2j7l: Difference between revisions
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[[Image:2j7l.jpg|left|200px]]<br /><applet load="2j7l" size=" | [[Image:2j7l.jpg|left|200px]]<br /><applet load="2j7l" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="2j7l, resolution 2.6Å" /> | caption="2j7l, resolution 2.6Å" /> | ||
'''E.COLI P PILUS CHAPERONE PAPD IN COMPLEX WITH A PILUS BIOGENESIS INHIBITOR, PILICIDE 2C'''<br /> | '''E.COLI P PILUS CHAPERONE PAPD IN COMPLEX WITH A PILUS BIOGENESIS INHIBITOR, PILICIDE 2C'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
2J7L is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] with XC2 as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Xc2 Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | 2J7L is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] with <scene name='pdbligand=XC2:'>XC2</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Xc2+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2J7L OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: periplasmic]] | [[Category: periplasmic]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:42:32 2008'' | ||
Revision as of 11:42, 3 February 2008
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E.COLI P PILUS CHAPERONE PAPD IN COMPLEX WITH A PILUS BIOGENESIS INHIBITOR, PILICIDE 2C
OverviewOverview
A chemical synthesis platform with broad applications and flexibility was, rationally designed to inhibit biogenesis of adhesive pili assembled by, the chaperone-usher pathway in Gram-negative pathogens. The activity of a, family of bicyclic 2-pyridones, termed pilicides, was evaluated in two, different pilus biogenesis systems in uropathogenic Escherichia coli., Hemagglutination mediated by either type 1 or P pili, adherence to bladder, cells, and biofilm formation mediated by type 1 pili were all reduced by, approximately 90% in laboratory and clinical E. coli strains. The, structure of the pilicide bound to the P pilus chaperone PapD revealed, that the pilicide bound to the surface of the chaperone known to interact, with the usher, the outer-membrane assembly platform where pili are, assembled. Point mutations in the pilicide-binding site dramatically, reduced pilus formation but did not block the ability of PapD to bind, subunits and mediate their folding. Surface plasmon resonance experiments, confirmed that the pilicide interfered with the binding of, chaperone-subunit complexes to the usher. These pilicides thus target key, virulence factors in pathogenic bacteria and represent a promising proof, of concept for developing drugs that function by targeting virulence, factors.
About this StructureAbout this Structure
2J7L is a Single protein structure of sequence from Escherichia coli with as ligand. Known structural/functional Site: . Full crystallographic information is available from OCA.
ReferenceReference
Rationally designed small compounds inhibit pilus biogenesis in uropathogenic bacteria., Pinkner JS, Remaut H, Buelens F, Miller E, Aberg V, Pemberton N, Hedenstrom M, Larsson A, Seed P, Waksman G, Hultgren SJ, Almqvist F, Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17897-902. Epub 2006 Nov 10. PMID:17098869
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