2q96

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{{STRUCTURE_2q96| PDB=2q96 | SCENE= }}
{{STRUCTURE_2q96| PDB=2q96 | SCENE= }}
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'''E. coli methionine aminopeptidase Mn-form with inhibitor A18'''
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===E. coli methionine aminopeptidase Mn-form with inhibitor A18===
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==Overview==
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BACKGROUND: Methionine aminopeptidase is a potential target of future antibacterial and anticancer drugs. Structural analysis of complexes of the enzyme with its inhibitors provides valuable information for structure-based drug design efforts. RESULTS: Five new X-ray structures of such enzyme-inhibitor complexes were obtained. Analysis of these and other three similar structures reveals the adaptability of a surface-exposed loop bearing Y62, H63, G64 and Y65 (the YHGY loop) that is an integral part of the substrate and inhibitor binding pocket. This adaptability is important for accommodating inhibitors with variations in size. When compared with the human isozymes, this loop either becomes buried in the human type I enzyme due to an N-terminal extension that covers its position or is replaced by a unique insert in the human type II enzyme. CONCLUSION: The adaptability of the YHGY loop in E. coli methionine aminopeptidase, and likely in other bacterial methionine aminopeptidases, enables the enzyme active pocket to accommodate inhibitors of differing size. The differences in this adaptable loop between the bacterial and human methionine aminopeptidases is a structural feature that can be exploited to design inhibitors of bacterial methionine aminopeptidases as therapeutic agents with minimal inhibition of the corresponding human enzymes.
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(as it appears on PubMed at http://www.pubmed.gov), where 18093325 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18093325}}
==About this Structure==
==About this Structure==
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[[Category: Hydrolase]]
[[Category: Hydrolase]]
[[Category: Metalloenzyme]]
[[Category: Metalloenzyme]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:33:40 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 04:01:05 2008''

Revision as of 01:01, 29 July 2008

Image:2q96.png

Template:STRUCTURE 2q96

E. coli methionine aminopeptidase Mn-form with inhibitor A18

Template:ABSTRACT PUBMED 18093325

About this Structure

2Q96 is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

Structural analysis of inhibition of E. coli methionine aminopeptidase: implication of loop adaptability in selective inhibition of bacterial enzymes., Ma ZQ, Xie SX, Huang QQ, Nan FJ, Hurley TD, Ye QZ, BMC Struct Biol. 2007 Dec 19;7:84. PMID:18093325

Page seeded by OCA on Tue Jul 29 04:01:05 2008

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