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5xp9

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Revision as of 06:56, 14 October 2020

Crystal structure of Bismuth bound NDM-1

Structural highlights

5xp9 is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Activity:	Beta-lactamase, with EC number 3.5.2.6
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[BLAN1_KLEPN] Confers resistance to many beta-lactam antibiotics, including some carbapenems. Does not confer resistance to the polymixin colistin or the fluoroquinolone ciprofloxacin.

Publication Abstract from PubMed

Drug-resistant superbugs pose a huge threat to human health. Infections by Enterobacteriaceae producing metallo-beta-lactamases (MBLs), e.g., New Delhi metallo-beta-lactamase 1 (NDM-1) are very difficult to treat. Development of effective MBL inhibitors to revive the efficacy of existing antibiotics is highly desirable. However, such inhibitors are not clinically available till now. Here we show that an anti-Helicobacter pylori drug, colloidal bismuth subcitrate (CBS), and related Bi(III) compounds irreversibly inhibit different types of MBLs via the mechanism, with one Bi(III) displacing two Zn(II) ions as revealed by X-ray crystallography, leading to the release of Zn(II) cofactors. CBS restores meropenem (MER) efficacy against MBL-positive bacteria in vitro, and in mice infection model, importantly, also slows down the development of higher-level resistance in NDM-1-positive bacteria. This study demonstrates a high potential of Bi(III) compounds as the first broad-spectrum B1 MBL inhibitors to treat MBL-positive bacterial infection in conjunction with existing carbapenems.

Bismuth antimicrobial drugs serve as broad-spectrum metallo-beta-lactamase inhibitors.,Wang R, Lai TP, Gao P, Zhang H, Ho PL, Woo PC, Ma G, Kao RY, Li H, Sun H Nat Commun. 2018 Jan 30;9(1):439. doi: 10.1038/s41467-018-02828-6. PMID:29382822^[1]

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

References

↑ Wang R, Lai TP, Gao P, Zhang H, Ho PL, Woo PC, Ma G, Kao RY, Li H, Sun H. Bismuth antimicrobial drugs serve as broad-spectrum metallo-beta-lactamase inhibitors. Nat Commun. 2018 Jan 30;9(1):439. doi: 10.1038/s41467-018-02828-6. PMID:29382822 doi:http://dx.doi.org/10.1038/s41467-018-02828-6

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

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/5xp9"

@@ Line 1: / Line 1: @@
 ==Crystal structure of Bismuth bound NDM-1==
-<StructureSection load='5xp9' size='340' side='right' caption='[[5xp9]], [[Resolution|resolution]] 1.55&Aring;' scene=''>
+<StructureSection load='5xp9' size='340' side='right'caption='[[5xp9]], [[Resolution|resolution]] 1.55&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[5xp9]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5XP9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5XP9 FirstGlance]. <br>
+<table><tr><td colspan='2'>[[5xp9]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5XP9 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5XP9 FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BS3:BISMUTH(III)+ION'>BS3</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
+</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BS3:BISMUTH(III)+ION'>BS3</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
 <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Beta-lactamase Beta-lactamase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.5.2.6 3.5.2.6] </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=5xp9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5xp9 OCA], [http://pdbe.org/5xp9 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5xp9 RCSB], [http://www.ebi.ac.uk/pdbsum/5xp9 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5xp9 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=5xp9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5xp9 OCA], [http://pdbe.org/5xp9 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5xp9 RCSB], [http://www.ebi.ac.uk/pdbsum/5xp9 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5xp9 ProSAT]</span></td></tr>
 </table>
 == Function ==
@@ Line 19: / Line 19: @@
 </div>
 <div class="pdbe-citations 5xp9" style="background-color:#fffaf0;"></div>
+==See Also==
+*[[Beta-lactamase 3D structures|Beta-lactamase 3D structures]]
 == References ==
 <references/>
@@ Line 24: / Line 27: @@
 </StructureSection>
 [[Category: Beta-lactamase]]
+[[Category: Large Structures]]
 [[Category: Lai, T P]]
 [[Category: Ma, G]]

5xp9

From Proteopedia

Revision as of 06:56, 14 October 2020

Crystal structure of Bismuth bound NDM-1

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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