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PDBsum entry 2i0j
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Transcription
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PDB id
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2i0j
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References listed in PDB file
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Key reference
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Title
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Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.
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Authors
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B.H.Norman,
J.A.Dodge,
T.I.Richardson,
P.S.Borromeo,
C.W.Lugar,
S.A.Jones,
K.Chen,
Y.Wang,
G.L.Durst,
R.J.Barr,
C.Montrose-Rafizadeh,
H.E.Osborne,
R.M.Amos,
S.Guo,
A.Boodhoo,
V.Krishnan.
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Ref.
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J Med Chem, 2006,
49,
6155-6157.
[DOI no: ]
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PubMed id
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Abstract
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Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent,
selective binding and agonist function in estrogen receptor beta (ERbeta) in
vitro assays. X-ray crystal structures of SERBA-1 in ERalpha and beta help
explain observed beta-selectivity of this ligand. SERBA-1 in vivo demonstrates
involution of the ventral prostate in CD-1 mice (ERbeta effect), while having no
effect on gonadal hormone levels (ERalpha effect) at 10x the efficacious dose,
consistent with in vitro properties of this molecule.
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