1c1b

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[[Image:1c1b.gif|left|200px]]
[[Image:1c1b.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1c1b |SIZE=350|CAPTION= <scene name='initialview01'>1c1b</scene>, resolution 2.5&Aring;
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The line below this paragraph, containing "STRUCTURE_1c1b", 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=CSW:CYSTEINE-S-DIOXIDE'>CSW</scene>, <scene name='pdbligand=GCA:6-(3&#39;,5&#39;-DIMETHYLBENZYL)-1-ETHOXYMETHYL-5-ISOPROPYLURACIL'>GCA</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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|DOMAIN=
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{{STRUCTURE_1c1b| PDB=1c1b | 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]], [[1c1c|1C1C]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1c1b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1c1b OCA], [http://www.ebi.ac.uk/pdbsum/1c1b PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1c1b RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GCA-186'''
'''CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GCA-186'''
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[[Category: Stuart, D I.]]
[[Category: Stuart, D I.]]
[[Category: Tanaka, H.]]
[[Category: Tanaka, H.]]
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[[Category: aid]]
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[[Category: Aid]]
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[[Category: drug design]]
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[[Category: Drug design]]
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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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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 12:12:53 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 19:12:27 2008''
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Revision as of 09:12, 2 May 2008

Image:1c1b.gif

Template:STRUCTURE 1c1b

CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GCA-186


Overview

Two analogues of the nonnucleoside inhibitor of HIV-1 RT, MKC-442 (emivirine), containing different C6 substituents have been designed to be less susceptible to the commonly found drug-resistance mutation of Tyr181Cys. Compound TNK-6123 had a C6 thiocyclohexyl group designed to have more flexibility in adapting to the mutated drug-binding site. GCA-186 had additional 3',5'-dimethyl substituents aimed at forming close contacts with the conserved residue Trp229. Both compounds showed approximately 30-fold greater inhibitory effect than MKC-442 to the Tyr181Cys mutant virus as well as to the clinically important Lys103Asn virus. X-ray crystallographic structure determination of complexes with HIV-1 RT confirmed the predicted binding modes. These strategies might be used to improve the resilience of other NNRTI series against common drug-resistance mutations.

About this Structure

1C1B is a Protein complex structure of sequences from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

Design of MKC-442 (emivirine) analogues with improved activity against drug-resistant HIV mutants., Hopkins AL, Ren J, Tanaka H, Baba M, Okamato M, Stuart DI, Stammers DK, J Med Chem. 1999 Nov 4;42(22):4500-5. PMID:10579814 Page seeded by OCA on Fri May 2 12:12:53 2008

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OCA

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