Molecular Target Focused Discovery of Anticancer Drugs

描述：结构新颖的发现，可能非常重要 来自动物、植物和微生物来源的抗癌药物 合成和/或结构修饰将形成尖锐的焦点 这项研究的目标是美国国家癌症研究所(NCI)。 还将特别强调新的抗肿瘤物质 基于分子靶标生物测定分离的或随后展示的 有效的抗血管生成、微管蛋白和/或各种与癌症相关的激酶 (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 以及极强的抗肿瘤活性。更多强调 将放在必要的进一步研究上，以推进 我们发现的Bryostatin 1、Dolastatins和其他药物的临床试验 作为一种强大的抗癌血管生成药物，康泰素A-4磷酸。 积极的平行研究将强烈集中在隔离上， 新的和潜在有用的表征和结构确定 来自确认的海洋无脊椎动物活性提取物的抗癌药物(和 脊椎动物)，海洋和陆地植物，以及海洋和陆地植物 微生物。只有那些给出最大希望产生新的 将寻求具有潜在临床活性的药物。拟议的研究 将为DCTD/NCI选择抗癌新药提供极大的帮助 并加快其向临床试验的发展。总而言之， 拟议的研究将尖锐地针对这一发现，并非常迅速 为NCI计划开发新的抗癌药物旨在提高 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.