Illimaquinone, a selective inhibitor of the RNase H activity of human immunodeficiency virus type 1 reverse transcriptase.
We studied the effect of the natural marine substance illimaquinone on the catalytic activities of reverse transcriptase from human immunodeficiency virus type 1. Illimaquinone inhibited the RNase H activity of the enzyme at concentrations of 5 to 10 microgram/ml, whereas RNA-dependent DNA polymerase and DNA-dependent DNA polymerase activities were considerably less susceptible to this inhibition. Two synthetic derivatives of illimaquinone, in which the 6'-hydroxyl group at the ortho position to one of carbonyl groups of the quinone ring was modified, proved ineffective in inhibiting the human immunodeficiency virus type 1 reverse transcriptase RNase H function, suggesting involvement of the 6'-hydroxyl group in blocking the enzymatic activity.
Loya
S
S
Department of Cell Biology and Histology, Sackler School of Medicine, Tel Aviv, Israel.
Tal
R
R
Kashman
Y
Y
Hizi
A
A
D004722:Endoribonucleases / Q000037:antagonists & inhibitors*; D006678:HIV / Q000187:drug effects* / Q000201:enzymology; D011809:Quinones / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors; D016914:Ribonuclease H; D013329:Structure-Activity Relationship
D011809:Quinones; D018894:Reverse Transcriptase Inhibitors; C067346:illimaquinone; D004722:Endoribonucleases; D016914:Ribonuclease H