Document 0100
 DOCN  M94A0100
 TI    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.
 DT    9412
 AU    Rubinek T; McMahon JB; Hizi A; Department of Cell Biology and Histology,
       Sackler School of; Medicine, Tel Aviv University, Israel.
 SO    FEBS Lett. 1994 Aug 22;350(2-3):299-303. Unique Identifier : AIDSLINE
       MED/94350120
 AB    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.
 DE    Antiviral Agents/PHARMACOLOGY  Benzoates/*PHARMACOLOGY  Chimeric
       Proteins  HIV-1/ENZYMOLOGY  HIV-2/ENZYMOLOGY  Reverse
       Transcriptase/*ANTAGONISTS & INHIB  Structure-Activity Relationship
       Sulfones/*PHARMACOLOGY  Support, U.S. Gov't, P.H.S.
       Thiocarbamates/*PHARMACOLOGY  JOURNAL ARTICLE

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