak consensus ribosome bind...

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Abstract

A screening method for identifying new drugs A screening method for identifying a candidate to drug wherein said method comprises the following steps: a) obtaining an expression vector which comprises a gene sequence codifying a naturally occurring pathogenic non- discriminating tRNA synthetase; b) transforming isolated mammalian cells with the expression vector; c) growing the recombinant cells resulting from (b) in a nutrient medium under conditions which allow the expression of the pathogenic tRNA synthetase, resulting the expression of the pathogenic tRNA synthetase into cell death or a decrease in the rate of cell division; d) providing a substance to be tested; and e) analyzing the resulting cell growth, wherein if there is an increase in cell growth, then the substance selectively inhibits the activity of the pathogenic tRNA synthetase and does not affect to its cellular ortholog, resulting that said substance is a candidate to drug.

Description

[0001] The present invention relates to new screening methods that allow the identification of new drugs. In particular, the present invention relates to screening methods for the selection of aminoacyl-tRNA synthetase (ARS) inhibitor compounds capable of being used, inter alia, as antibacterial agents and antifungal agents. Background technique [0002] In modern drug discovery programs, chemical libraries are used in combination with robotic systems to rapidly evaluate the effect of large numbers of compounds on a given reaction. This approach has two major disadvantages. First, it is often necessary to develop easily monitored biochemical assays to identify candidate compounds. This method is expensive and insensitive due to potential adverse effects of the selected drugs. Second, this method ignores bioavailability and toxicity parameters. Most initially selected compounds were later abandoned due to solubility, bioavailability or toxicity issues. [0003] Aminoacyl-t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12Q1/68G01N33/50
CPCG01N2333/9015G01N33/5008C12Q1/527C12Q1/18C12Q1/02G01N33/15C12N15/52C12N15/63
Inventor L·里瓦斯德普布拉纳T·博里桑
Owner INSTITUCIO CATALANA DE RECERCA I ESTUDIS AVANCATS
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