Metastin derivatives and use thereof

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/47 (2006.01)

Patent

CA 2571420

The invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, etc.). By modifying the constituent amino acids of metastin with specific modifying groups, metastin derivatives having more improved blood stability, etc. than native metastin and showing excellent cancer metastasis suppressing activity or cancer growth suppressing activity have been found. Furthermore, it has been found that these metastin derivatives exhibit effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc., which are wholly different from the effects heretofore known.

La présente invention a trait à des dérivés de métastine présentant d'excellentes activité biologiques (une activité de suppression de la métastase, une activité de suppression de croissance cancéreuse, et analogues). Grâce à la modification des acides aminés constitutifs de la métastine à l'aide de groupes modificateurs, on a découvert des dérivés de métastine ayant une stabilité sanguine plus améliorée que la métastine native et présentant une excellente activité de suppression de la métastase du cancer ou une activité de suppression de croissance cancéreuse. En outre, on a découvert que ces dérivés de métastine présente des effets de suppression de sécrétion de hormones gonadotropes, la suppression de sécrétion d'hormones sexuelles, qui sont entièrement différents des effets connus à ce jour.

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