1HJ1

RAT OESTROGEN RECEPTOR BETA LIGAND-BINDING DOMAIN IN COMPLEX WITH PURE ANTIOESTROGEN ICI164,384

Summary for 1HJ1

• Entry DOI: 10.2210/pdb1hj1/pdb
• Related: 1QKN
• Descriptor: OESTROGEN RECEPTOR BETA, N-BUTYL-11-[(7R,8R,9S,13S,14S,17S)-3,17-DIHYDROXY-13-METHYL-7,8,9,11,12,13,14,15,16,17-DECAHYDRO-6H-CYCLOPENTA[A]PHENANTHREN-7-YL]-N-METHYLUNDECANAMIDE, PARA-MERCURY-BENZENESULFONIC ACID, ... (5 entities in total)
• Functional Keywords: nuclear receptor, transcription factor, oestrogen, antagonist
• Biological source: RATTUS NORVEGICUS (NORWAY RAT)
• Total number of polymer chains: 1
• Total formula weight: 29686.95

Authors

Pike, A.C.W.,Brzozowski, A.M.,Carlquist, M. (deposition date: 2001-01-08, release date: 2002-01-04, Last modification date: 2023-12-13)

Primary citation

Pike, A.C.W.,Brzozowski, A.M.,Walton, J.,Hubbard, R.E.,Thorsell, A.G.,Li, Y.L.,Gustafsson, J.A.,Carlquist, M.
Structural Insights Into the Mode of Action of a Pure Antiestrogen
Structure, 9:145-, 2001

PubMed Abstract: Estrogens exert their effects on target tissues by binding to a nuclear transcription factor termed the estrogen receptor (ER). Previous structural studies have demonstrated that each class of ER ligand (agonist, partial agonist, and SERM antagonist) induces distinctive orientations in the receptor's carboxy-terminal transactivation helix. The conformation of this portion of the receptor determines whether ER can recruit and interact with the components of the transcriptional machinery, thereby facilitating target gene expression.

PubMed: 11250199
DOI: 10.1016/S0969-2126(01)00568-8

Experimental method

X-RAY DIFFRACTION (2.3 Å)