Molecular Target Focused Discovery of Anticancer Drugs

描述：结构新颖且可能非常重要的发现 动物、植物和微生物来源的抗癌药物 合成和/或结构修饰将形成重点突出的 美国国家癌症研究所 (NCI) 的这项研究的目的。 将特别强调新的抗肿瘤药物 基于分子靶标生物测定或随后展示此类分离 有效的抗血管生成、微管蛋白和/或各种癌症相关激酶 （细胞周期蛋白依赖性、蛋白激酶 C、酪氨酸激酶和端粒酶）特性 以及异常强的抗肿瘤活性。额外强调 将进行必要的进一步研究，以推进不断扩大的 苔藓抑素 1、多拉司他汀以及我们发现的其他药物的临床试验 作为强效癌症抗血管生成药物考布他汀A-4磷酸酯。 积极的并行研究将重点关注隔离， 新的和潜在有用的特征和结构测定 来自经证实的海洋无脊椎动物活性提取物的抗癌药物（以及 脊椎动物）、海洋和陆地植物以及海洋和陆地植物 微生物。只有那些最有希望产生新物种的物种 将寻求具有潜在临床活性的药物。拟议的研究 将为DCTD/NCI筛选抗癌新药提供极大帮助 候选者并加速他们向临床试验的发展。总而言之， 拟议的研究将针对这一发现并且非常迅速 为 NCI 项目开发新的抗癌药物，旨在改善 人类癌症治疗。

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.