Inhibition of rat prostate tumor growth by an octapeptide analog of somatostatin.
Analogs of a potent octapeptide analog of somatostatin (SRIF) H-(D)Phe-Cys-Tyr-(D)Trp-Lys-Val-Cys-Thr(NH2) were synthesized. Aromatic substitutions for Tyr resulted in little change in inhibitory potency on growth hormone (GH) secretion in the rat. Substitutions for Val or (D)Trp resulted in analogs with diminished activity. Substitution of (D)Nal for (D)Phe increased duration of GH inhibition. Final weights of subcutaneously implanted prostate tumors (R3327) were 41% lower in rats treated with an N-terminal 4-chloro-(D)phenylalanyl analog as compared to vehicle treated controls. The analog had no effect on testicular weight or final plasma testosterone levels. SRIF analogs may represent an alternative treatment for prostate cancer that would be free of the untoward reproductive effects of other treatments (e.g. LH-RH or castration).
D000818:Animals; D005934:Glucagon / Q000378:metabolism; D013006:Growth Hormone / Q000378:metabolism; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D008297:Male; D009842:Oligopeptides / Q000138:chemical synthesis; D009929:Organ Size / Q000187:drug effects; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D051381:Rats; D012636:Secretory Rate / Q000187:drug effects; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D013739:Testosterone / Q000097:blood
D007328:Insulin; D009842:Oligopeptides; D013739:Testosterone; D013004:Somatostatin; D013006:Growth Hormone; D005934:Glucagon