1u3r

From Proteopedia

proteopedia linkproteopedia link

Template:STRUCTURE 1u3r

Contents 1 Crystal Structure of Estrogen Receptor beta complexed with WAY-338 2 Function 3 About this Structure 4 See Also 5 Reference

Crystal Structure of Estrogen Receptor beta complexed with WAY-338

Template:ABSTRACT PUBMED 15456246

Function

[ESR2_HUMAN] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.

About this Structure

1u3r is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

• Estrogen receptor

Reference

• Malamas MS, Manas ES, McDevitt RE, Gunawan I, Xu ZB, Collini MD, Miller CP, Dinh T, Henderson RA, Keith JC Jr, Harris HA. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. J Med Chem. 2004 Oct 7;47(21):5021-40. PMID:15456246 doi:10.1021/jm049719y