HIV-1 PG120 V3 LOOP TARGETING--NOVEL POTENTIAL INHIBITOR

HIV-1 PG120 V3 环靶向——新型潜在抑制剂

• 批准号: 2751045
• 负责人: A ROBERT ROBERT NEURATH
• 金额: $ 2万
• 依托单位: NEW YORK BLOOD CENTER
• 依托单位国家: 美国
• 财政年份: 1996
• 资助国家: 美国
• 起止时间: 1996-08-01 至 1999-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2751045
• 关键词: HIV envelope protein gp120; antiAIDS agent; chemical conjugate; drug design /synthesis /production; human immunodeficiency virus 1; oligonucleotides; porphyrins

DESCRIPTION: The parent grant (CA43315-09) deals with the synthesis of antiviral compounds targeted to the V3 loop, the definition of their structure-function relationships, assessment of their antiviral activity against primary HIV-1 isolates, and the design of compounds with reactive groups leading to irreversible binding to gp120/41. The proposed FIRCA aims are the synthesis of (a) new porphyrin derivatives, (b) phosphorothioate cytosine oligonucleotides with various pentofuranosyl configurations and phosphonate cytosine oligonucleotides with hydrophobic functional groups inserted in the vicinity of the phosphonate moieties, and (c) conjugates of the porphyrin derivatives and oligonucleotides. The in vitro testing of the synthesized molecules for anti-HIV effect and their binding to gp120 and the V3 loop will be done as part of the parent grant. The foreign collaborator (principal investigator) is Dr. Ivan Rosenberg of the Institute of Organic Chemistry and Biochemistry in Prague, assisted by Drs. Tocik, Liboska and Endova.

描述：母基金（CA 43315 -09）涉及以下化合物的合成： 靶向V3环的抗病毒化合物，它们的定义 结构-功能关系，评估其抗病毒活性 针对主要HIV-1分离株，并设计具有反应活性的化合物， 导致与GP 120/41不可逆结合的基团。拟议的FIRCA 目的是合成（a）新的卟啉衍生物，（B） 具有各种戊呋喃糖基的硫代磷酸胞嘧啶寡核苷酸 构型和膦酸胞嘧啶寡核苷酸， 疏水性官能团插入在所述膜的附近， 膦酸酯部分，和（c）卟啉衍生物的缀合物，和 寡核苷酸合成的分子的体外测试， 将进行抗HIV作用及其与gp 120和V3环的结合 作为家长补助的一部分外国合作者（主要） 研究员）是有机研究所的伊万·罗森伯格博士 化学和生物化学在布拉格，由博士协助。 恩多瓦

项目成果

Efficient synthesis of 2'-deoxynucleoside 3'-C-phosphonates: reactivity of geminal hydroxyphosphonate moiety.

2-脱氧核苷3-C-膦酸酯的有效合成：孪生羟基膦酸酯部分的反应性。

• DOI: 10.1080/15257770008035038
• 发表时间: 2000
• 期刊: Nucleosides, nucleotides & nucleic acids.
• 作者: Kralikova,S;Budyysinsky,M;Masojidkova,M;Rosenberg,I
• 通讯作者: Rosenberg,I