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Probe Development for Bromodomains Networks

Bromodomains 网络的探针开发

基本信息

批准号：
8903609
负责人：
HAICHING MA
金额：
$ 29.04万
依托单位：
REACTION BIOLOGY CORPORATION
依托单位国家：
美国
项目类别：
财政年份：
2015
资助国家：
美国
起止时间：
2015-05-01 至 2016-10-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8903609
关键词：
Affect Area Binding Sites Biological Assay Biological Availability Biological Factors Biology Bromodomain Categories Cell physiology Cells Chemicals Chromatin Clinical Clinical Trials Collection Databases Development Drug Compounding Drug Targeting Drug usage Epigenetic Process FDA approved Family Fluorescent Dyes Funding Gene Expression Goals Grant Health Histones Human Industry Inflammation Inhibitory Concentration 50 Knowledge Label Laboratories Length Lysine Malignant Neoplasms Methods Methyltransferase Modification Peptides Pharmaceutical Preparations Phase Phosphotransferases Preclinical Drug Evaluation Process Production Property Protein Family Proteins Reaction Reader Reagent Research Resources Services Small Business Innovation Research Grant Source Staging Tertiary Protein Structure Testing Therapeutic Therapeutic Agents Toxic effect United States National Institutes of Health Validation Work assay development base case-by-case basis chromatin modification commercialization cost drug discovery epigenetic regulation experience histone methyltransferase human disease improved inhibitor/antagonist interest new technology phase 2 study product development public health relevance screening small molecule small molecule libraries success tool

项目摘要

DESCRIPTION (provided by applicant): Epigenetic regulation of gene expression is a highly dynamic and reversible process essential to normal cellular function. However, it also contributes to human diseases, such as cancer and inflammation. Protein families that participate in epigenetic regulation include writers, which covalently modify chromatin; readers, which recognize chromatin modifications; and erasers, which remove modifications. A large volume of research in the field over the past decade has shown that many epigenetic proteins are potential druggable targets. Bromodomains, which belong to the reader's category, recognize acetylated lysine residues on histones and other proteins. Several potent, selective and cellularly active bromodomain compounds have recently been identified, increasing appreciation of the functional importance and therapeutic potential of this family. However, studies are limited and focus only on a few bromodomain subfamilies, such as the bromodomain and extraterminal (BET) proteins. There are a number of reasons that the studies have not expanded into more reader proteins; the key limitations are in both the availabilities of products and the body of knowledge for these non-BET subfamily targets. As part of the proposed project, we will systematically develop 1) complete, high-quality bromodomain proteins, 2) substrate knowledge for each target, 3) multiple assay formats for each target, 4) probe(s) for each target, 5) easy-to-use assay kits, 6) assay services for newly produced reader domains, and importantly, 7) the first drug-bromodomain interaction database, which we will build by testing each bromodomain against a large number of FDA-approved drugs and agents in clinical trials, to provide information on how these commonly used drugs and chemicals affect epigenetic activities relevant to human health.