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PDBsum entry 1qaq
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Contents |
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* Residue conservation analysis
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References listed in PDB file
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Key reference
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Title
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The 2.2 a structure of the rrna methyltransferase ermc' And its complexes with cofactor and cofactor analogs: implications for the reaction mechanism.
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Authors
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G.Schluckebier,
P.Zhong,
K.D.Stewart,
T.J.Kavanaugh,
C.Abad-Zapatero.
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Ref.
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J Mol Biol, 1999,
289,
277-291.
[DOI no: ]
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PubMed id
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Abstract
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The rRNA methyltransferase ErmC' transfers methyl groups from S
-adenosyl-l-methionine to atom N6 of an adenine base within the
peptidyltransferase loop of 23 S rRNA, thus conferring antibiotic resistance
against a number of macrolide antibiotics. The crystal structures of ErmC' and
of its complexes with the cofactor S -adenosyl-l-methionine, the reaction
product S-adenosyl-l-homocysteine and the methyltransferase inhibitor
Sinefungin, respectively, show that the enzyme undergoes small conformational
changes upon ligand binding. Overall, the ligand molecules bind to the protein
in a similar mode as observed for other methyltransferases. Small differences
between the binding of the amino acid parts of the different ligands are
correlated with differences in their chemical structure. A model for the
transition-state based on the atomic details of the active site is consistent
with a one-step methyl-transfer mechanism and might serve as a first step
towards the design of potent Erm inhibitors.
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Figure 3.
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Figure 4.
Figure 4. Comparison of the AdoMet conformation when bound to
different AdoMet-dependent MTases: M. TaqI (blue, PDB entry
2ADM; [Schluckebier et al 1998]), catechol-O-MTase (red, 1VID;
[Vidgren et al 1994]), RNA-O2′-MTase VP39 (green, 1VPT; [Hodel
et al 1996]) and ErmC′ (this work). AdoMet was superimposed at
the adenine rings. Prepared with QUANTA.
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The above figures are
reprinted
by permission from Elsevier:
J Mol Biol
(1999,
289,
277-291)
copyright 1999.
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Secondary reference #1
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Title
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Crystal structure of ermc', An rrna methyltransferase which mediates antibiotic resistance in bacteria.
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Authors
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D.E.Bussiere,
S.W.Muchmore,
C.G.Dealwis,
G.Schluckebier,
V.L.Nienaber,
R.P.Edalji,
K.A.Walter,
U.S.Ladror,
T.F.Holzman,
C.Abad-Zapatero.
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Ref.
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Biochemistry, 1998,
37,
7103-7112.
[DOI no: ]
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PubMed id
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