Enzyme and receptor modulation

Details Enzyme and receptor modulation Enzyme and receptor modulation

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2607020

Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

L'invention porte sur la conjugaison covalente d'un ester d'acide aminé alpha et d'un modulateur de l'activité d'une enzyme ou d'un récepteur intracellulaire cible, le groupe ester du conjugué étant hydrolysable par une ou plusieurs enzymes carboxylestérases intracellulaires à l'acide correspondant, qui mène à une accumulation du produit de l'hydrolyse de l'acide carboxylique dans la cellule et permet une modulation de l'enzyme ou du récepteur améliorée ou prolongée par rapport au modulateur non conjugué.

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