Novel somatostatin analogs with tyrosine kinase inhibitory and antitumor activity.
A series of new somatostatin analogs have been developed and tested for antitumor activity. Some analogs strongly inhibited tyrosine kinase activity of human colon tumor cells and this activity correlated well with their antiproliferative effect, but did not correlate with GH release inhibition. The best analogs strongly inhibited the metastasis formation in the Lewis lung metastasis model in mice. On the basis of these in vitro and in vivo data we were able to select one analog with strong tyrosine kinase inhibitory and antitumor activity, without inhibiting growth hormone release.
Kéri
G
G
1st Inst. Biochemistry, Joint. Res. Org. of Hung. Acad. Sci. and Semmelweis Med. Univ., Budapest.
Mezö
I
I
Horváth
A
A
Vadász
Z
Z
Balogh
A
A
Idei
M
M
Vántus
T
T
Teplán
I
I
Mák
M
M
Horváth
J
J
D000595:Amino Acid Sequence; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D013006:Growth Hormone / Q000378:metabolism; D013007:Growth Hormone-Releasing Hormone / Q000378:metabolism; D006801:Humans; D008175:Lung Neoplasms / Q000473:pathology; D051379:Mice; D008969:Molecular Sequence Data; D009362:Neoplasm Metastasis; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; C051458:vapreotide; D013004:Somatostatin; D013006:Growth Hormone; D013007:Growth Hormone-Releasing Hormone; D011505:Protein-Tyrosine Kinases