BACTERIAL DNA POLYMERASES: TARGETS FOR NOVEL ANTIBIOTIC
细菌 DNA 聚合酶:新型抗生素的靶标
基本信息
- 批准号:6337296
- 负责人:
- 金额:$ 22.43万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2001
- 资助国家:美国
- 起止时间:2001-09-30 至 2002-03-31
- 项目状态:已结题
- 来源:
- 关键词:
项目摘要
DESCRIPTION (Applicant's abstract): The objective of this project is to
identify novel drugs to treat antibiotic-resistant Gr+ and Gr- bacterial
infections. The work will utilize an unexploited target, the class III
bacterial DNA polymerase (pol III). The bacterial pol IIIs are highly conserved
enzymes that are required for the synthesis of DNA during chromosomal
replication. When an inhibitor of pol III is applied to a growing bacterium, it
stops replication, and, thus, like the replication-specific quinolone
antibiotics, it is bactericidal. Furthermore, the pol III-selective inhibitors
are equally effective against clinically relevant antibiotic-resistant and
antibiotic-sensitive pathogens. Therefore, they provide an excellent basis for
developing novel agents, which are effective in the treatment of
antibiotic-resistant infections.
The research plan for the phase I studies proposes to identify novel inhibitors
via moderate throughput screening of diverse chemical libraries against three
pol IIIs (the Gr- pol III E, and the Gr+ E and C types). The goal of this
screening will be to identify one or more novel chemical scaffolds that can be
suitably modified for development as new bactericidal drug candidates.
Health relatedness: The project exploits a novel target to identify new
bactericidal compounds to confront the growing crisis in the therapy of
infections caused by antibiotic-resistant bacterial pathogens.
PROPOSED COMMERCIAL APPLICATION:
Microbiotix will identify bactericidal inhibitors of Gr+ and Gr- pathogens with strong potential for development as broad-spectrum antimicrobials effective in the treatment of problematic antibioticresistant infections. The SBIR phase I study proposes to identify distinct pharmacophores selective for one or more of the three Gr+ and Gr- specific pol Ms. In phase II Microbiotix will chemically modify and further develop these pol III-specific pharmacophores into bona fide drug candidates
描述(申请人摘要):本项目的目标是
寻找治疗耐药Gr+和Gr-细菌的新药
感染。这部作品将利用一个未被开发的目标,即III类
细菌DNA聚合酶(PolIII)。细菌聚合酶III高度保守
染色体过程中合成DNA所需的酶
复制。当一种POL III的抑制剂被应用于正在生长的细菌时,它
停止复制,因此,就像复制特异性的喹诺酮一样
抗生素,它是杀菌的。此外,PolIII选择性抑制剂
对临床相关的抗生素耐药和
抗生素敏感的病原体。因此,它们提供了一个很好的基础
开发新的药物,这些药物在治疗癌症方面很有效
抗生素耐药感染。
第一阶段研究的研究计划建议寻找新的抑制剂。
通过对不同的化学文库进行中等吞吐量的筛选
POL III(Gr-POL III E、Gr+E和C型)。这样做的目的是
筛选将确定一个或多个新的化学支架,可以
经适当修改后可作为新的杀菌药物候选药物。
与健康相关:该项目利用一个新的目标来确定新的
杀菌化合物将面临日益严重的危机
由抗药性细菌病原体引起的感染。
建议的商业应用:
MicroBiotix将确定Gr+和Gr-病原体的杀菌抑制剂,作为有效治疗有问题的耐药性感染的广谱抗菌剂具有很大的开发潜力。SBIR第一阶段研究建议确定对三个Gr+和Gr特定的Pol MS中的一个或多个具有选择性的不同药效团。在第二阶段,MicroBiotix将对这些Pol III特定的药效团进行化学修饰,并将其进一步发展为真正的候选药物
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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Michelle M. Butler其他文献
Midwifery education in Canada
- DOI:
10.1016/j.midw.2015.11.019 - 发表时间:
2016-02-01 - 期刊:
- 影响因子:
- 作者:
Michelle M. Butler;Eileen K. Hutton;Patricia S. McNiven - 通讯作者:
Patricia S. McNiven
Michelle M. Butler的其他文献
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{{ truncateString('Michelle M. Butler', 18)}}的其他基金
Oxadiazole Inhibitors of Non-Stop Ribosome Rescue to treat MDR Neisseria gonorrhoeae
不间断核糖体救援恶二唑抑制剂治疗耐多药淋病奈瑟菌
- 批准号:
10231210 - 财政年份:2017
- 资助金额:
$ 22.43万 - 项目类别:
Aminospectinomycin antibacterials for the treatment of antibiotic-resistant gonorrhea and other bacterial STDs
氨基大观霉素抗菌药用于治疗抗生素耐药性淋病和其他细菌性 STD
- 批准号:
9252872 - 财政年份:2017
- 资助金额:
$ 22.43万 - 项目类别:
Novel Spectinamide Antibiotics for the Treatment of MDR/XDR Tuberculosis
用于治疗 MDR/XDR 结核病的新型 Spectinamide 抗生素
- 批准号:
8436177 - 财政年份:2012
- 资助金额:
$ 22.43万 - 项目类别:
Novel spectinamide antibiotics for the treatment of MDR/XDR tuberculosis
用于治疗 MDR/XDR 结核病的新型大观酰胺抗生素
- 批准号:
8857368 - 财政年份:2012
- 资助金额:
$ 22.43万 - 项目类别:
Novel spectinamide antibiotics for the treatment of MDR/XDR tuberculosis
用于治疗 MDR/XDR 结核病的新型大观酰胺抗生素
- 批准号:
8714556 - 财政年份:2012
- 资助金额:
$ 22.43万 - 项目类别:
Novel Spectinamide Antibiotics for the Treatment of MDR/XDR Tuberculosis
用于治疗 MDR/XDR 结核病的新型 Spectinamide 抗生素
- 批准号:
10252947 - 财政年份:2012
- 资助金额:
$ 22.43万 - 项目类别:
Novel Plasmodial Surface Anion Channel Inhibitors as Antimalarial Drugs
作为抗疟药物的新型疟原虫表面阴离子通道抑制剂
- 批准号:
10062806 - 财政年份:2012
- 资助金额:
$ 22.43万 - 项目类别:
Novel Plasmodial Surface Anion Channel Inhibitors as Antimalarial Drugs
作为抗疟药物的新型疟原虫表面阴离子通道抑制剂
- 批准号:
8549102 - 财政年份:2012
- 资助金额:
$ 22.43万 - 项目类别:
Novel Plasmodial Surface Anion Channel Inhibitors as Antimalarial Drugs
作为抗疟药物的新型疟原虫表面阴离子通道抑制剂
- 批准号:
8832349 - 财政年份:2012
- 资助金额:
$ 22.43万 - 项目类别:
Novel Plasmodial Surface Anion Channel Inhibitors as Antimalarial Drugs
作为抗疟药物的新型疟原虫表面阴离子通道抑制剂
- 批准号:
8311901 - 财政年份:2012
- 资助金额:
$ 22.43万 - 项目类别:
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