Antagonistic analogs of gh-rh (2003)

Details Antagonistic analogs of gh-rh (2003) Antagonistic analogs of gh-rh (2003)

C - Chemistry, Metallurgy

07

K

C07K 14/60 (2006.01) A61K 38/25 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2534436

There is provided a novel series of synthetic antagonistic analogs of hGH-RH(1- 29)NH2. These analogs inhibit the activity of endogenous hGH-RH on the pituitary GH-RH receptors, and therefore prevent the release of growth hormone. The analogs also inhibit the proliferation of human cancers through a direct effect on the cancer cells. The higher inhibitory potencies of the new analogs, as compared to previously described ones, results from replacement of various amino acids.

L'invention concerne une nouvelle série d'analogues antagonistes synthétiques de hGH-RH(1-29)NH¿2?. Ces analogues inhibent l'activité de la hGH-RH endogène sur les récepteurs GH-RH hypophysaires et, par conséquent, empêchent la libération de l'hormone de croissance. Les analogues inhibent également la prolifération de cancers humains, car ils ont un effet direct sur les cellules cancéreuses. La puissance inhibitrice supérieure de ces nouveaux analogues, par rapport aux précédents analogues, résulte du remplacement de divers acides aminés.

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