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PDBsum entry 2cw0
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229 a.a.
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1119 a.a.
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1392 a.a.
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95 a.a.
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345 a.a.
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References listed in PDB file
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Key reference
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Title
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Inhibition of bacterial RNA polymerase by streptolydigin: stabilization of a straight-Bridge-Helix active-Center conformation.
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Authors
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S.Tuske,
S.G.Sarafianos,
X.Wang,
B.Hudson,
E.Sineva,
J.Mukhopadhyay,
J.J.Birktoft,
O.Leroy,
S.Ismail,
A.D.Clark,
C.Dharia,
A.Napoli,
O.Laptenko,
J.Lee,
S.Borukhov,
R.H.Ebright,
E.Arnold.
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Ref.
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Cell, 2005,
122,
541-552.
[DOI no: ]
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PubMed id
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Abstract
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We define the target, mechanism, and structural basis of inhibition of bacterial
RNA polymerase (RNAP) by the tetramic acid antibiotic streptolydigin (Stl). Stl
binds to a site adjacent to but not overlapping the RNAP active center and
stabilizes an RNAP-active-center conformational state with a straight-bridge
helix. The results provide direct support for the proposals that alternative
straight-bridge-helix and bent-bridge-helix RNAP-active-center conformations
exist and that cycling between straight-bridge-helix and bent-bridge-helix
RNAP-active-center conformations is required for RNAP function. The results set
bounds on models for RNAP function and suggest strategies for design of novel
antibacterial agents.
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Figure 1.
Figure 1. Target of Stl
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Figure 5.
Figure 5. Structural Basis of Inhibition by Stl:
Stabilization of Straight-Bridge-Helix Active-Center Conformation
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The above figures are
reprinted
by permission from Cell Press:
Cell
(2005,
122,
541-552)
copyright 2005.
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