NOVEL ENZYMATIC APPROACH TO SEMI-SYNTHESIS OF TAXOL

描述（改编自申请人的摘要）： 这个项目是为了确定开发一种新的 紫杉醇的酶促半合成方法。 紫杉醇是一种很有前途的药物 用于治疗卵巢癌和其他癌症。 但目前 只有从稀有树木中提取的有限数量才能获得; 化学合成是困难和不切实际的。 本有限 但是，由于药物的可获得性， 对抗多种癌症。 在第一阶段，研究人员 将研究使用酶通过偶联紫杉醇生产紫杉醇， 紫杉醇前体的侧链，其可容易地从 观赏灌木 该偶联或酰化步骤是最重要的步骤。 这是从紫杉醇前体半合成紫杉醇的困难步骤。 如果 第一阶段的结果是有希望的，那么第二阶段的努力将针对 将这一步骤纳入紫杉醇的合成方案，以及 在半合成的其他关键步骤中开发酶促方法 紫杉醇。 该计划可能导致商业上经济的生产 使其他癌症的临床研究得以进行 同时提供足够的量用于治疗癌症 患者

DESCRIPTION (Adapted from the Applicant's Abstract): The objective of this project is to determine the feasibility of developing a novel enzymatic process for semi-synthesis of taxol. Taxol is a promising drug for treatment of ovarian and other cancers. However, it is currently available only in limited quantity by extraction from a rare tree; chemical synthesis is difficult and impractical. This limited availability has prevented wide-scale clinical testing for efficacy against many types of cancer. In this Phase I program,the investigators will investigate the use of enzymes to produce taxol by coupling the taxol side-chain to a taxol precursor, which is readily obtainable from ornamental shrubs. This coupling, or acylation, step is the most difficult step in the semi-synthesis of taxol from its precursor. If the results of Phase I are promising, then efforts in Phase II will be aimed at incorporating this step into synthesis schemes for taxol, as well as developing enzymatic approaches to other key steps in the semi-synthesis of taxol. This program could lead to commercially economical production of taxol, enabling clinical studies for other cancers to be undertaken with taxol while providing sufficient quantities for treatment of cancer patients.