 |
PDBsum entry 3cxc
|
|
|
|
 |
Contents |
 |
|
|
|
|
|
|
|
|
|
237 a.a.
|
 |
|
|
|
|
|
|
|
337 a.a.
|
 |
|
|
|
|
|
|
|
246 a.a.
|
 |
|
|
|
|
|
|
|
140 a.a.
|
 |
|
|
|
|
|
|
|
172 a.a.
|
 |
|
|
|
|
|
|
|
119 a.a.
|
 |
|
|
|
|
|
|
|
29 a.a.
|
 |
|
|
|
|
|
|
|
156 a.a.
|
 |
|
|
|
|
|
|
|
142 a.a.
|
 |
|
|
|
|
|
|
|
132 a.a.
|
 |
|
|
|
|
|
|
|
145 a.a.
|
 |
|
|
|
|
|
|
|
194 a.a.
|
 |
|
|
|
|
|
|
|
186 a.a.
|
 |
|
|
|
|
|
|
|
115 a.a.
|
 |
|
|
|
|
|
|
|
143 a.a.
|
 |
|
|
|
|
|
|
|
95 a.a.
|
 |
|
|
|
|
|
|
|
150 a.a.
|
 |
|
|
|
|
|
|
|
81 a.a.
|
 |
|
|
|
|
|
|
|
119 a.a.
|
 |
|
|
|
|
|
|
|
53 a.a.
|
 |
|
|
|
|
|
|
|
65 a.a.
|
 |
|
|
|
|
|
|
|
154 a.a.
|
 |
|
|
|
|
|
|
|
82 a.a.
|
 |
|
|
|
|
|
|
|
142 a.a.
|
 |
|
|
|
|
|
|
|
73 a.a.
|
 |
|
|
|
|
|
|
|
56 a.a.
|
 |
|
|
|
|
|
|
|
46 a.a.
|
 |
|
|
|
|
|
|
|
92 a.a.
|
 |
|
|
|
|
|
|
|
|
|
|
|
|
_CL
×22
|
 |
|
|
|
|
|
|
|
_NA
×86
|
 |
|
|
|
|
|
|
|
_MG
×117
|
 |
|
|
|
|
|
|
|
_CD
×5
|
 |
|
|
|
|
|
|
|
__K
×2
|
 |
|
|
|
|
|
|
* Residue conservation analysis
|
|
|
|
|
PDB id:
|
 |
|
 |
| Name: |
 |
Ribosome
|
 |
|
Title:
|
 |
The structure of an enhanced oxazolidinone inhibitor bound to the 50s ribosomal subunit of h. Marismortui
|
|
Structure:
|
 |
23s ribosomal RNA. Chain: 0. 5s ribosomal RNA. Chain: 9. 5'-r( Cp Cp A)-3'. Chain: 4. Engineered: yes. Ribosomal protein l2. Chain: a.
|
|
Source:
|
 |
Haloarcula marismortui. Organism_taxid: 2238. Synthetic: yes. Organism_taxid: 2238
|
|
Resolution:
|
 |
|
3.00Å
|
R-factor:
|
0.186
|
R-free:
|
0.229
|
|
|
Authors:
|
 |
J.A.Ippolito,D.Wang,Z.F.Kanyo,E.M.Duffy
|
|
Key ref:
|
 |
J.Zhou
et al.
(2008).
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
Bioorg Med Chem Lett,
18,
6175-6178.
PubMed id:
|
 |
|
Date:
|
 |
|
24-Apr-08
|
Release date:
|
28-Apr-09
|
|
|
|
|
|
PROCHECK
|
|
|
|
|
Headers
|
 |
|
|
References
|
|
|
|
|
|
|
P20276
(RL2_HALMA) -
Large ribosomal subunit protein uL2 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
240 a.a.
237 a.a.*
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P20279
(RL3_HALMA) -
Large ribosomal subunit protein uL3 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
338 a.a.
337 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P12735
(RL4_HALMA) -
Large ribosomal subunit protein uL4 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
246 a.a.
246 a.a.*
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P14124
(RL5_HALMA) -
Large ribosomal subunit protein uL5 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
177 a.a.
140 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P14135
(RL6_HALMA) -
Large ribosomal subunit protein uL6 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
178 a.a.
172 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P12743
(RL7A_HALMA) -
Large ribosomal subunit protein eL8 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
120 a.a.
119 a.a.*
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P15825
(RL10_HALMA) -
Large ribosomal subunit protein uL10 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
348 a.a.
29 a.a.*
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
No UniProt id for this chain
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P29198
(RL13_HALMA) -
Large ribosomal subunit protein uL13 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
145 a.a.
142 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P22450
(RL14_HALMA) -
Large ribosomal subunit protein uL14 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
132 a.a.
132 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P12737
(RL15_HALMA) -
Large ribosomal subunit protein uL15 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
165 a.a.
145 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
No UniProt id for this chain
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P14123
(RL18_HALMA) -
Large ribosomal subunit protein uL18 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
187 a.a.
186 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P12733
(RL18E_HALMA) -
Large ribosomal subunit protein eL18 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
116 a.a.
115 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P14119
(RL19E_HALMA) -
Large ribosomal subunit protein eL19 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
149 a.a.
143 a.a.*
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P12734
(RL21_HALMA) -
Large ribosomal subunit protein eL21 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
96 a.a.
95 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P10970
(RL22_HALMA) -
Large ribosomal subunit protein uL22 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
155 a.a.
150 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P12732
(RL23_HALMA) -
Large ribosomal subunit protein uL23 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
85 a.a.
81 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P10972
(RL24_HALMA) -
Large ribosomal subunit protein uL24 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
120 a.a.
119 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P14116
(RL24E_HALMA) -
Large ribosomal subunit protein eL24 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
67 a.a.
53 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P10971
(RL29_HALMA) -
Large ribosomal subunit protein uL29 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
71 a.a.
65 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P14121
(RL30_HALMA) -
Large ribosomal subunit protein uL30 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
154 a.a.
154 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P18138
(RL31_HALMA) -
Large ribosomal subunit protein eL31 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
92 a.a.
82 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P12736
(RL32_HALMA) -
Large ribosomal subunit protein eL32 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
241 a.a.
142 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
No UniProt id for this chain
|
|
|
|
|
|
|
|
|
 |
 |
|
|
|
|
P32410
(RL37_HALMA) -
Large ribosomal subunit protein eL37 from Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
|
|
|
|
Seq: Struc:
|
 |
 |
 |
57 a.a.
56 a.a.
|
|
|
|
|
|
|
|
|
 |
 |
|
 |
|
|
 |
 |
 |
 |
Enzyme class:
|
 |
Chains A, B, C, D, E, F, G, I, J, K, M, N, O, P, Q, R, S, T, U, V, W, X, Z, 1, 2:
E.C.?
|
|
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
|
|
|
| |
|
|
Bioorg Med Chem Lett
18:6175-6178
(2008)
|
|
PubMed id:
|
|
|
|
|
| |
|
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
|
|
J.Zhou,
A.Bhattacharjee,
S.Chen,
Y.Chen,
E.Duffy,
J.Farmer,
J.Goldberg,
R.Hanselmann,
J.A.Ippolito,
R.Lou,
A.Orbin,
A.Oyelere,
J.Salvino,
D.Springer,
J.Tran,
D.Wang,
Y.Wu,
G.Johnson.
|
|
|
|
| |
ABSTRACT
|
|
|
| |
|
We have developed a first generation of hybrid sparsomycin-linezolid compounds
into a new family of orally bioavailable biaryloxazolidinones that have activity
against both linezolid-susceptible and -resistant gram-positive bacteria as well
as the fastidious gram-negative bacteria Haemophilus influenzae and Moraxella
catarrahalis. The convergent synthesis of these new compounds is detailed.
|
|
|
|
|
|
|
 |
 |
|
 |
 |
 |
 |
 |
 |
 |
 |
 |
|
Literature references that cite this PDB file's key reference
|
|
 |
| |
PubMed id
|
 |
Reference
|
 |
|
|
|
 |
A.R.Renslo
(2010).
Antibacterial oxazolidinones: emerging structure-toxicity relationships.
|
| |
Expert Rev Anti Infect Ther,
8,
565-574.
|
 |
|
|
|
|
 |
H.David-Eden,
A.S.Mankin,
and
Y.Mandel-Gutfreund
(2010).
Structural signatures of antibiotic binding sites on the ribosome.
|
| |
Nucleic Acids Res,
38,
5982-5994.
|
 |
|
|
|
|
 |
S.Lemaire,
P.M.Tulkens,
and
F.Van Bambeke
(2010).
Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils.
|
| |
Antimicrob Agents Chemother,
54,
2540-2548.
|
 |
|
 |
 |
|
The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
|
');
}
}
| | |