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Table 1 Ligand-binding affinities for WT and mutant ERα LBDs

From: Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer

  Ki±SD, nM (fold change over WT)
Ligand WT Y537S D538G
17β-Estradiola,b 0.22±0.11 1.40±0.54 (6.36) 1.77±0.66 (8.05)
Lasofoxifene 0.21±0.06 2.34±0.60 (11.14) 2.19±0.24 (10.43)
4-Hydroxytamoxifen 0.12±0.003 2.64±0.40 (22.00) 2.29±0.80 (19.08)
Fulvestrantb 0.13±0.03 3.68±0.77 (28.31) 5.06±1.16 (38.92)
  1. LBD, ligand binding domain; SD, standard deviation; WT, wild type
  2. aAffinity was expressed as Kd (nM) for 17β-Estradiol
  3. bPreviously published data from Zhao et al. [14]