有機合成化学協会誌
Online ISSN : 1883-6526
Print ISSN : 0037-9980
ISSN-L : 0037-9980
エイズウイルスの複製に関わる転写因子を阻害する人工化合物の分子設計
藤田 美歌子大塚 雅巳
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1997 年 55 巻 8 号 p. 697-704

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HF-κB, HIV-EP1 Sp1, and TBP-E1A are transcriptional proteins involved in the long terminal repeat-directed expression of human immunodeficiency virus. Inhibitory effect of eighteen compounds against NF-κB, HIV-EP1, Sp1, and E1A was studied. The compounds could be classified into six types based on the inhibitory profile. Compounds of class A (ent-2, 11, 12, 13) and B (7, 9) are inhibitory against HIV-EP1. Class B compounds are more potent. Class C (14) compound is a Spl inhibitor. Compounds of D class (1, ent-1, 2) and E (5, 6, 8, 10) are inhibitors of both HIV-EP1 and Sp1. Class E compounds are more potent. NF-κB, HIV-EP1, and Sp1 are all inhibited by class F compounds (3, 4). Zinc complexes of class F compounds inhibit NF-κB without affecting zinc finger proteins. Relevant combination of these inhibitors would allow us to inhibit NF-κB, HIV-EP1, and Sp1 in any combinations.

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