Table 1.
Ability of TG and its analogues to inhibit SERCA pump, increase intracellular free calcium, decrease AR protein, and induce cell death of LNCaP cells
| Analog | Amino acid | SEARCA pump inhibition | Intracellular free calcium | AR | Cell death of LNCaP |
|---|---|---|---|---|---|
| IC50 | (nmol/L)* | Protein† | LC50‡ | ||
| (nmol/L) | (% of control) | (nmol/L) | |||
| TG | None | 13 ± 2 | 441 ± 35 | 10 ± 2 | 10 ± 5 |
| 12ADT | None | 35 ± 4 | 369 ± 23 | 14 ± 3 | 55 ± 12 |
| A12ADT | Alanine | 17 ± 2 | 410 ± 45 | 15 ± 4 | 8 ± 4 |
| D12ADT | Aspartate | 18 ± 2 | 385 ± 40 | 11 ± 6 | 40 ± 12 |
| L12ADT | Leucine | 45 ± 3 | 414 ± 44 | 8 ± 4 | 14 ± 8 |
NOTE: Values are the mean of a minimum of three independent experiments ± SE.
Abbreviations: A-12ADT, alanyl-12ADT; D-12ADT, asparty-12ADT; L-12DT, leucyl-12ADT.
After 10 min after exposure to 1 µmol/L TG, starting concentration was ~40 nmol/L.
After 24 h of exposure to 1 µmol/L TG of LNCap cells.
After 48 h of exposure to TG.