MECHANISM OF ACTION OF NUCLEOSIDE ANALOGS
核苷类似物的作用机制
基本信息
- 批准号:6563810
- 负责人:
- 金额:$ 22.84万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2002
- 资助国家:美国
- 起止时间:2002-02-01 至 2003-01-31
- 项目状态:已结题
- 来源:
- 关键词:DNA directed DNA polymerase antineoplastics biological transport cell growth regulation cell line chemical kinetics chemical structure function cysteine endopeptidases cytosine arabinoside cytotoxicity drug metabolism drug screening /evaluation enzyme induction /repression high performance liquid chromatography neoplasm /cancer pharmacology nucleic acid metabolism nucleoside analog phosphorylation prodrugs protein metabolism protein purification radiotracer ribonucleotide reductase
项目摘要
APPLICANT'S DESCRIPTION (provided by Applicant) The overall goal of the
program project is to design and synthesize new drugs for the treatment of
cancer. The goal of this "Mechanism of action of nucleoside analogs" is
to perform experiments to characterize the biochemical pharmacology of the new
compounds that will be synthesized in projects 2 and 4. The information that
will be gained about the mechanism of action of these compounds is vital to
the rational development of these compounds as anticancer agents. In
addition, this information will be provided to the organic chemists in
projects 2 and 4 during regular group meetings to be used in the rational
design of new agents. This project has 3 specific aims. In the first aim we
will evaluate all compounds for toxicity to CEM cells to identify active and
inactive agents. In the second aim we will perform biochemical experiments on
selected compounds to gain a preliminary understanding of their mechanism of
action. In the third aim, we will perform extensive studies on compounds that
warrant a more thorough evaluation. Studies are planned to characterize in
detail the mechanism of action of 2 agents that have demonstrated excellent in
vivo antitumor activity, 4'-thio-arabinofuranosylcytosine and
2-Cl-2'-F-2'-deoxy- arabinofuranosyladenine (Clofarabine). These studies
should lead to a comprehensive understanding of the mechanism of action of new
agents that will aid in their development by determining how these compounds
differ form existing anticancer drugs.
申请人的描述(由申请人提供)的总体目标
该项目的目的是设计和合成新的药物,用于治疗
癌 本“核苷类似物的作用机制”的目的是
进行实验,以表征新的生物化学药理学
将在项目2和4中合成的化合物。 的信息
将获得有关这些化合物的作用机制是至关重要的,
这些化合物作为抗癌剂的合理开发。 在
此外,这些信息将提供给有机化学家,
在定期小组会议期间,项目2和4将用于合理性分析
设计新的代理人。 该项目有三个具体目标。 在第一个目标中,
将评估所有化合物对CEM细胞的毒性,以鉴定活性和
不活跃的特工 在第二个目标中,我们将进行生物化学实验,
选择的化合物,以获得其机制的初步了解
行动上 在第三个目标中,我们将对化合物进行广泛的研究,
需要更彻底的评估 计划进行研究,以表征
详细介绍了2种药物的作用机制,这些药物在
体内抗肿瘤活性,4 '-硫代-阿拉伯呋喃糖基胞嘧啶和
2-Cl-2 '-F-2'-脱氧-阿拉伯呋喃糖基腺嘌呤(氯法拉滨)。 这些研究
应导致全面了解新的作用机制,
通过确定这些化合物
与现有的抗癌药物不同。
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
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WILLIAM B PARKER其他文献
WILLIAM B PARKER的其他文献
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{{ truncateString('WILLIAM B PARKER', 18)}}的其他基金
2013 Nucleosides, Nucleotides, and Oligonucleotides Gordon Research Conference
2013年核苷、核苷酸和寡核苷酸戈登研究会议
- 批准号:
8519771 - 财政年份:2013
- 资助金额:
$ 22.84万 - 项目类别:
2011 Nucleosides, Nucleotides, and Oligonucleotides GRC
2011 核苷、核苷酸和寡核苷酸 GRC
- 批准号:
8116777 - 财政年份:2011
- 资助金额:
$ 22.84万 - 项目类别:
Purine Analog Anti-Mycobacterial Drug Development
嘌呤类似物抗分枝杆菌药物开发
- 批准号:
7232669 - 财政年份:1999
- 资助金额:
$ 22.84万 - 项目类别:
PURINE ANALOG ANTIMYCOBACTERIAL DRUG DEVELOPMENT
嘌呤类似物抗真菌药物的开发
- 批准号:
2797353 - 财政年份:1999
- 资助金额:
$ 22.84万 - 项目类别:
BIOCHEMISTRY OF PURINE NUCLEOSIDE ANALOGS ACTIVATED BY E COLI PNP
大肠杆菌 PNP 激活的嘌呤核苷类似物的生物化学
- 批准号:
6203306 - 财政年份:1999
- 资助金额:
$ 22.84万 - 项目类别:
Purine Analog Anti-Mycobacterial Drug Development
嘌呤类似物抗分枝杆菌药物开发
- 批准号:
7609201 - 财政年份:1999
- 资助金额:
$ 22.84万 - 项目类别:
Purine Analog Anti-Mycobacterial Drug Development
嘌呤类似物抗分枝杆菌药物开发
- 批准号:
7012750 - 财政年份:1999
- 资助金额:
$ 22.84万 - 项目类别:
PURINE ANALOG ANTIMYCOBACTERIAL DRUG DEVELOPMENT
嘌呤类似物抗真菌药物的开发
- 批准号:
6341712 - 财政年份:1999
- 资助金额:
$ 22.84万 - 项目类别:
Purine Analog Anti-Mycobacterial Drug Development
嘌呤类似物抗分枝杆菌药物开发
- 批准号:
6947999 - 财政年份:1999
- 资助金额:
$ 22.84万 - 项目类别:
Purine Analog Anti-Mycobacterial Drug Development
嘌呤类似物抗分枝杆菌药物开发
- 批准号:
7410131 - 财政年份:1999
- 资助金额:
$ 22.84万 - 项目类别:
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