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2giu

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2giu, resolution 2.20Å ()
Ligands:
Gene: ESR2 (Homo sapiens)
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Contents

Human estrogen receptor beta ligand-binding domain in complex with compound 45

Publication Abstract from PubMed

Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.

The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands., Wilkening RR, Ratcliffe RW, Tynebor EC, Wildonger KJ, Fried AK, Hammond ML, Mosley RT, Fitzgerald PM, Sharma N, McKeever BM, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin ET, Wilkinson HA, Mitra S, Cai S, Hayes EC, Schaeffer JM, Rohrer SP, Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2. PMID:16632357

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

2giu is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Wilkening RR, Ratcliffe RW, Tynebor EC, Wildonger KJ, Fried AK, Hammond ML, Mosley RT, Fitzgerald PM, Sharma N, McKeever BM, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin ET, Wilkinson HA, Mitra S, Cai S, Hayes EC, Schaeffer JM, Rohrer SP. The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2. PMID:16632357 doi:10.1016/j.bmcl.2006.03.098

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