Pharmacological chaperones for treating obesity

Details Pharmacological chaperones for treating obesity Pharmacological chaperones for treating obesity

A - Human Necessities

61

K

A61K 31/505 (2006.01) A61K 31/496 (2006.01) A61P 3/04 (2006.01) C12Q 1/00 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2610860

The invention relates to methods of enhancing normal melanocortin-4 receptor (MC4R) activity, and to enhancing activity of an MC4R having a mutation which affects protein folding and/or processing of the MC4R. The invention provides a method of treating an individual having a condition in which increased activity of an MC4R at the cell surface would be beneficial, for example in obesity, by administering an effective amount of a pharmacological chaperone for the MC4R. The invention provides MC4R pharmacological chaperones which enhance the activity of MC4R. The invention further provides a method of screening to identify pharmacological chaperones which enhance folding of an MC4R in the endoplasmic reticulum (ER), in order to enhance the activity of the MC4R at the cell surface.

L'invention concerne des méthodes destinées à renforcer l'activité du récepteur de la mélanocortine 4 (MC4R) normal et à renforcer l'activité d'un MC4R présentant une mutation modifiant le repliement et/ou la maturation protéique du MC4R. L'invention concerne une méthode destinée à traiter un individu présentant une affection, telle que l'obésité, pour laquelle une activité accrue d'un MC4R au niveau de la surface cellulaire serait bénéfique. Cette méthode consiste à administrer une dose efficace d'une chaperone pharmacologique pour ce MC4R. L'invention concerne des chaperones pharmacologiques de MC4R renforçant l'activité de MC4R. Elle se rapporte en outre à une méthode de criblage destinée à identifier des chaperones pharmacologiques augmentant le repliement d'un MC4R dans le réticulum endoplasmique (RE) en vue d'un renforcement de l'activité du MC4R au niveau de la surface cellulaire.

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