Conference on Tissue-Selective Nuclear Receptors

描述(由申请人提供)： 核激素受体引起了人们极大的研究兴趣。2005年组织选择性核受体的Keystone会议将是独一无二的。它将把通过核受体影响人类健康的三个研究小组聚集在一起：(A)基础科学家，(B)药物研发人员和(C)临床医生。会议将确定组织选择性NR药物尚未得到满足的医疗需求，组织选择性作为提高疗效和安全性标志的分子理解的最新进展，以及满足和满足对新兴新型研究工具的需求的资源研讨会。许多新的NR药物正在进入治疗糖尿病和肥胖症、甲状腺功能障碍和充血性心力衰竭的市场，但很少有药物表现出适度的组织选择性。目前对组织选择性的机制还知之甚少。共激活蛋白和共抑制蛋白被认为起到了作用，但人们对特定组织中存在复杂的基因表达时间模式知之甚少。另一方面，制药科学已经创造了数以千计的小分子核受体活性调节剂。这些化合物可以是很好的研究工具，也可以被“抛弃”。我们建议将来自广泛科学领域的研究人员聚集在一起，在组织水平上展示对核受体功能的最先进的理解。指导思想将是对未来受体药物的治疗需求的概述，评估当前药物实现这些特征的程度，然后提出可以促进对受体-配体功能的机制理解的科学方法。会议将集中在我们对一类转录因子的理解上，这些转录因子的药理作用涉及一些最常见的人类疾病

DESCRIPTION (provided by applicant): The nuclear hormone receptors engender great research interest. The Keystone Meeting on Tissue Selective Nuclear Receptors in 2005 will be unique. It will bring together three research groups impacting human health via the nuclear receptors (NR's): (a) basic scientists, (b) pharmaceutical drug discoverers and (c) clinicians. The meeting will define unmet medical needs for tissue-selective NR drugs, recent advances towards a molecular understanding of tissue-selectivity as a hallmark for improved efficacy and safety, and resources workshops to address and fulfill needs for emerging novel research tools. Many new NR drugs are entering the market for diabetes and obesity, thyroid dysfunction, and congestive heart failure but few display even modest tissue selectivity. There is only scant understanding of the mechanisms of tissue selectivity. Co-activator and co-repressor proteins are thought to contribute, but little is known about how complex temporal patterns of gene expression exist in particular tissues. Pharmaceutical science, on the other hand, has created literally thousands of small molecule modulators of nuclear receptor activity. These compounds can be excellent investigative tools, and can be "abandoned" compounds. We propose to bring together researchers from a broad spectrum of science to present a state-of-the-art understanding of nuclear receptor function at the tissue level. The guiding concept will be to present an overview of therapeutic needs for future receptor drugs, assess the degree to which current drugs achieve these profiles, and then present scientific methodology that can advance mechanistic understanding of receptor-ligand function. The meeting will center upon our understanding of a class of transcription factors whose pharmacology touches some of the most prevalent human diseases