miRNA modulators of thermogenesis

A technology of has-mir-22 and hsa-mir-99a, which is applied in the field of thermogenic miRNA regulators, can solve the problems of long-term treatment of obesity, unsatisfactory short-term efficacy and safety performance, and changes in patients' lifestyles.

Pending Publication Date: 2017-08-22
APTAMIR THERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Existing symptomatic medical treatments for obesity fail to achieve long-term therapeutic goals, largely due to limited drug efficacy and poor patient adherence to lifestyle changes and treatments
Several obesity drugs have been taken off the market due to safety concerns, while some small molecules in development are struggling to gain approval due to suboptimal short-term efficacy and unknown safety profiles

Method used

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  • miRNA modulators of thermogenesis
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0218] Example 1. Computer Analysis of Thermogenic Regulators

[0219] Eighty-three proteins involved in the regulation of thermogenesis were selected based on a critical evaluation and review of available scientific information and our own experimental data. Based on their function, these proteins are classified as thermogenic activators or repressors. These thermoregulatory proteins are described in Table 2.

[0220] Table 2.

[0221] Thermoregulatory proteins:

[0222]

[0223]

[0224]

[0225] These 83 candidate molecules were tested using the known STRING 9.0 database and predicted protein interactions (string-db.org / ). The interactions include direct (physical) and indirect (functional) associations; they arise from four sources: genomic context; high-throughput experiments; co-expression; and prior knowledge. STRING quantitatively integrates interaction data in a large number of organisms from these sources, transferring information between these organisms...

Embodiment 2

[0228] Example 2. In silico selection of relevant miRNA targets

[0229] In order to select thermogenic regulators suitable as targets for miRNA reagents, several Internet-based resources were employed to match miRNAs to their targets ("micronome"). Exemplary tools are described in Table 3.

[0230] table 3.

[0231] Exemplary bioinformatics tools for selecting miRNAs and their targets:

[0232]

[0233]

[0234]

[0235]

[0236]

[0237] Specifically, these tools were used to perform: 1) integrated data mining (8 tools); 2) miRNA mining and mapping (6 tools); 3) miRNA-targeted targets and expression (21 tools); 4 ) integrated miRNA targets and expression (13 tools) 5) prediction and comparison of miRNA secondary structures (5 tools); 6) web search and analysis (8 tools); 7) molecular display (4 tools) ; and 8) information integration and development (1 tool).

[0238] A single gene target can be controlled by several miRNAs, whereas a single miRNA can cont...

Embodiment 3

[0373] Example 3. High content cell phenotype screening

[0374] A high-content screening approach was used to screen for novel miRNA agents that modulate the activity of thermogenic regulators such as UCP1 and UCP2. High-content screening is a drug discovery method that uses live-cell images to aid in molecular discovery. Such automated imaging-based screening methods are particularly useful for identifying agents that alter the phenotype of cells.

[0375] WAT cells contain large lipid droplets, whereas BAT cells, in contrast, contain many smaller droplets and a higher number of mitochondria, which contain iron and give it a brown color. The high number of mitochondria in BAT leads to increased oxygen consumption compared with WAT. Thus, BAT cells can be visually distinguished from WAT cells based on their cellular phenotype.

[0376] Therefore, a high-content screening approach was used to screen for novel miRNAs that modulate the activity of thermogenic regulators. Spe...

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Abstract

Provided are novel methods and compositions for the modulation of thermogenesis. Such methods are particularly advantageous in that they allow for the reduction of body fat in a subject without the subject having to adjust their caloric intake through dieting, modify their physical activity or undergo bariatric surgery. Accordingly, the methods of the invention are particularly useful for treating or preventing obesity. Also provided are methods of screening for novel agents that modulate the activity of thermogenic regulators.

Description

[0001] This application is a divisional application of a Chinese patent application with application number 201380030602.5, and the original application is a Chinese national phase application of the international application PCT / US2013 / 037579. [0002] Cross References to Related Applications [0003] This application claims priority to: U.S. Application Serial No. 61 / 636,059, filed April 20, 2012; U.S. Application Serial No. 61 / 681,750, filed August 10, 2012; and US Application Serial No. 61 / 782,838 filed on the 14th, each of which is hereby incorporated by reference. technical field [0004] The present application relates to novel methods of treating obesity and, in particular, to thermogenic miRNA modulators. Background technique [0005] Obesity has reached epidemic proportions, affecting all age groups and socioeconomic groups. The World Health Organization estimates that in 2008, 1.5 billion adults aged 20 and over were overweight, and more than 200 million men a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N15/113A61K31/7105A61K48/00A61P3/04
CPCA61K31/7105C12N15/113C12N2320/30C12N2310/113C12N2310/141C12N2310/16A61P3/04A61P43/00
Inventor 马克·蒂博尼耶
Owner APTAMIR THERAPEUTICS
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