Sr-bi antagonists and use thereof as contraceptives and in...

Details Sr-bi antagonists and use thereof as contraceptives and in... Sr-bi antagonists and use thereof as contraceptives and in...

A - Human Necessities

61

K

A61K 38/17 (2006.01) A61K 39/395 (2006.01) C07K 14/705 (2006.01) C07K 16/28 (2006.01) C12N 15/85 (2006.01) G01N 33/53 (2006.01) A61K 38/00 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2302403

SR-BI is present on the membranes of hepatocytes and steroidogenic tissues, including the adrenal gland, testes, and ovaries, where it mediates the uptake and transport of cholesteryl ester from high density lipoproteins. It has been demonstrated that transgenic animals which do not produce SR-BI are perfectly healthy, with the exception that the females are infertile. This provides evidence that inhibition of uptake, binding or transport of cholesteryl ester to SR-BI can be used to inhibit pregnancy. The same pathway can also be used to decrease production of steroids, and therefore be used as a therapy for disorders involving steroidal overproduction.

L'invention concerne le SR-BI qui est présent dans les membranes d'hépatocytes et de tissus stéroïdogènes, y compris dans la glande surrénale, les testicules et les ovaires, où il régule le prélèvement et le transport d'ester de cholestéryle à partir de lipoprotéines de haute densité. Il a été démontré que des animaux transgéniques ne produisant pas de SR-BI sont en parfaite santé, à l'exception de l'infertilité des femelles. Cela prouve qu'une inhibition du prélèvement, de la liaison ou du transport de l'ester de cholestéryle à SR-BI peut s'utiliser pour inhiber la grossesse. On peut également utiliser la même voie pour réduire la production de stéroïdes, et donc l'utiliser comme thérapie de troubles induisant une surproduction de stéroïdes.

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