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. Author manuscript; available in PMC: 2009 Jun 9.
Published in final edited form as: Ann N Y Acad Sci. 2009 Feb;1155:99–111. doi: 10.1111/j.1749-6632.2009.04114.x

Figure 3.

Figure 3

Competitive binding assay of TAM and metabolites of TAM. The cytosolic fraction of MCF-7 cells was incubated (500 μL total reaction) for 18 h at 4°C with the indicated concentration of competitor (10−9 to 10−6 M) or [3H]-labeled E2 (10−11 to 10−6 M). After incubation, 5% dextran-coated charcoal was added to adsorb unbound ligand for 15 min at 4°C, and radioactivity was measured in the supernatant. Data are expressed as the percentage of specific binding of [3H]-E2 for the ER when competitor was not present. Numbers in parentheses, RBA to ER for each test compound, with all data normalized to the RBA of E2 (set at 100). (A) T4, trans-4-OH-TAM; T4O, trans-TAM-4-O-glucuronide, T4N, trans-4-OH-TAM-N-glucuronide; (B) C4, cis-4-OH-TAM; C4O, cis-TAM-4-O-glucuronide; C4N, cis-4-OH-TAM-N-glucuronide; (C) TE, trans-endoxifen; TEO, trans-endoxifen-O- glucuronide; CE, cis-endoxifen; CEO, cis-endoxifen-O-glucuronide; (D) TN, TAM-N-glucuronide.

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