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The inhibition of human immunodeficiency virus type 1 reverse transcriptase by avarol and avarone derivatives
Author(s) -
Loya Shoshana,
Hizi Am
Publication year - 1990
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(90)81137-d
Subject(s) - reverse transcriptase , virology , human immunodeficiency virus (hiv) , chemistry , biology , biochemistry , rna , gene
We have analyzed the effects of several natural compounds related to avarols and avarones on the catalytic functions of human immunodeficiency virus type 1 (HIV‐1) reverse transcriptase (RT). The most potent substances, designated as avarone A,B and E and avarol F, inhibited indiscriminately the enzymatic activities of HIV‐1 RT, namely the RNA‐dependent and DNA‐dependent DNA polymerase as well as the ribonuclease H. The inhibition of the DNA polymerase activity was found to be non‐competitive with respect to either the template‐primer or the deoxynucleotide‐triphosphate. These studies suggest that the hydroxyl group at the ortho position to the carbonyl group at the quinone ring is involved in blocking the RT activity. The identification of the active site of the inhibitors will hopefully lead to the rational design of new potent anti‐HIV drugs.