2bb7

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{{STRUCTURE_2bb7| PDB=2bb7 | SCENE= }}
{{STRUCTURE_2bb7| PDB=2bb7 | SCENE= }}
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'''Mn Form Of E. coli Methionine Aminopeptidase In Complex With a quinolinyl sulfonamide inhibitor'''
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===Mn Form Of E. coli Methionine Aminopeptidase In Complex With a quinolinyl sulfonamide inhibitor===
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==Overview==
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Quinolinyl sulfonamides, such as N-(quinolin-8-yl)methanesulfonamide (10) and N-(5-chloroquinolin-8-yl)methanesulfonamide (11), were identified as potent methionine aminopeptidase (MetAP) inhibitors by high throughput screening of a diverse chemical library of small organic compounds. They showed different inhibitory potencies on Co(II)-, Ni(II)-, Fe(II)-, Mn(II)-, and Zn(II)-forms of Escherichia coli MetAP, and their inhibition is dependent on metal concentration. X-ray structures of E. coli MetAP complexed with 10 revealed that the inhibitor forms a metal complex with the residue H79 at the enzyme active site; the complex is further stabilized by an extended H-bond and metal interaction network. Analysis of the inhibition of MetAP by these inhibitors indicates that this is a typical mechanism of inhibition for many non-peptidic MetAP inhibitors and emphasizes the importance of defining in vitro conditions for identifying and evaluating MetAP inhibitors that will be capable of giving information relevant to the in vivo situation.
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{{ABSTRACT_PUBMED_16300729}}
==About this Structure==
==About this Structure==
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[[Category: Metalloenzyme]]
[[Category: Metalloenzyme]]
[[Category: Trimetallic]]
[[Category: Trimetallic]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:03:53 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 05:07:42 2008''

Revision as of 02:07, 29 July 2008

Image:2bb7.png

Template:STRUCTURE 2bb7

Mn Form Of E. coli Methionine Aminopeptidase In Complex With a quinolinyl sulfonamide inhibitor

Template:ABSTRACT PUBMED 16300729

About this Structure

2BB7 is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

Metal mediated inhibition of methionine aminopeptidase by quinolinyl sulfonamides., Huang M, Xie SX, Ma ZQ, Hanzlik RP, Ye QZ, Biochem Biophys Res Commun. 2006 Jan 13;339(2):506-13. Epub 2005 Nov 15. PMID:16300729

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