Low efficacy gonadotropin agonists and antagonists

Details Low efficacy gonadotropin agonists and antagonists Low efficacy gonadotropin agonists and antagonists

C - Chemistry, Metallurgy

07

K

C07K 14/59 (2006.01) A61K 38/24 (2006.01) A61P 15/08 (2006.01) C07K 14/61 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2511800

The present invention provides glycoprotein hormone analogs having partial agonist/antagonist activity comprising an .alpha.-subunit polypeptide and a .beta.-subunit polypeptide. The analog lacks a naturally occurring oligosaccharide on .alpha.-subunit.alpha. loop 2 and is crosslinked to the .beta.-subunit by a disulfide bond. The present invention also provides a method for stimulating fertility in mammals by promoting apoptosis of ovarian cells and/or luteal cells, which comprises administering to the mammal a therapeutically effective amount of a glycoprotein hormone analog having partial agonist/antagonist activity.

L'invention concerne des analogues d'hormone glycoprotéine présentant une activité agoniste/antagoniste partielle comprenant un polypeptide de sous-unité .alpha. et un polypeptide de sous-unité .beta.. L'analogue ne possède pas d'oligosaccharide naturel sur la boucle 2 de la sous-unité .alpha. et est réticulé avec la sous-unité .beta. par une liaison disulfure. L'invention concerne également une méthode qui permet de stimuler la fertilité dans des mammifères en promouvant l'apoptose des cellules de l'ovaire et/ou des cellules lutéiniques. Cette méthode consiste à administrer au mammifère une quantité efficace sur le plan thérapeutique d'un analogue d'hormone glycoprotéine présentant une activité agoniste/antagoniste partielle.

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