Author/Authors :
Hohla، نويسنده , , Florian and Buchholz، نويسنده , , Stefan and Schally، نويسنده , , Andrew V. and Krishan، نويسنده , , Awtar and Rick، نويسنده , , Ferenc G. and Szalontay، نويسنده , , Luca and Papadia، نويسنده , , Andrea and Halmos، نويسنده , , Gabor and Koster، نويسنده , , Frank and Aigner، نويسنده , , Elmar and Datz، نويسنده , , Christian and Seitz، نويسنده , , Stephan، نويسنده ,
Abstract :
The effect of the targeted cytotoxic somatostatin (SST) analog AN-162, consisting of doxorubicin (DOX) conjugated to SST carrier RC-121, was investigated on the growth of human colorectal cancer (CRC) cell lines HT-29, HCT-15, and HCT-116 and a DOX-resistant mouse leukemia cell line P388/R84. mRNA for SST-receptors and high affinity binding sites for SST were detected in all CRC cell lines and in P388/R84 cells. In contrast to DOX alone, AN-162 blocked HCT-116 cells and P388/R84 cells in S/G2 phase and increased the number of apoptotic cells. In vivo, AN-162 reduced the volume of CRC xenografts more effectively than its unconjugated components. Our results suggest that AN-162 inhibits growth of experimental CRC more effectively than DOX and increases sensitivity of DOX resistant human leukemia cells.
Keywords :
Targeted therapy , AN-162 , Colon cancer , Somatostatin , doxorubicin