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| [[Image:2b0q.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_2b0q| PDB=2b0q | SCENE= }} | | {{STRUCTURE_2b0q| PDB=2b0q | SCENE= }} |
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| '''Crystal Structure Of 3',5"-Aminoglycoside Phosphotransferase Type IIIa ADP Neomycin B Complex'''
| | ===Crystal Structure Of 3',5"-Aminoglycoside Phosphotransferase Type IIIa ADP Neomycin B Complex=== |
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| ==Overview==
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| The misuse of antibiotics has selected for bacteria that have evolved mechanisms for evading the effects of these drugs. For aminoglycosides, a group of clinically important bactericidal antibiotics that target the A-site of the 16S ribosomal RNA, the most common mode of resistance is enzyme-catalyzed chemical modification of the drug. While aminoglycosides are structurally diverse, a single enzyme can confer resistance to many of these antibiotics. For example, the aminoglycoside kinase APH(3')-IIIa, produced by pathogenic Gram-positive bacteria such as enterococci and staphylococci, is capable of detoxifying at least 10 distinct aminoglycosides. Here we describe the crystal structures of APH(3')-IIIa in complex with ADP and kanamycin A or neomycin B. These structures reveal that the basis for this enzyme's substrate promiscuity is the presence of two alternative subsites in the antibiotic binding pocket. Furthermore, comparison between the A-site of the bacterial ribosome and APH(3')-IIIa shows that mimicry is the second major factor in dictating the substrate spectrum of APH(3')-IIIa. These results suggest a potential strategy for drug design aimed at circumventing antibiotic resistance. | | The line below this paragraph, {{ABSTRACT_PUBMED_12006485}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 12006485 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_12006485}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Fong, D H.]] | | [[Category: Fong, D H.]] |
| [[Category: Protein kinase-like]] | | [[Category: Protein kinase-like]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:42:35 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 14:28:36 2008'' |
