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| {{STRUCTURE_1mu2| PDB=1mu2 | SCENE= }} | | {{STRUCTURE_1mu2| PDB=1mu2 | SCENE= }} |
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| '''CRYSTAL STRUCTURE OF HIV-2 REVERSE TRANSCRIPTASE'''
| | ===CRYSTAL STRUCTURE OF HIV-2 REVERSE TRANSCRIPTASE=== |
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| ==Overview==
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| The HIV-2 serotype of HIV is a cause of disease in parts of the West African population, and there is evidence for its spread to Europe and Asia. HIV-2 reverse transcriptase (RT) demonstrates an intrinsic resistance to non-nucleoside RT inhibitors (NNRTIs), one of two classes of anti-AIDS drugs that target the viral RT. We report the crystal structure of HIV-2 RT to 2.35 A resolution, which reveals molecular details of the resistance to NNRTIs. HIV-2 RT has a similar overall fold to HIV-1 RT but has structural differences within the "NNRTI pocket" at both conserved and nonconserved residues. The structure points to the role of sequence differences that can give rise to unfavorable inhibitor contacts or destabilization of part of the binding pocket at positions 101, 106, 138, 181, 188, and 190. We also present evidence that the conformation of Ile-181 compared with the HIV-1 Tyr-181 could be a significant contributory factor to this inherent drug resistance of HIV-2 to NNRTIs. The availability of a refined structure of HIV-2 RT will provide a stimulus for the structure-based design of novel non-nucleoside inhibitors that could be used against HIV-2 infection. | | The line below this paragraph, {{ABSTRACT_PUBMED_12386343}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 12386343 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_12386343}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Hiv-2 reverse transcriptase]] | | [[Category: Hiv-2 reverse transcriptase]] |
| [[Category: Polymerase]] | | [[Category: Polymerase]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 01:42:48 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:26:34 2008'' |