Split-luciferase Epigenetic Assays for Drug Discovery

用于药物发现的分裂荧光素酶表观遗传学分析

基本信息

  • 批准号:
    10482555
  • 负责人:
  • 金额:
    $ 24.04万
  • 依托单位:
  • 依托单位国家:
    美国
  • 项目类别:
  • 财政年份:
    2022
  • 资助国家:
    美国
  • 起止时间:
    2022-04-01 至 2024-03-31
  • 项目状态:
    已结题

项目摘要

Project Summary Epigenetic control is essential for maintaining transcriptional integrity. Regulation of the dynamic epigenome is mediated through a range of post translational modifications on DNA and histone tails. Histone modifications are mediated by enzymes which can be broadly classified into “writers” that catalyze the addition of chemical modifications, “erasers” that remove the modifications, and “readers” that can recognize chemical modifications through specific protein domains. The writing and erasing of histone marks by enzymes is a dynamic process, and when dysregulated is associated with cancer, inflammatory and neurological diseases. In this application we focus on the two classes of histone modifying enzymes, lysine methyl transferases (KMTs) and lysine demethylases (KDMs), and aim to develop and validate cell- based assays targeting both KMTs and KDMs. These assays, based on a three-hybrid split luciferase system, are reversible allowing dose dependent quantification of inhibitor binding. These efforts are both significant and innovative as they can report on the direct binding of a drug to the target protein at its intended site of action, thereby facilitating the generation of lead therapeutic candidates and identification of chemical probes for studying histone biology and pathways.
项目总结

项目成果

期刊论文数量(0)
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专利数量(0)

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REENA ZUTSHI其他文献

REENA ZUTSHI的其他文献

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{{ truncateString('REENA ZUTSHI', 18)}}的其他基金

Enabling Toxoplasma gondii Kinome Directed Drug Discovery
实现弓形虫激酶组定向药物发现
  • 批准号:
    10602259
  • 财政年份:
    2019
  • 资助金额:
    $ 24.04万
  • 项目类别:
Kinase Targeted Antimalarial Agents
激酶靶向抗疟药
  • 批准号:
    9918203
  • 财政年份:
    2019
  • 资助金额:
    $ 24.04万
  • 项目类别:
Tools for Accelerating R&D for Historically Understudied Protein Kinases
加速 R 的工具
  • 批准号:
    9264156
  • 财政年份:
    2017
  • 资助金额:
    $ 24.04万
  • 项目类别:
Enabling Malarial Kinome Directed Drug Discovery
实现疟疾激酶组定向药物发现
  • 批准号:
    8714538
  • 财政年份:
    2014
  • 资助金额:
    $ 24.04万
  • 项目类别:
Kinome-wide Cell-Based Assays
全激酶组细胞检测
  • 批准号:
    9205516
  • 财政年份:
    2014
  • 资助金额:
    $ 24.04万
  • 项目类别:
Kinome-wide cell-based assays
全激酶组细胞分析
  • 批准号:
    8780886
  • 财政年份:
    2014
  • 资助金额:
    $ 24.04万
  • 项目类别:
Kinome-wide Cell-Based Assays
全激酶组细胞检测
  • 批准号:
    9053369
  • 财政年份:
    2014
  • 资助金额:
    $ 24.04万
  • 项目类别:
A Poly(ADP-Ribose) Detection Assay Enabling Drug Discovery and Development
聚 (ADP-核糖) 检测分析促进药物发现和开发
  • 批准号:
    8123053
  • 财政年份:
    2011
  • 资助金额:
    $ 24.04万
  • 项目类别:
Rapid Kinase Profiling with Luminescent Reporters
使用发光报告基因快速分析激酶
  • 批准号:
    8005176
  • 财政年份:
    2010
  • 资助金额:
    $ 24.04万
  • 项目类别:
Rapid Kinase Profiling with Luminescent Reporters
使用发光报告基因快速分析激酶
  • 批准号:
    7745380
  • 财政年份:
    2009
  • 资助金额:
    $ 24.04万
  • 项目类别:

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