Estrogen receptor ligands
AssigneeKara Bio AB
InventorsJan Ljunggren, Ann-Gerd Thorsell, Owe Engstrom, Tomas Bonn, Mats Carlquist, Andrzeji Brzozowski, Ashley Pike, Roderick Hubbard
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Abstract
The present invention is directed to crystals of ERβ ligand binding domain complexed with (1) N-(n-butyl)-11-[3,17β-dihydroxyestra-1,3,5(10)-trien-7α-yl]N-methylundecanamide; estradiol and a peptide comprising the amino acid sequence LXXLL; or 17-epiestriol and a peptide comprising the amino acid sequence LXXLL.
Claims9
A crystal of ERβ ligand binding domain of SEQ ID NO:2 complexed with N-(n-butyl)-11-[3,17β-dihydroxyestra-1,3,5(10)-trien-7α-yl]N-methylundecanamide, said crystal belonging to the space group I212121 and having unit cell dimensions a=59.37 Å, b=81.4 Å, c=520.97 Å, and containing five ligand binding domain monomers per asymmetric unit.
A crystal of ERβ ligand binding domain of SEQ ID NO:2 complexed with estradiol and a peptide comprising the amino acid sequence of SEQ ID NO:3, said crystal belonging to the space group P4122 and having the unit cell dimensions a=62.55 Å, b=62.55 Å, c=171.70 Å.
A crystal of ERβ ligand binding domain SEQ ID NO:2 complexed with 17-epiestriol and a peptide comprising the amino acid sequence of SEQ ID NO:3, said crystal belonging to the space group P4122 and having the unit cell dimensions a=62.64 Å, b=62.64 Å, c=171.64 Å.
Dependencies are inferred from the claim text.