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Molecules that inhibit a metabolic pathway that involves the protein tyrosine kinase Syk and identification procedure of said molecules
专利权人:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
发明人:
DARIAVACH, PIONA,MARTINEAU, PIERRE,VILLOUTREIX, BRUNO
申请号:
ES09738328
公开号:
ES2537518T3
申请日:
2009.04.08
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A molecule that binds to the Syk tyrosine kinase protein in a three-dimensional cavity comprising the arginine moiety located at position 68 and the two glutamic acid residues located at positions 121 and 155 of the human Syk tyrosine kinase protein, whose sequence is defined in SED ID No. 1, and (b) which can inhibit at least 5 in 10% in vitro the binding of (i) the G4G11 antibody fragment (SEQ ID No. 2), or, (ii) an antibody or fragment of antibody that binds to human Syk tyrosine kinase in an epitope comprising at least one of residues 65 to 74 of the amino acid sequence of the human Syk tyrosine kinase protein (SEQ ID NO: 1), or (iii) an antibody or antibody fragment that binds with the human Syk tyrosine kinase protein and inhibits at least 10% the binding of the G4G11 antibody fragment with the human Syk tyrosine kinase protein (SEQ ID NO: 1), with the protein tyrosine kinase protein Human Syk or with one of its variants in animals, for use in the prevention or treatment of a pathology dependent on a metabolic pathway that involves Syk in the human or animal, in which said pathology is caused by a type I hypersensitivity, or is rheumatoid polyarthritis , an autoimmune disease, an inflammation or a cancer, wherein said molecule is the C-13 molecule that has the formula ** Formula ** or is an organic molecule that has a molecular weight between 50 and 2500 Da, equivalent from the functional point of view of the C-13 molecule, selected from the molecules that have one of the following formulas: ** Formula ** in which - R1 is a substituted or unsubstituted aromatic group, or a substituted or unsubstituted heterocycle comprising at least one atom of S, O or N; R2 is a substituted or unsubstituted aromatic group, an unsubstituted or substituted heterocycle, a saturated or unsaturated carbon chain comprising an amino group, a saturated or unsaturated carbon chain comprising a substituted or unsubstituted aromatic group or a chain unsaturated or saturated carbon compr
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