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Evaluation of receptors for somatostatin in various tumors using different analogs.
The binding characteristics of several somatostatin (SS-14) analogs developed in our laboratory were examined in various human and animal tumors and normal tissues. In rat cerebral cortex and humanExpand
Synthesis and biological activity of highly potent octapeptide analogs of somatostatin.
In the search for selective and long-acting analogs of somatostatin, nearly 200 compounds were synthesized by solid-phase methods, purified, and tested biologically. Among these octapeptides, someExpand
Inhibition of growth of androgen-independent DU-145 prostate cancer in vivo by luteinising hormone-releasing hormone antagonist Cetrorelix and bombesin antagonists RC-3940-II and RC-3950-II.
The aim of this study was to test the antagonist of LH-RH (Cetrorelix), agonist [D-Trp6]LH-RH (triptorelin) and new bombesin antagonists RC-3940-II and RC-3950-II for their effect on the growth of anExpand
Antagonists of bombesin/gastrin‐releasing peptide inhibit growth of SW‐1990 human pancreatic adenocarcinoma and production of cyclic AMP
We investigated the effects of bombesin/GRP antagonists RC‐3095 and RC‐3940‐II on the growth of SW‐1990 human pancreatic adenocarcinoma cells xenografted into nude mice or cultured in vitro. NudeExpand
Biological Activity and Receptor Binding Characteristics to Various Human Tumors of Acetylated Somatostatin Analogs
Abstract Several somatostatin analogs with recently synthesized acetylated N terminus were assayed In vivo for their effects on sodium pentobarbital-stimuiated growth hormone (GH) levels in fed maleExpand
Synthesis and biological evaluation of cytotoxic analogs of somatostatin containing doxorubicin or its intensely potent derivative, 2-pyrrolinodoxorubicin.
To create cytotoxic hybrid analogs of somatostatin (SST), octapeptides RC-160 (D-Phe-Cys-Tyr-D-Trp- Lys-Val-Cys-Trp-NH2) and RC-121 (D-Phe-Cys-Tyr-D-Trp- Lys-Val-Cys-Thr-NH2) were linked toExpand
The Binding of Bombesin and Somatostatin and Their Analogs to Human Colon Cancers
Abstract Specific receptors for bombesin/gastrin-releasing peptide, somatostatin, and EGF were investigated in 15 human colon cancer specimens. Eight of 15 clinical specimens (15%) of colon cancerExpand
Potent bombesin antagonists with C-terminal Leu-psi(CH2-N)-Tac-NH2 or its derivatives.
Various pseudononapeptide bombesin (BN)-(6-14) antagonists with a reduced peptide bond (CH2-NH) between positions 13 and 14 can suppress the mitogenic activity of BN or gastrin-releasing peptide inExpand
Design, synthesis, and in vitro evaluation of cytotoxic analogs of bombesin-like peptides containing doxorubicin or its intensely potent derivative, 2-pyrrolinodoxorubicin.
Five peptide fragments, based on the C-terminal sequence of bombesin (BN)-(6-14) or BN-(7-14), were selected as carriers for radicals doxorubicin (DOX) and 2-pyrrolino-DOX to create hybrid cytotoxicExpand
Bombesin antagonists inhibit in vitro and in vivo growth of human gastric cancer and binding of bombesin to its receptors
We investigated the effect of bombesin/gastrinreleasing peptide (GRP) antagonist RC-3095 and other analogs on the growth of Hs746T human gastric cancer cells implanted in nude mice or culturedinExpand