Molecular Target Focused Discovery of Anticancer Drugs

抗癌药物的分子靶点聚焦发现

• 批准号: 6858674
• 负责人: GEORGE R PETTIT
• 金额: $ 78.01万
• 依托单位: ARIZONA STATE UNIVERSITY-TEMPE CAMPUS
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-04-01 至 2006-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6858674
• 关键词: angiogenesis inhibitors; animal extract; antineoplastics; bryostatin; chemical synthesis; drug design /synthesis /production; enzyme inhibitors; marine toxins; microorganism toxin; plant extracts

DESCRIPTION: Discovery of structurally novel and potentially very important anticancer drugs from animal, plant and microorganism sources followed by their synthesis and/or structural modification will form the sharply focused objective of this research for the U.S. National Cancer Institute (NCI) . Special emphasis will be placed on new antineoplastic substances either isolated based on molecular target bioassays or subsequently displaying such potent antiangiogenesis, tubulin and/or various cancer-implicated kinase (cyclin-dependent, protein kinase C, tyrosine kinase and telomerase) properties as well as exceptionally strong antineoplastic activity. Additional emphasis will be placed on further research necessary to advancing the expanding clinical trials of bryostatin 1, the dolastatins, and others we discovered such as the powerful cancer antiangiogenesis drug combretastatin A-4 phosphate. vigorous parallel research will be strongly focused on the isolation, characterization, and structural determination of new and potentially useful anticancer drugs from confirmed active extracts of marine invertebrates (and vertebrates) , marine and terrestrial plants, and marine as well as terrestrial microorganisms. Only those species that give maximum promise of yielding new drugs with potential clinical activity will be pursued. The proposed research will provide great assistance to the DCTD/NCI in selecting new anticancer drug candidates and speeding their development toward clinical trial. In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs directed at improving human cancer treatments.

描述：发现结构新颖的，潜在的非常重要的 来自动物，植物和微生物来源的抗癌药，然后 合成和/或结构修饰将形成浓缩的 这项研究的目的是美国国家癌症研究所（NCI）。 特别重点将放在新的抗肿瘤物质上 基于分子靶向生物测定或随后显示这种孤立 有效的抗血管生成，微管蛋白和/或各种癌症的激酶 （依赖细胞周期蛋白，蛋白激酶C，酪氨酸激酶和端粒酶）特性 以及异常强大的抗塑性活性。其他重点 将进行进一步的研究，以推进扩展 Bryostatin 1，Dolastatins和其他的临床试验我们发现了这样 作为强大的癌症抗血管生成药物combretastatin A-4磷酸盐。 有力的平行研究将重点关注隔离， 表征和结构性确定新的和潜在的有用 来自抗癌药物的抗癌药物的抗癌药物提取物（和 脊椎动物），海洋和陆地植物以及海洋以及陆地 微生物。只有那些最大的希望产生新的物种 将寻求具有潜在临床活性的药物。拟议的研究 将为DCTD/NCI选择新的抗癌药物提供极大的帮助 候选人并加快了他们进入临床试验的发展。总之， 拟议的研究将针对发现，并且非常迅速 为NCI计划开发新的抗癌药物，旨在改善 人类癌症治疗。