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STRUCTURAL BIOLOGY & TARGETED DRUG DESIGN FOR AIDS

STRUCTURAL BIOLOGY & TARGETED DRUG DESIGN FOR AIDS
结构生物学
批准号:
6120227
负责人:
Charles Scott Craik
金额:
$1.33万
依托单位国家:
美国
项目类别:
财政年份:
1999
资助国家:
美国
项目状态:
已结题
起止时间:
1999-03-01 至 2000-02-29

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项目成果

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中文摘要
翻译
我们这个项目的目标是设计,合成和测试新的 特异性靶向HIV-1的抗病毒化疗剂 逆转录酶和HIV-1核糖核酸酶H和HIV蛋白酶, 是HIV-1生命周期的关键酶。 我们已经设计并 合成了各种各样的化合物,包括: 核苷酸和脱氧核苷酸类似物抑制剂,焦磷酸类似物 抑制剂,杂芳族抑制剂,非天然氨基酸, 肽类和拟肽抑制剂。 质谱仪 与~ 1H NMR、~(13)C NMR、~(19)F NMR的关联起重要作用 和~(31)P NMR对这些不同化学结构的先导化合物进行了表征 性质和背景。 质谱分析仍将是 我们在分析下一代抑制剂方面的研究成果。
英文摘要
Our goal for this project is to design, synthesize and test novel antiviral chemotherapeutic agents, specifically targeted against HIV-1 reverse transcriptase and HIV-1 ribonuclease H and HIV protease, which are vital enzymes to the life cycle of HIV-1. We have designed and synthesized a wide variety of chemical compounds which include: nucleotide and deoxynucleotide analog inhibitors, pyrophosphate analog inhibitors, heteroaromatic inhibitors, unnatural amino acids, peptide-based and petidomimetic inhibitors. Mass spectrometry has played an important role in association with 1H NMR, 13C NMR, 19F NMR and 31P NMR in characterizing these lead compounds of diverse chemical nature and background. Mass spectrometry will remain an integral part of our research in analyzing the next generation of inhibitors.
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Developing Antivirals Targeting Proteases and Polymerases of Coronaviruses, Picornaviruses and Bunyavirales
New radiotracer development to study immune cell mobilization of granzyme proteolytic activity
New radiotracer development to study immune cell mobilization of granzyme proteolytic activity
New radiotracer development to study immune cell mobilization of granzyme proteolytic activity
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