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1fko

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[[Image:1fko.gif|left|200px]]
[[Image:1fko.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1fko |SIZE=350|CAPTION= <scene name='initialview01'>1fko</scene>, resolution 2.9&Aring;
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The line below this paragraph, containing "STRUCTURE_1fko", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CSD:3-SULFINOALANINE'>CSD</scene>, <scene name='pdbligand=EFZ:(-)-6-CHLORO-4-CYCLOPROPYLETHYNYL-4-TRIFLUOROMETHYL-1,4-DIHYDRO-2H-3,1-BENZOXAZIN-2-ONE'>EFZ</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/RNA-directed_DNA_polymerase RNA-directed DNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.49 2.7.7.49] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1fko| PDB=1fko | SCENE= }}
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|RELATEDENTRY=[[1rtv|1rtv]], [[1rth|1rth]], [[1vru|1vru]], [[1rti|1rti]], [[1rtj|1rtj]], [[1rev|1rev]], [[1rt1|1rt1]], [[1rt2|1rt2]], [[1klm|1klm]], [[1rt3|1rt3]], [[1rt4|1rt4]], [[1rt5|1rt5]], [[1rt6|1rt6]], [[1rt7|1rt7]], [[1c0t|1c0t]], [[1c0u|1c0u]], [[1c1b|1c1b]], [[1c1c|1c1c]], [[1dtq|1dtq]], [[1dtt|1dtt]], [[1ep4|1ep4]], [[1fk9|1fk9]], [[1fkp|1fkp]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1fko FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1fko OCA], [http://www.ebi.ac.uk/pdbsum/1fko PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1fko RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF NNRTI RESISTANT K103N MUTANT HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH DMP-266(EFAVIRENZ)'''
'''CRYSTAL STRUCTURE OF NNRTI RESISTANT K103N MUTANT HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH DMP-266(EFAVIRENZ)'''
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[[Category: Stuart, D I.]]
[[Category: Stuart, D I.]]
[[Category: Weaver, K L.]]
[[Category: Weaver, K L.]]
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[[Category: aid]]
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[[Category: Aid]]
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[[Category: dmp-266]]
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[[Category: Dmp-266]]
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[[Category: drug design]]
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[[Category: Drug design]]
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[[Category: drug resistance mutation]]
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[[Category: Drug resistance mutation]]
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[[Category: efavirenz]]
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[[Category: Efavirenz]]
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[[Category: hiv-1 reverse transcriptase]]
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[[Category: Hiv-1 reverse transcriptase]]
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[[Category: non-nucleoside inhibitor]]
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[[Category: Non-nucleoside inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 16:26:21 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:24:53 2008''
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Revision as of 13:26, 2 May 2008

Image:1fko.gif

Template:STRUCTURE 1fko

CRYSTAL STRUCTURE OF NNRTI RESISTANT K103N MUTANT HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH DMP-266(EFAVIRENZ)


Overview

BACKGROUND: Efavirenz is a second-generation non-nucleoside inhibitor of HIV-1 reverse transcriptase (RT) that has recently been approved for use against HIV-1 infection. Compared with first-generation drugs such as nevirapine, efavirenz shows greater resilience to drug resistance mutations within HIV-1 RT. In order to understand the basis for this resilience at the molecular level and to help the design of further-improved anti-AIDS drugs, we have determined crystal structures of efavirenz and nevirapine with wild-type RT and the clinically important K103N mutant. RESULTS: The relatively compact efavirenz molecule binds, as expected, within the non-nucleoside inhibitor binding pocket of RT. There are significant rearrangements of the drug binding site within the mutant RT compared with the wild-type enzyme. These changes, which lead to the repositioning of the inhibitor, are not seen in the interaction with the first-generation drug nevirapine. CONCLUSIONS: The repositioning of efavirenz within the drug binding pocket of the mutant RT, together with conformational rearrangements in the protein, could represent a general mechanism whereby certain second-generation non-nucleoside inhibitors are able to reduce the effect of drug-resistance mutations on binding potency.

About this Structure

1FKO is a Protein complex structure of sequences from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

Structural basis for the resilience of efavirenz (DMP-266) to drug resistance mutations in HIV-1 reverse transcriptase., Ren J, Milton J, Weaver KL, Short SA, Stuart DI, Stammers DK, Structure. 2000 Oct 15;8(10):1089-94. PMID:11080630 Page seeded by OCA on Fri May 2 16:26:21 2008

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