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Chemical Compound Review:

P-Cttlvc-T 10-(4-aminobutyl)-N-(1- aminocarbonyl-2...

Synonyms: RC-121, AR-1B9973, RC 121, IM 4-28, AC1L2RX7, ...

Karashima, T. et al., Srkalovic, G. et al., Banks, W.A. et al., Radulovic, S. et al., Schally, A.V. et al., et al.

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Disease relevance of RC 121

In specimens of human meningioma the highest binding was found with analogs RC-121, RC-95-I, and RC-101-I [1].
In human epithelial ovarian cancers and an arrhenoblastoma, analogs D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Trp-NH2 (RC-95-I), D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 (RC-121) and D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Trp-NH2 (RC-160) appeared to be the most potent in displacing labeled SS-14 [1].
This study was conducted to investigate the effects of targeted cytotoxic SST analogue AN-238, consisting of 2-pyrrolinodoxorubicin (AN-201), a potent derivative of doxorubicin (DOX) linked to somatostatin analogue RC-121, on the growth of SST receptor-positive U-87 MG human glioblastomas [2].
Octapeptide somatostatin analogs, RC-160 and RC-121, showed 10 times higher binding affinity for somatostatin receptors on colon cancer membranes than somatostatin [3].
Nude mice bearing xenografts of MIA PaCa-2 human pancreatic cancer cell line were treated for 4 weeks with AN-51, a somatostatin octapeptide analog D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 (RC-121) containing methotrexate attached to the alpha-amino group of D-Phe in position 1 [4].

High impact information on RC 121

When SST-like activities of AN-238 and its carrier, RC-121, were compared in the rat pituitary superfusion system, both compounds were found to suppress a stimulated growth hormone release at nanomolar concentrations [5].
We studied the ability of three therapeutically promising radioactively labeled somatostatin octapeptide analogs, RC-160, RC-121, and RC-161, to cross the blood-brain barrier (BBB) after peripheral or central injection [6].
The clearance from the CNS of RC-160 and RC-121, but not RC-161, was faster than could be accounted for by reabsorption of cerebrospinal fluid [6].
When haloperidol was used to elevate PRL level, a single injection of RC-121 inhibited PRL release in EB-pretreated female rats or untreated female and male rats [7].
Control groups of mice received saline, RC-121 or methotrexate [4].

Anatomical context of RC 121

Several octapeptide analogs of somatostatin including D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Trp-NH2 (RC-160) and D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 (RC-121), which were superactive in tests on suppression of GH levels, were 4-5 times more potent than S-S-14 in inhibiting desglugastrin-stimulated gastric acid secretion in GF dogs [8].

Associations of RC 121 with other chemical compounds

Cytotoxic radical AN-201, the unconjugated mixture of somatostatin analogue RC-121 and AN-201 or RC-121 alone had no significant effects [9].
Analog D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 (RC-121), at a dose of 5 micrograms/100 g body wt, did not decrease basal PRL levels in thiopental-anesthetized female rats, untreated or treated with estrogen benzoate (EB) (8 micrograms/rat) for 5 days [7].
The cytotoxic somatostatin (SST) analog, AN-238, consists of a superactive derivative of doxorubicin (DOX), 2-pyrrolino-DOX (AN-201), linked to the SST analog carrier, RC-121 [10].
The cytoprotective effect of a highly potent somatostatin (SRIF) analog, RC-121 (H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2), was examined in the absolute ethanol-induced gastric erosion model in rat [11].

Gene context of RC 121

Blockade of somatostatin receptors by excess RC-121 abolished the effect of AN-238, demonstrating targeting [9].
These results indicate that analogs RC-160 and RC-121 possess prolonged and enhanced biological activities, the former analog showing a high selectivity in inhibiting GH and glucagon release in vivo as compared with that of insulin secretion [12].

Analytical, diagnostic and therapeutic context of RC 121

Tumor volume was significantly decreased by [D-Trp6]LH-RH microcapsules or RC-121 given alone [13].

References

Evaluation of receptors for somatostatin in various tumors using different analogs. Srkalovic, G., Cai, R.Z., Schally, A.V. J. Clin. Endocrinol. Metab. (1990) [Pubmed]
Regression of U-87 MG human glioblastomas in nude mice after treatment with a cytotoxic somatostatin analog AN-238. Kiaris, H., Schally, A.V., Nagy, A., Sun, B., Szepeshazi, K., Halmos, G. Clin. Cancer Res. (2000) [Pubmed]
The binding of bombesin and somatostatin and their analogs to human colon cancers. Radulovic, S.S., Milovanovic, S.R., Cai, R.Z., Schally, A.V. Proc. Soc. Exp. Biol. Med. (1992) [Pubmed]
Cytotoxic analog of somatostatin containing methotrexate inhibits growth of MIA PaCa-2 human pancreatic cancer xenografts in nude mice. Radulovic, S., Nagy, A., Szoke, B., Schally, A.V. Cancer Lett. (1992) [Pubmed]
Synthesis and biological evaluation of cytotoxic analogs of somatostatin containing doxorubicin or its intensely potent derivative, 2-pyrrolinodoxorubicin. Nagy, A., Schally, A.V., Halmos, G., Armatis, P., Cai, R.Z., Csernus, V., Kovács, M., Koppán, M., Szepesházi, K., Kahán, Z. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
Permeability of the murine blood-brain barrier to some octapeptide analogs of somatostatin. Banks, W.A., Schally, A.V., Barrera, C.M., Fasold, M.B., Durham, D.A., Csernus, V.J., Groot, K., Kastin, A.J. Proc. Natl. Acad. Sci. U.S.A. (1990) [Pubmed]
Inhibitory effects of somatostatin analogs on prolactin secretion in rats pretreated with estrogen or haloperidol. Karashima, T., Schally, A.V. Proc. Soc. Exp. Biol. Med. (1987) [Pubmed]
Effect of somatostatin analogs on gastric acid secretion in dogs and rats. Schally, A.V., Colaluca, J., Paulson, D., Carter, W.H., Neitzschman, H.R., Lafaye, H., Cai, R.Z. Int. J. Pept. Protein Res. (1990) [Pubmed]
Growth inhibition of experimental non-Hodgkin's lymphomas with the targeted cytotoxic somatostatin analogue AN-238. Keller, G., Engel, J.B., Schally, A.V., Nagy, A., Hammann, B., Halmos, G. Int. J. Cancer (2005) [Pubmed]
Targeted therapy with a cytotoxic somatostatin analog, AN-238, inhibits growth of human experimental endometrial carcinomas expressing multidrug resistance protein MDR-1. Engel, J.B., Schally, A.V., Halmos, G., Baker, B., Nagy, A., Keller, G. Cancer (2005) [Pubmed]
Protective effect of an orally administered, highly potent somatostatin analog (RC-121) against absolute ethanol-induced hemorrhagic erosions of the rat gastric mucosa. László, F., Pávó, I., Penke, B., Bálint, G.A. Life Sci. (1989) [Pubmed]
Effects of highly potent octapeptide analogs of somatostatin on growth hormone, insulin and glucagon release. Karashima, T., Cai, R.Z., Schally, A.V. Life Sci. (1987) [Pubmed]
Somatostatin analogs as adjuncts to agonists of luteinizing hormone-releasing hormone in the treatment of experimental prostate cancer. Schally, A.V., Redding, T.W. Proc. Natl. Acad. Sci. U.S.A. (1987) [Pubmed]

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