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  • Increased binding to sigma sites of N-[1′(2-piperidinyl)ethyl)-4-[I-125]-iodobenzamide (I-125-PAB) with onset of tumor cell proliferation
  • Add time:08/25/2019         Source:sciencedirect.com

    This study evaluated if the density of sigma sites was modulated following stimulation of mitosis and progression through the cell cycle. The sigma ligand N-[1′(2-piperidinyl)ethyl)-4-[I-125]-iodobenzamide (I-125-PAB) was a binding probe on the mammary tumor cell lines T47D and MCF-7, and the prostate tumor cell line DU-145. Cells at low density and in log phase growth bound more I-125-IPAB than those at high density at or the near plateau phase. Stimulation of mitosis with insulin or fresh 10% serum increased I-125-IPAB binding in all three cell lines. In cell-cycle synchronized cells, the highest amount of binding was found in cells treated with colcemid to block cells in the M-phase, while the lowest amount of binding was found in cells treated with low serum to block the cells in G1. Cells treated with aphidicolin to block cells at G1/S also bound less than cells block in the M-phase. Collectively, these results support a direct correlation between I-125-PAB binding and proliferative status, and suggest an up-regulation of sigma binding sites prior to mitosis.

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