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Inhibition of reverse transcriptase of human immunodeficiency virus type 1 and chimeric enzymes of human immunodeficiency viruses types 1 and 2 by two novel non‐nucleoside inhibitors
Author(s) -
Rubinek Tami,
McMahon James B.,
Hizi Am
Publication year - 1994
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(94)00793-4
Subject(s) - reverse transcriptase , nucleoside , virology , enzyme , dna , rna directed dna polymerase , polymerase , dna polymerase , virus , nucleoside analogue , nucleotidyltransferase , sulfone , biology , chemistry , reverse transcriptase inhibitor , human immunodeficiency virus (hiv) , rna , microbiology and biotechnology , biochemistry , gene , polymer chemistry
We have studied the effects of two non‐nucleoside reverse transcriptase inhibitors (NNRTI), nitrophenyl phenyl sulfone (NPPS) and a potent derivative of oxathiin carboxanilide (UC‐38), on enzymatically active molecular chimeras composed of complementary segments of the reverse transcriptases (RTs) of human immunodeficiency virus type 1 (HIV‐1) and ‐2 (HIV‐2). The substances inhibit only the DNA polymerase activity of HIV‐1 RT with no effect on HIV‐2 RT. The results suggest that there is a protein segment located between residues 158 and 190 that is critical for the inhibition by both compounds. However, there is probably a second segment that resides between residues 192 and 202, as in the case of NPPS, or residues 203 and 224, as in the case of UC‐38, that is also crucial for the sensitivity of HIV‐1 RT to both inhibitors.