2hah

From Proteopedia

(Difference between revisions)

Current revision

The structure of FIV 12S protease in complex with TL-3

Structural highlights

2hah is a 1 chain structure with sequence from Feline immunodeficiency virus (isolate Petaluma). Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 1.7Å
Ligands:
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

Q66972_9RETR

Evolutionary Conservation

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

Publication Abstract from PubMed

We have obtained the 1.7 A crystal structure of FIV protease (PR) in which 12 critical residues around the active site have been substituted with the structurally equivalent residues of HIV PR (12X FIV PR). The chimeric PR was crystallized in complex with the broad-based inhibitor TL-3, which inhibits wild type FIV and HIV PRs, as well as 12X FIV PR and several drug-resistant HIV mutants 1234. Biochemical analyses have demonstrated that TL-3 inhibits these PRs in the order HIV PR > 12X FIV PR > FIV PR, with Ki values of 1.5 nM, 10 nM, and 41 nM, respectively 234. Comparison of the crystal structures of the TL-3 complexes of 12X FIV and wild-typeFIV PR revealed theformation of additinal van der Waals interactions between the enzyme inhibitor in the mutant PR. The 12X FIV PR retained the hydrogen bonding interactions between residues in the flap regions and active site involving the enzyme and the TL-3 inhibitor in comparison to both FIV PR and HIV PR. However, the flap regions of the 12X FIV PR more closely resemble those of HIV PR, having gained several stabilizing intra-flap interactions not present in wild type FIV PR. These findings offer a structural explanation for the observed inhibitor/substrate binding properties of the chimeric PR.

Crystal structure of an FIV/HIV chimeric protease complexed with the broad-based inhibitor, TL-3.,Heaslet H, Lin YC, Tam K, Torbett BE, Elder JH, Stout CD Retrovirology. 2007 Jan 9;4:1. PMID:17212810^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Heaslet H, Lin YC, Tam K, Torbett BE, Elder JH, Stout CD. Crystal structure of an FIV/HIV chimeric protease complexed with the broad-based inhibitor, TL-3. Retrovirology. 2007 Jan 9;4:1. PMID:17212810 doi:10.1186/1742-4690-4-1

1 Structural highlights
2 Function
3 Evolutionary Conservation
4 Publication Abstract from PubMed
5 See Also
6 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2hah"

Categories: Large Structures | Elder JH | Heaslet H | Lin YC | Stout CD

@@ Line 1: / Line 1: @@
 ==The structure of FIV 12S protease in complex with TL-3==
-<StructureSection load='2hah' size='340' side='right' caption='[[2hah]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
+<StructureSection load='2hah' size='340' side='right'caption='[[2hah]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[2hah]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Fiv Fiv]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HAH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2HAH FirstGlance]. <br>
+<table><tr><td colspan='2'>[[2hah]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Feline_immunodeficiency_virus_(isolate_Petaluma) Feline immunodeficiency virus (isolate Petaluma)]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HAH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2HAH FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3TL:BENZYL+[(1S,4S,7S,8R,9R,10S,13S,16S)-7,10-DIBENZYL-8,9-DIHYDROXY-1,16-DIMETHYL-4,13-BIS(1-METHYLETHYL)-2,5,12,15,18-PENTAOXO-20-PHENYL-19-OXA-3,6,11,14,17-PENTAAZAICOS-1-YL]CARBAMATE'>3TL</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.7&#8491;</td></tr>
-<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5fiv|5fiv]], [[2az8|2az8]]</td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3TL:BENZYL+[(1S,4S,7S,8R,9R,10S,13S,16S)-7,10-DIBENZYL-8,9-DIHYDROXY-1,16-DIMETHYL-4,13-BIS(1-METHYLETHYL)-2,5,12,15,18-PENTAOXO-20-PHENYL-19-OXA-3,6,11,14,17-PENTAAZAICOS-1-YL]CARBAMATE'>3TL</scene></td></tr>
-<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">POL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=11674 FIV])</td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2hah FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2hah OCA], [https://pdbe.org/2hah PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2hah RCSB], [https://www.ebi.ac.uk/pdbsum/2hah PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2hah ProSAT]</span></td></tr>
-<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] </span></td></tr>
-<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2hah FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2hah OCA], [http://pdbe.org/2hah PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2hah RCSB], [http://www.ebi.ac.uk/pdbsum/2hah PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2hah ProSAT]</span></td></tr>
 </table>
 == Function ==
-[[http://www.uniprot.org/uniprot/POL_FIVPE POL_FIVPE]] During replicative cycle of retroviruses, the reverse-transcribed viral DNA is integrated into the host chromosome by the viral integrase enzyme. RNase H activity is associated with the reverse transcriptase.
+[https://www.uniprot.org/uniprot/Q66972_9RETR Q66972_9RETR]
 == Evolutionary Conservation ==
 [[Image:Consurf_key_small.gif|200px|right]]
@@ Line 33: / Line 31: @@
 ==See Also==
-*[[Immunodeficiency virus protease|Immunodeficiency virus protease]]
+*[[Immunodeficiency virus protease 3D structures|Immunodeficiency virus protease 3D structures]]
 == References ==
 <references/>
 __TOC__
 </StructureSection>
-[[Category: Fiv]]
+[[Category: Large Structures]]
-[[Category: HIV-1 retropepsin]]
+[[Category: Elder JH]]
-[[Category: Elder, J H]]
+[[Category: Heaslet H]]
-[[Category: Heaslet, H]]
+[[Category: Lin YC]]
-[[Category: Lin, Y C]]
+[[Category: Stout CD]]
-[[Category: Stout, C D]]
-[[Category: Aspartyl]]
-[[Category: Feline]]
-[[Category: Hydrolase-hydrolase inhibitor complex]]
-[[Category: Protease]]
-[[Category: Retroviral]]

2hah

From Proteopedia

Current revision

The structure of FIV 12S protease in complex with TL-3

Structural highlights

Function

Evolutionary Conservation

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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