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| {{STRUCTURE_1bsk| PDB=1bsk | SCENE= }} | | {{STRUCTURE_1bsk| PDB=1bsk | SCENE= }} |
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| '''ZINC DEFORMYLASE INHIBITOR COMPLEX FROM E.COLI'''
| | ===ZINC DEFORMYLASE INHIBITOR COMPLEX FROM E.COLI=== |
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| ==Overview==
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| While protein synthesis in bacteria begins with a formylated methionine, the formyl group of the nascent polypeptide is removed by peptide deformylase. Since eukaryotic protein synthesis does not involve formylation and deformylation at the N-terminus, there has been increasing interest in peptide deformylase as a potential target for antibacterial chemotherapy. Toward this end and to aid in the design of effective antibiotics targeting peptide deformylase, the structures of the protein-inhibitor complexes of both the cobalt and the zinc containing Escherichia coli peptide deformylase bound to the transition-state analogue, (S)-2-O-(H-phosphonoxy)-L-caproyl-L-leucyl-p-nitroanilide (PCLNA), have been determined. The proteins for both deformylase-inhibitor complexes show basically the same fold as for the native enzyme. The PCLNA inhibitor adopts an extended conformation and fits nicely into a hydrophobic cavity located near the metal site. On the basis of these structures, guidelines for the design of high-affinity deformylase inhibitors are suggested. As our results show that the protein residues which interact with the PCLNA inhibitor are conserved over a wide variety of species, we suggest that antibiotics targeting deformylase could have wide applicability.
| | The line below this paragraph, {{ABSTRACT_PUBMED_10200158}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 10200158 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_10200158}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Inhibitor]] | | [[Category: Inhibitor]] |
| [[Category: Metalloproteinase]] | | [[Category: Metalloproteinase]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 11:54:22 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 19:39:25 2008'' |