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==Overview==

We have used a structure-based approach to design a novel series of, non-nucleoside inhibitors of HIV-1 RT (NNRTIs). Detailed analysis of a, wide range of crystal structures of HIV-1 RT-NNRTI complexes together with, data on drug resistance mutations has identified factors important for, tight binding of inhibitors and resilience to mutations. Using this, approach we have designed and synthesized a novel series of quinolone, NNRTIs. Crystal structure analysis of four of these compounds in complexes, with HIV-1 RT confirms the predicted binding modes. Members of this, quinolone series retain high activity against the important resistance, mutations in RT at Tyr181Cys and Leu100Ile.

We have used a structure-based approach to design a novel series of non-nucleoside inhibitors of HIV-1 RT (NNRTIs). Detailed analysis of a wide range of crystal structures of HIV-1 RT-NNRTI complexes together with data on drug resistance mutations has identified factors important for tight binding of inhibitors and resilience to mutations. Using this approach we have designed and synthesized a novel series of quinolone NNRTIs. Crystal structure analysis of four of these compounds in complexes with HIV-1 RT confirms the predicted binding modes. Members of this quinolone series retain high activity against the important resistance mutations in RT at Tyr181Cys and Leu100Ile.

==About this Structure==

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[[Category: Protein complex]]

[[Category: RNA-directed DNA polymerase]]

[[Category: Hopkins, A.L.]]

[[Category: Hopkins, A L.]]

[[Category: Ren, J.]]

[[Category: Stammers, D.K.]]

[[Category: Stammers, D K.]]

[[Category: Stuart, D.I.]]

[[Category: Stuart, D I.]]

[[Category: H18]]

[[Category: PO4]]

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[[Category: nnrti]]

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@@ Line 4: / Line 4: @@
 ==Overview==
-We have used a structure-based approach to design a novel series of, non-nucleoside inhibitors of HIV-1 RT (NNRTIs). Detailed analysis of a, wide range of crystal structures of HIV-1 RT-NNRTI complexes together with, data on drug resistance mutations has identified factors important for, tight binding of inhibitors and resilience to mutations. Using this, approach we have designed and synthesized a novel series of quinolone, NNRTIs. Crystal structure analysis of four of these compounds in complexes, with HIV-1 RT confirms the predicted binding modes. Members of this, quinolone series retain high activity against the important resistance, mutations in RT at Tyr181Cys and Leu100Ile.
+We have used a structure-based approach to design a novel series of non-nucleoside inhibitors of HIV-1 RT (NNRTIs). Detailed analysis of a wide range of crystal structures of HIV-1 RT-NNRTI complexes together with data on drug resistance mutations has identified factors important for tight binding of inhibitors and resilience to mutations. Using this approach we have designed and synthesized a novel series of quinolone NNRTIs. Crystal structure analysis of four of these compounds in complexes with HIV-1 RT confirms the predicted binding modes. Members of this quinolone series retain high activity against the important resistance mutations in RT at Tyr181Cys and Leu100Ile.
 ==About this Structure==
@@ Line 14: / Line 14: @@
 [[Category: Protein complex]]
 [[Category: RNA-directed DNA polymerase]]
-[[Category: Hopkins, A.L.]]
+[[Category: Hopkins, A L.]]
 [[Category: Ren, J.]]
-[[Category: Stammers, D.K.]]
+[[Category: Stammers, D K.]]
-[[Category: Stuart, D.I.]]
+[[Category: Stuart, D I.]]
 [[Category: H18]]
 [[Category: PO4]]
@@ Line 26: / Line 26: @@
 [[Category: nnrti]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:57:31 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:14:44 2008''