Title：Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation

标题：选择性靶向溴结构域-PHD指家族的溴结构域可损害破骨细胞分化

Introduction

The paper 'Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation' by Julia C. Meier et al., published in ACS Chemical Biology (2017), explores the potential of selective inhibitors targeting bromodomains in the Bromodomain-PHD Fingers (BRPF) family to disrupt osteoclast differentiation. This process plays a crucial role in bone metabolism, and its regulation may provide therapeutic benefits for diseases like osteoporosis.

研究简介

题目：选择性靶向溴结构域-PHD手指家族的溴结构域抑制破骨细胞分化
发表期刊：ACS Chemical Biology
发表时间：2017年10月20日
作者：Julia C. Meier 等

这篇文章研究了通过选择性抑制溴结构域-PHD手指（BRPF）家族中的溴结构域来抑制破骨细胞分化的潜力。破骨细胞分化在骨代谢中起重要作用，其调控可能为骨质疏松等疾病提供治疗途径。

Key Findings

1. BRPF Bromodomains as a Target: Bromodomains recognize acetylated lysine residues on histones, influencing gene regulation. By targeting BRPF bromodomains, the study aimed to interfere with osteoclast differentiation, crucial for bone resorption.
2. Discovery of Inhibitors: The researchers identified three selective inhibitors that impaired osteoclast formation without affecting cell viability, indicating potential therapeutic applications.
3. Mechanistic Insights: The inhibitors affected gene expression related to osteoclast differentiation, providing further insight into the pathways influenced by BRPF bromodomains.
4. Therapeutic Application: The findings suggest these inhibitors could be developed for treating bone-related diseases like osteoporosis.

主要发现

1. BRPF溴结构域作为靶点：溴结构域识别组蛋白上乙酰化的赖氨酸残基，从而影响基因调控。通过靶向BRPF溴结构域，研究旨在干扰破骨细胞分化，这在骨吸收中至关重要。
2. 抑制剂的发现：研究者发现了三种选择性抑制剂，它们能在不影响细胞活力的情况下抑制破骨细胞的形成，表明其在治疗方面的潜力。
3. 机制见解：抑制剂影响与破骨细胞分化相关的基因表达，进一步阐明了BRPF溴结构域影响的通路。
4. 治疗应用：研究表明，这些抑制剂可能被开发用于治疗骨质疏松等骨相关疾病。

Related Compounds and CAS Numbers

Here are a few related compounds often studied in similar research contexts:
1. I-BET151 – CAS: 1314890-29-3
2. JQ1 – CAS: 1268524-70-4