2oz5

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{{STRUCTURE_2oz5| PDB=2oz5 | SCENE= }}
{{STRUCTURE_2oz5| PDB=2oz5 | SCENE= }}
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'''Crystal structure of Mycobacterium tuberculosis protein tyrosine phosphatase PtpB in complex with the specific inhibitor OMTS'''
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===Crystal structure of Mycobacterium tuberculosis protein tyrosine phosphatase PtpB in complex with the specific inhibitor OMTS===
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==Overview==
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Tyrosine kinases and phosphatases establish the crucial balance of tyrosine phosphorylation in cellular signaling, but creating specific inhibitors of protein Tyr phosphatases (PTPs) remains a challenge. Here, we report the development of a potent, selective inhibitor of Mycobacterium tuberculosis PtpB, a bacterial PTP that is secreted into host cells where it disrupts unidentified signaling pathways. The inhibitor, (oxalylamino-methylene)-thiophene sulfonamide (OMTS), showed an IC(50) of 440 +/- 50 nM and &gt;60-fold specificity for PtpB over six human PTPs. The 2 A resolution crystal structure of PtpB in complex with OMTS revealed a large rearrangement of the enzyme, with some residues shifting &gt;27 A relative to the PtpB:PO(4) complex. Extensive contacts with the catalytic loop provide a potential basis for inhibitor selectivity. Two OMTS molecules bound adjacent to each other, raising the possibility of a second substrate phosphotyrosine binding site in PtpB. The PtpB:OMTS structure provides an unanticipated framework to guide inhibitor improvement.
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The line below this paragraph, {{ABSTRACT_PUBMED_17437721}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17437721 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17437721}}
==About this Structure==
==About this Structure==
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[[Category: Tb structural genomics consortium]]
[[Category: Tb structural genomics consortium]]
[[Category: Tbsgc]]
[[Category: Tbsgc]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:58:28 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 14:34:06 2008''

Revision as of 11:34, 29 July 2008

Image:2oz5.png

Template:STRUCTURE 2oz5

Crystal structure of Mycobacterium tuberculosis protein tyrosine phosphatase PtpB in complex with the specific inhibitor OMTS

Template:ABSTRACT PUBMED 17437721

About this Structure

2OZ5 is a Single protein structure of sequence from Mycobacterium tuberculosis. Full crystallographic information is available from OCA.

Reference

Structural basis for selective inhibition of Mycobacterium tuberculosis protein tyrosine phosphatase PtpB., Grundner C, Perrin D, Hooft van Huijsduijnen R, Swinnen D, Gonzalez J, Gee CL, Wells TN, Alber T, Structure. 2007 Apr;15(4):499-509. PMID:17437721

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