1qvu

From Proteopedia

(Difference between revisions)

Current revision

Crystal structure of the multidrug binding transcriptional repressor QacR bound to two drugs: ethidium and proflavine

Structural highlights

1qvu is a 4 chain structure with sequence from Staphylococcus aureus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2.96Å
Ligands:	,
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

QACR_STAAU Transcriptional repressor of qacA. Binds to IR1, an unusually long 28 bp operator, which is located downstream from the qacA promoter and overlaps its transcription start site. QacR is induced from its IR1 site by binding to one of many structurally dissimilar cationic lipophilic compounds, which are also substrates of QacA.

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

The structural basis of simultaneous binding of two or more different drugs by any multidrug-binding protein is unknown and also how this can lead to a noncompetitive, uncompetitive or cooperative binding mechanism. Here, we describe the crystal structure of the Staphylococcus aureus multidrug-binding transcription repressor, QacR, bound simultaneously to ethidium (Et) and proflavin (Pf). The structure underscores the plasticity of the multidrug-binding pocket and reveals an alternative, Pf-induced binding mode for Et. To monitor the simultaneous binding of Pf and Et to QacR, as well as to determine the effects on the binding affinity of one drug when the other drug is prebound, a novel application of near-ultraviolet circular dichroism (UVCD) was developed. The UVCD equilibrium-binding studies revealed identical affinities of Pf for QacR in the presence or absence of Et, but significantly diminished affinity of Et for QacR when Pf is prebound, findings that are readily explicable by their structures. The principles for simultaneous binding of two different drugs discerned here are likely employed by the multidrug efflux transporters.

Structural mechanism of the simultaneous binding of two drugs to a multidrug-binding protein.,Schumacher MA, Miller MC, Brennan RG EMBO J. 2004 Aug 4;23(15):2923-30. Epub 2004 Jul 15. PMID:15257299^[1]

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

References

↑ Schumacher MA, Miller MC, Brennan RG. Structural mechanism of the simultaneous binding of two drugs to a multidrug-binding protein. EMBO J. 2004 Aug 4;23(15):2923-30. Epub 2004 Jul 15. PMID:15257299 doi:http://dx.doi.org/10.1038/sj.emboj.7600288

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/1qvu"

Categories: Large Structures | Staphylococcus aureus | Brennan RG | Miller MC | Schumacher MA

@@ Line 3: / Line 3: @@
 <StructureSection load='1qvu' size='340' side='right'caption='[[1qvu]], [[Resolution|resolution]] 2.96&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[1qvu]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/"micrococcus_aureus"_(rosenbach_1884)_zopf_1885 "micrococcus aureus" (rosenbach 1884) zopf 1885]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QVU OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=1QVU FirstGlance]. <br>
+<table><tr><td colspan='2'>[[1qvu]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QVU OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1QVU FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ET:ETHIDIUM'>ET</scene>, <scene name='pdbligand=PRL:PROFLAVIN'>PRL</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]] 2.96&#8491;</td></tr>
-<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1qvt|1qvt]], [[1jty|1jty]], [[1jt0|1jt0]], [[1jus|1jus]], [[1jt6|1jt6]], [[1jtx|1jtx]]</div></td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ET:ETHIDIUM'>ET</scene>, <scene name='pdbligand=PRL:PROFLAVIN'>PRL</scene></td></tr>
-<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">QACR OR SAVP031 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=1280 "Micrococcus aureus" (Rosenbach 1884) Zopf 1885])</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=1qvu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1qvu OCA], [https://pdbe.org/1qvu PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1qvu RCSB], [https://www.ebi.ac.uk/pdbsum/1qvu PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1qvu ProSAT]</span></td></tr>
-<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=1qvu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1qvu OCA], [http://pdbe.org/1qvu PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1qvu RCSB], [http://www.ebi.ac.uk/pdbsum/1qvu PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1qvu ProSAT]</span></td></tr>
 </table>
 == Function ==
-[[http://www.uniprot.org/uniprot/QACR_STAAU QACR_STAAU]] Transcriptional repressor of qacA. Binds to IR1, an unusually long 28 bp operator, which is located downstream from the qacA promoter and overlaps its transcription start site. QacR is induced from its IR1 site by binding to one of many structurally dissimilar cationic lipophilic compounds, which are also substrates of QacA.
+[https://www.uniprot.org/uniprot/QACR_STAAU QACR_STAAU] Transcriptional repressor of qacA. Binds to IR1, an unusually long 28 bp operator, which is located downstream from the qacA promoter and overlaps its transcription start site. QacR is induced from its IR1 site by binding to one of many structurally dissimilar cationic lipophilic compounds, which are also substrates of QacA.
 == Evolutionary Conservation ==
 [[Image:Consurf_key_small.gif|200px|right]]
@@ Line 33: / Line 32: @@
 ==See Also==
 *[[Tetracycline repressor protein 3D structures|Tetracycline repressor protein 3D structures]]
+*[[Transcriptional activator 3D structures|Transcriptional activator 3D structures]]
 == References ==
 <references/>
@@ Line 38: / Line 38: @@
 </StructureSection>
 [[Category: Large Structures]]
-[[Category: Brennan, R G]]
+[[Category: Staphylococcus aureus]]
-[[Category: Miller, M C]]
+[[Category: Brennan RG]]
-[[Category: Schumacher, M A]]
+[[Category: Miller MC]]
-[[Category: Cooperative dna binding]]
+[[Category: Schumacher MA]]
-[[Category: Multidrug binding protein]]
-[[Category: Qacr]]
-[[Category: Repressor]]
-[[Category: Transcription]]

1qvu

From Proteopedia

Current revision

Crystal structure of the multidrug binding transcriptional repressor QacR bound to two drugs: ethidium and proflavine

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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