5hu4: Difference between revisions
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The entry | ==Cystal structure of listeria monocytogenes sortase A== | ||
<StructureSection load='5hu4' size='340' side='right' caption='[[5hu4]], [[Resolution|resolution]] 2.30Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5hu4]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5HU4 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5HU4 FirstGlance]. <br> | |||
</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=5hu4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5hu4 OCA], [http://pdbe.org/5hu4 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5hu4 RCSB], [http://www.ebi.ac.uk/pdbsum/5hu4 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5hu4 ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
The critical role of sortase A in gram-positive bacterial pathogenicity makes this protein a good potential target for antimicrobial therapy. In this study, we report for the first time the crystal structure of Listeria monocytogenes sortase A and identify the active sites that mediate its transpeptidase activity. We also used a sortase A (SrtA) enzyme activity inhibition assay, simulation, and isothermal titration calorimetry analysis to discover that chalcone, an agent with little anti-L. monocytogenes activity, could significantly inhibit sortase A activity with an IC50 of 28.41 +/- 5.34 muM by occupying the active site of SrtA. The addition of chalcone to a co-culture of L. monocytogenes and Caco-2 cells significantly inhibited bacterial entry into the cells and L. monocytogenes-mediated cytotoxicity. Additionally, chalcone treatment decreased the mortality of infected mice, the bacterial burden in target organs, and the pathological damage to L. monocytogenes-infected mice. In conclusion, these findings suggest that chalcone is a promising candidate for the development of treatment against L. monocytogenes infection. | |||
Inhibition of sortase A by chalcone prevents Listeria monocytogenes infection.,Li H, Chen Y, Zhang B, Niu X, Song M, Luo Z, Lu G, Liu B, Zhao X, Wang J, Deng X Biochem Pharmacol. 2016 Apr 15;106:19-29. doi: 10.1016/j.bcp.2016.01.018. Epub, 2016 Jan 28. PMID:26826492<ref>PMID:26826492</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 5hu4" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Li, H]] | [[Category: Li, H]] | ||
[[Category: Hydrolase]] | |||
[[Category: Protease]] | |||
[[Category: Sortase some]] | |||
Revision as of 20:55, 1 February 2017
Cystal structure of listeria monocytogenes sortase ACystal structure of listeria monocytogenes sortase A
Structural highlights
Publication Abstract from PubMedThe critical role of sortase A in gram-positive bacterial pathogenicity makes this protein a good potential target for antimicrobial therapy. In this study, we report for the first time the crystal structure of Listeria monocytogenes sortase A and identify the active sites that mediate its transpeptidase activity. We also used a sortase A (SrtA) enzyme activity inhibition assay, simulation, and isothermal titration calorimetry analysis to discover that chalcone, an agent with little anti-L. monocytogenes activity, could significantly inhibit sortase A activity with an IC50 of 28.41 +/- 5.34 muM by occupying the active site of SrtA. The addition of chalcone to a co-culture of L. monocytogenes and Caco-2 cells significantly inhibited bacterial entry into the cells and L. monocytogenes-mediated cytotoxicity. Additionally, chalcone treatment decreased the mortality of infected mice, the bacterial burden in target organs, and the pathological damage to L. monocytogenes-infected mice. In conclusion, these findings suggest that chalcone is a promising candidate for the development of treatment against L. monocytogenes infection. Inhibition of sortase A by chalcone prevents Listeria monocytogenes infection.,Li H, Chen Y, Zhang B, Niu X, Song M, Luo Z, Lu G, Liu B, Zhao X, Wang J, Deng X Biochem Pharmacol. 2016 Apr 15;106:19-29. doi: 10.1016/j.bcp.2016.01.018. Epub, 2016 Jan 28. PMID:26826492[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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