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Title
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Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors.
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Authors
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J.Ding,
K.Das,
H.Moereels,
L.Koymans,
K.Andries,
P.A.Janssen,
S.H.Hughes,
E.Arnold.
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Ref.
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Nat Struct Biol, 1995,
2,
407-415.
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PubMed id
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Abstract
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We report the structure of HIV-1 reverse transcriptase (RT) complexed with the
nonnucleoside inhibitor TIBO R 86183 at 3.0 A resolution. Comparing this
structure with those of complexes of HIV-1 RT/alpha-APA R 95845 and HIV-1
RT/nevirapine provides a basis for understanding the nature of nonnucleoside
inhibitor binding, the structure of the binding site and the interactions
between the bound inhibitors and surrounding amino acid residues as well as for
understanding mechanisms of inhibition by and resistance to nonnucleoside
inhibitors. All three inhibitors considered assume a similar butterfly-like
shape and bind to HIV-1 RT in a very similar way. Important differences occur in
the conformation of amino acid residues that form the binding pocket.
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