1xbp

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{{STRUCTURE_1xbp| PDB=1xbp | SCENE= }}
{{STRUCTURE_1xbp| PDB=1xbp | SCENE= }}
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'''Inhibition of peptide bond formation by pleuromutilins: The structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with Tiamulin'''
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===Inhibition of peptide bond formation by pleuromutilins: The structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with Tiamulin===
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==Overview==
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Tiamulin, a prominent member of the pleuromutilin class of antibiotics, is a potent inhibitor of protein synthesis in bacteria. Up to now the effect of pleuromutilins on the ribosome has not been determined on a molecular level. The 3.5 A structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with tiamulin provides for the first time a detailed picture of its interactions with the 23S rRNA, thus explaining the molecular mechanism of the antimicrobial activity of the pleuromutilin class of antibiotics. Our results show that tiamulin is located within the peptidyl transferase center (PTC) of the 50S ribosomal subunit with its tricyclic mutilin core positioned in a tight pocket at the A-tRNA binding site. Also, the extension, which protrudes from its mutilin core, partially overlaps with the P-tRNA binding site. Thereby, tiamulin directly inhibits peptide bond formation. Comparison of the tiamulin binding site with other PTC targeting drugs, like chloramphenicol, clindamycin and streptogramins, may facilitate the design of modified or hybridized drugs that extend the applicability of this class of antibiotics.
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{{ABSTRACT_PUBMED_15554968}}
==About this Structure==
==About this Structure==
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[[Category: Pleuromutilin]]
[[Category: Pleuromutilin]]
[[Category: Tiamulin]]
[[Category: Tiamulin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:49:27 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 05:31:49 2008''

Revision as of 02:31, 28 July 2008

Image:1xbp.png

Template:STRUCTURE 1xbp

Inhibition of peptide bond formation by pleuromutilins: The structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with Tiamulin

Template:ABSTRACT PUBMED 15554968

About this Structure

1XBP is a Protein complex structure of sequences from Deinococcus radiodurans. Full crystallographic information is available from OCA.

Reference

Inhibition of peptide bond formation by pleuromutilins: the structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with tiamulin., Schlunzen F, Pyetan E, Fucini P, Yonath A, Harms JM, Mol Microbiol. 2004 Dec;54(5):1287-94. PMID:15554968

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