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M94A0100.TXT
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1994-10-01
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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
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).