Covalent attachment of ligands to nucleophilic proteins...

A - Human Necessities – 61 – K

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A61K 38/02 (2006.01) A61K 39/00 (2006.01) A61K 39/395 (2006.01) A61K 47/48 (2006.01) C07H 21/00 (2006.01) C07K 7/00 (2006.01) C07K 14/00 (2006.01) G01N 33/53 (2006.01)

Patent

CA 2520392

A covalently reactive ligand analogue (CAL) of formula (1): wherein, L1 ...Lx...Lm are components defining a ligand determinant, LX is a component unit of the ligand determinant selected from the group consisting of an amino acid residue, sugar residue, a fatty acid residue and a nucleotide, L' is a functional group of LX, Y" is atom, covalent bond or linker, Y' is an optional charged or neutral group Y is a covalently reactive electrophilic group that reacts specifically with a receptor that binds to said ligand determinant, and n is an integer from 1 to 1000 m is an integer from 1 to 30.

L'invention concerne un analogue de ligands réactif par covalence (CAL) de formule (1), dans laquelle L¿1? ...L¿x?...L¿m? sont des constituants définissant un déterminant des ligands; L<SB>X</SB> est un constituant du déterminant des ligands sélectionné dans le groupe constitué par un résidu d'acides aminés, un résidu de sucre, un résidu d'acides gras et un nucléotide; L' est un groupe fonctionnel de L<SB>X</SB>; Y" est un atome, une liaison covalente ou un lieur; Y' est un groupe facultatif chargé ou neutre; Y est un groupe électrophile à réaction covalente qui réagit spécifiquement en présence d'un récepteur, lequel se lie audit déterminant des ligands; n est un entier compris entre 1 et 1000; et m est un entier compris entre 1 et 30.

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