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PDBsum entry 1qkn
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Nuclear receptor
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PDB id
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1qkn
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Contents |
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* Residue conservation analysis
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DOI no:
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EMBO J
18:4608-4618
(1999)
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PubMed id:
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Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist.
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A.C.Pike,
A.M.Brzozowski,
R.E.Hubbard,
T.Bonn,
A.G.Thorsell,
O.Engström,
J.Ljunggren,
J.A.Gustafsson,
M.Carlquist.
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ABSTRACT
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Oestrogens exert their physiological effects through two receptor subtypes. Here
we report the three-dimensional structure of the oestrogen receptor beta isoform
(ERbeta) ligand-binding domain (LBD) in the presence of the phyto-oestrogen
genistein and the antagonist raloxifene. The overall structure of ERbeta-LBD is
very similar to that previously reported for ERalpha. Each ligand interacts with
a unique set of residues within the hormone-binding cavity and induces a
distinct orientation in the AF-2 helix (H12). The bulky side chain of raloxifene
protrudes from the cavity and physically prevents the alignment of H12 over the
bound ligand. In contrast, genistein is completely buried within the hydrophobic
core of the protein and binds in a manner similar to that observed for ER's
endogenous hormone, 17beta-oestradiol. However, in the ERbeta-genistein complex,
H12 does not adopt the distinctive 'agonist' position but, instead, lies in a
similar orientation to that induced by ER antagonists. Such a sub-optimal
alignment of the transactivation helix is consistent with genistein's partial
agonist character in ERbeta and demonstrates how ER's transcriptional response
to certain bound ligands is attenuated.
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Selected figure(s)
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Figure 3.
Figure 3 Chemical structures of (A) GEN and (B) RAL showing the
atom numbering scheme and ring nomenclature used in the text.
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Figure 5.
Figure 5 (A) Schematic representation showing the interactions
between RAL and rER  -LBD.
Distance cut-offs and colouring used are as in Figure 4A. (B)
Comparison of the ligand-binding mode of GEN (protein, light
blue; ligand, green) and RAL (protein, red; ligand, purple)
within the rER -LBD
binding cavity. Solid arrows highlight concerted shifts in the
framework of the cavity that accompany the binding of RAL. The
binding cavity is viewed in the same orientation as in Figure 4C.
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The above figures are
reprinted
from an Open Access publication published by Macmillan Publishers Ltd:
EMBO J
(1999,
18,
4608-4618)
copyright 1999.
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Figures were
selected
by an automated process.
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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PDB codes:
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PDB code:
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PDB code:
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IUBMB Life,
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PDB code:
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| |
J Biol Chem,
282,
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PDB code:
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E.A.Hillard,
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| |
Dalton Trans,
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F.F.Vajdos,
L.R.Hoth,
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and
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(2007).
The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene.
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| |
Protein Sci,
16,
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PDB code:
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G.Pochetti,
C.Godio,
N.Mitro,
D.Caruso,
A.Galmozzi,
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P.Tortorella,
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and
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(2007).
Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
|
| |
J Biol Chem,
282,
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|
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PDB codes:
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H.B.Zhou,
K.W.Nettles,
J.B.Bruning,
Y.Kim,
A.Joachimiak,
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and
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(2007).
Elemental isomerism: a boron-nitrogen surrogate for a carbon-carbon double bond increases the chemical diversity of estrogen receptor ligands.
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J Biol Chem,
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C.Stehlin-Gaon,
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All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
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PDB codes:
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E.Diamanti-Kandarakis,
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Interaction of organophosphate pesticides and related compounds with the androgen receptor.
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Environ Health Perspect,
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Estrogenic compounds suppressed interferon-gamma production in mouse splenocytes through direct cell-cell interaction.
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In Vitro Cell Dev Biol Anim,
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Discovery of diverse thyroid hormone receptor antagonists by high-throughput docking.
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Proc Natl Acad Sci U S A,
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Synthesis, receptor binding, molecular modeling, and proliferative assays of a series of 17alpha-arylestradiols.
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Chembiochem,
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Nucl Recept,
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J Biol Chem,
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Clin Endocrinol (Oxf),
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J Biol Chem,
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J Biol Chem,
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Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism.
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Nat Struct Biol,
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PDB codes:
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A.Ohno,
M.Shimizu,
and
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(2002).
Fluorinated vitamin D analogs to probe the conformation of vitamin D in its receptor complex: 19F-NMR studies and biological activity.
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Chem Pharm Bull (Tokyo),
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A.Wärnmark,
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Interaction of transcriptional intermediary factor 2 nuclear receptor box peptides with the coactivator binding site of estrogen receptor alpha.
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J Biol Chem,
277,
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PDB codes:
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J.D.Love,
J.T.Gooch,
S.Benko,
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L.Nagy,
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The structural basis for the specificity of retinoid-X receptor-selective agonists: new insights into the role of helix H12.
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J Biol Chem,
277,
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PDB code:
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K.Morito,
T.Aomori,
T.Hirose,
J.Kinjo,
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Interaction of phytoestrogens with estrogen receptors alpha and beta (II).
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Biol Pharm Bull,
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K.Steketee,
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Broadened ligand responsiveness of androgen receptor mutants obtained by random amino acid substitution of H874 and mutation hot spot T877 in prostate cancer.
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Int J Cancer,
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S.H.Safe,
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Problems for risk assessment of endocrine-active estrogenic compounds.
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Environ Health Perspect,
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Y.Dobrydneva,
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G.Z.Morris,
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Dietary phytoestrogens and their synthetic structural analogues as calcium channel blockers in human platelets.
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J Cardiovasc Pharmacol,
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Y.Jacquot,
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A.Boulahdour,
L.Bermont,
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Pharmacological profile of 6,12-dihydro-3-methoxy-1-benzopyrano[3,4-b] [1,4]benzothiazin-6-one, a novel human estrogen receptor agonist.
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Biol Pharm Bull,
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J.A.Gustafsson,
and
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(2001).
Structural insights into the mode of action of a pure antiestrogen.
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| |
Structure,
9,
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PDB code:
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|
A.C.Steinmetz,
J.P.Renaud,
and
D.Moras
(2001).
Binding of ligands and activation of transcription by nuclear receptors.
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Annu Rev Biophys Biomol Struct,
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C.M.Klinge
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Estrogen receptor interaction with estrogen response elements.
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Nucleic Acids Res,
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C.Wang,
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S.E.Kiefer,
Y.An,
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Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone.
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Proc Natl Acad Sci U S A,
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PDB codes:
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|
|
K.Morito,
T.Hirose,
J.Kinjo,
T.Hirakawa,
M.Okawa,
T.Nohara,
S.Ogawa,
S.Inoue,
M.Muramatsu,
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(2001).
Interaction of phytoestrogens with estrogen receptors alpha and beta.
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Biol Pharm Bull,
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Role of estrogen receptor beta in estrogen action.
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Annu Rev Physiol,
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L.Gaughan,
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D.E.Neal,
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Tip60 is a co-activator specific for class I nuclear hormone receptors.
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J Biol Chem,
276,
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M.A.Iannone,
T.G.Consler,
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D.J.Parks,
and
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Multiplexed molecular interactions of nuclear receptors using fluorescent microspheres.
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Cytometry,
44,
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N.Greenfield,
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M.A.Gallo,
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(2001).
Increase in the stability and helical content of estrogen receptor alpha in the presence of the estrogen response element: analysis by circular dichroism spectroscopy.
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Biochemistry,
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N.M.Brown,
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Animal models impacted by phytoestrogens in commercial chow: implications for pathways influenced by hormones.
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Lab Invest,
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Estrogen receptor and breast cancer.
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Semin Cancer Biol,
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M.Gangloff,
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Different ligands-different receptor conformations: modeling of the hER alpha LBD in complex with agonists and antagonists.
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Med Res Rev,
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Estrogen receptor transcription and transactivation: Estrogen receptor alpha and estrogen receptor beta: regulation by selective estrogen receptor modulators and importance in breast cancer.
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Breast Cancer Res,
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Crystal structure of human sex hormone-binding globulin: steroid transport by a laminin G-like domain.
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EMBO J,
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PDB code:
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J.A.Gustafsson
(2000).
New insights in oestrogen receptor (ER) research - the ERbeta.
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Eur J Cancer,
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M.Ruff,
M.Gangloff,
J.M.Wurtz,
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Estrogen receptor transcription and transactivation: Structure-function relationship in DNA- and ligand-binding domains of estrogen receptors.
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Breast Cancer Res,
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Estrogen receptor transcription and transactivation: Basic aspects of estrogen action.
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Curr Opin Obstet Gynecol,
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Selective estrogen receptor modulators in reproductive medicine and biology.
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Obstet Gynecol Surv,
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W.Bourguet,
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Nuclear receptor ligand-binding domains: three-dimensional structures, molecular interactions and pharmacological implications.
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Trends Pharmacol Sci,
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W.Bourguet,
V.Vivat,
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H.Gronemeyer,
and
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(2000).
Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains.
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| |
Mol Cell,
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PDB code:
|
|
|
|
|
|
|
|
A.Mueller-Fahrnow,
and
U.Egner
(1999).
Ligand-binding domain of estrogen receptors.
|
| |
Curr Opin Biotechnol,
10,
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|
|
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|
|
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.
Where a reference describes a PDB structure, the PDB
code is
shown on the right.
|
|
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