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Hypothalamic Hormones and Cancer
Treatment of many cancers remains a major challenge, but new therapeutic modalities are being developed based on antagonists of GH-RH and bombesin, which inhibit growth factors or their receptors, and somatostatin, which can be targeted to receptors for these peptides in various cancers and their metastases.
High incidence of receptors for luteinizing hormone-releasing hormone (LHRH) and LHRH receptor gene expression in human prostate cancers.
The expression of specific receptor proteins for L HRH in human prostate cancer provides a rationale for the improvement in methods for therapy of this malignancy based on LHRH analogs.
Presence of receptors for bombesin/gastrin‐releasing peptide and mRNA for three receptor subtypes in human prostate cancers
Three bombesin receptor subtypes, termed gastrin‐releasing peptide receptor (GRPR), neuromedin B receptor (NMBR), and bombesIn receptor subtype 3 (BRS‐3), have been identified in rodents and humans.
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.
Since Cetrorelix and bombesin antagonists inhibit growth of androgen-independent DU-145 prostate cancers, these compounds could be considered for the therapy of advanced prostate cancer in men, especially after relapse.
Growth inhibition of experimental pancreatic cancers and sustained reduction in epidermal growth factor receptors during therapy with hormonal peptide analogs
The pattern of down-regulation of EGF receptors in pancreatic cancers appears to depend on the peptide used for therapy, and information on the time course of changes in these receptors during treatment with these analogs may lead to an improvement in therapeutic regimens.
Isolation and sequencing of cDNAs for splice variants of growth hormone-releasing hormone receptors from human cancers.
The findings support the view that distinct receptors are expressed on human cancer cells, which may mediate the antiproliferative effect of GHRH antagonists.
Cytotoxic analogs of luteinizing hormone-releasing hormone containing doxorubicin or 2-pyrrolinodoxorubicin, a derivative 500-1000 times more potent.
Doxorubicin (DOX) and its daunosamine-modified derivative, 2-pyrrolino-DOX, which is 500-1000 times more active than DOX, were incorporated into agonistic and antagonistic analogs of luteinizing
The Role of Indoleamine-2,3-Dioxygenase in Cancer Development, Diagnostics, and Therapy
The biochemical role of IDO1 in tumor metabolism and immune surveillance is assessed, and current diagnostic and therapeutic approaches that are intended to increase the effectiveness of immunotherapies against highly aggressive and difficult-to-treat IDO-expressing cancers are reviewed.
Inhibition of growth of MKN45 human gastric‐carcinoma xenografts in nude mice by treatment with bombesin/gastrin‐releasing‐peptide antagonist (RC‐3095) and somatostatin analogue RC‐160
It is demonstrated, for the first time, that the growth of human gastric cancer in nude mice can be inhibited not only by somatostatin analogues, but also by administration of modern bombesin/GRP antagonists, such as RC‐3095.
Inhibition of in vivo proliferation of androgen-independent prostate cancers by an antagonist of growth hormone-releasing hormone.
The results indicate that GH-RH antagonist MZ-4-71 suppresses growth of PC-3, DU-145 and Dunning AT-1 androgen-independent prostate cancers, through diminution of GH release and the resulting decrease in the secretion of hepatic IGF-I, or through mechanisms involving a lowering of tumour IGF-i levels and possibly an inhibition of tumours IGF- I and IGF-II production.