5T92
ESTROGEN RECEPTOR ALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH (2E)-3-{4-[(1R)-2-(4-fluorophenyl)-6-hydroxy-1-methy l-1,2,3,4- tetrahydroisoquinolin-1-yl]phenyl}prop-2-enoic acid
Summary for 5T92
Entry DOI | 10.2210/pdb5t92/pdb |
Descriptor | Estrogen receptor, (2E)-3-{4-[(1R)-2-(4-fluorophenyl)-6-hydroxy-1-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl]phenyl}prop-2-enoic acid (3 entities in total) |
Functional Keywords | nuclear receptor, protein-ligand complex, hormone receptor |
Biological source | Homo sapiens (Human) |
Cellular location | Isoform 1: Nucleus . Isoform 3: Nucleus. Nucleus: P03372 |
Total number of polymer chains | 2 |
Total formula weight | 58602.64 |
Authors | |
Primary citation | Burks, H.E.,Abrams, T.,Kirby, C.A.,Baird, J.,Fekete, A.,Hamann, L.G.,Kim, S.,Lombardo, F.,Loo, A.,Lubicka, D.,Macchi, K.,McDonnell, D.P.,Mishina, Y.,Norris, J.D.,Nunez, J.,Saran, C.,Sun, Y.,Thomsen, N.M.,Wang, C.,Wang, J.,Peukert, S. Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ER alpha + Breast Cancer. J. Med. Chem., 60:2790-2818, 2017 Cited by PubMed: 28296398DOI: 10.1021/acs.jmedchem.6b01468 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.22 Å) |
Structure validation
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