1ynn: Difference between revisions

Revision as of 16:33, 3 May 2008

Taq RNA polymerase-rifampicin complex

OverviewOverview

A combined structural, functional, and genetic approach was used to investigate inhibition of bacterial RNA polymerase (RNAP) by sorangicin (Sor), a macrolide polyether antibiotic. Sor lacks chemical and structural similarity to the ansamycin rifampicin (Rif), an RNAP inhibitor widely used to treat tuberculosis. Nevertheless, structural analysis revealed Sor binds in the same RNAP beta subunit pocket as Rif, with almost complete overlap of RNAP binding determinants, and functional analysis revealed that both antibiotics inhibit transcription by directly blocking the path of the elongating transcript at a length of 2-3 nucleotides. Genetic analysis indicates that Rif binding is extremely sensitive to mutations expected to change the shape of the antibiotic binding pocket, while Sor is not. We suggest that conformational flexibility of Sor, in contrast to the rigid conformation of Rif, allows Sor to adapt to changes in the binding pocket. This has important implications for drug design against rapidly mutating targets.

About this StructureAbout this Structure

1YNN is a Protein complex structure of sequences from Thermus aquaticus. Full crystallographic information is available from OCA.

ReferenceReference

Structural, functional, and genetic analysis of sorangicin inhibition of bacterial RNA polymerase., Campbell EA, Pavlova O, Zenkin N, Leon F, Irschik H, Jansen R, Severinov K, Darst SA, EMBO J. 2005 Feb 23;24(4):674-82. Epub 2005 Feb 3. PMID:15692574 Page seeded by OCA on Sat May 3 16:33:09 2008

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OCA

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 [[Image:1ynn.gif|left|200px]]
- {{Structure
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+The line below this paragraph, containing "STRUCTURE_1ynn", creates the "Structure Box" on the page.
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+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=RFP:RIFAMPICIN'>RFP</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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-|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/DNA-directed_RNA_polymerase DNA-directed RNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.6 2.7.7.6] </span>
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-|GENE=
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-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ynn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ynn OCA], [http://www.ebi.ac.uk/pdbsum/1ynn PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ynn RCSB]</span>
-}}
 '''Taq RNA polymerase-rifampicin complex'''
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 [[Category: Severinov, K.]]
 [[Category: Zenkin, N.]]
-[[Category: rifampicin]]
+[[Category: Rifampicin]]
-[[Category: rna polymerase]]
+[[Category: Rna polymerase]]
-[[Category: transferase]]
+[[Category: Transferase]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 16:33:09 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:14:34 2008''