Abstract
213Bi-PAI2 conjugate selectively induces apoptosis in PC3 metastatic prostate cancer cell line and shows anti-cancer activity in a xenograft animal model
Highlights
A-particle therapy has been proposed for use in single-cell disorders such as leukaemias, lymphoma and micrometastatic carcinomas (Jurcic et al, 1997; McDevitt et al, 1998; Allen, 1999; Kennel et al, 1999), in which rapid targeting to cancer cells is possible
We show that 213Bi-PAI2 was cytotoxic to PC3 cells in a concentration-dependent fashion, causing the cells to undergo apoptosis in vitro, whereas a therapeutic dose of 213BiPAI2 obviously regressed tumour growth and prevented metastases in the lymph nodes in animal models
The results showed that the uPA histogram has a strong shift to the right compared with the negative and isotype controls, suggesting that uPA is expressed on the cell surface and provides a good target for 213Bi-PAI2 conjugate in vitro
Summary
A-particle therapy has been proposed for use in single-cell disorders such as leukaemias, lymphoma and micrometastatic carcinomas (Jurcic et al, 1997; McDevitt et al, 1998; Allen, 1999; Kennel et al, 1999), in which rapid targeting to cancer cells is possible. The radionuclide 213Bi (t1⁄2=46 min) emits an a-particle with short range (80 mm) and high linear energy transfer (LET) radiation which is about 100 times greater than that for beta particles (Allen and Blagojevic, 1997). This is manifested by a high relative biological effectiveness (RBE). We show that 213Bi-PAI2 was cytotoxic to PC3 cells in a concentration-dependent fashion, causing the cells to undergo apoptosis in vitro, whereas a therapeutic dose of 213BiPAI2 obviously regressed tumour growth and prevented metastases in the lymph nodes in animal models
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