Inhibitors of pla2

Details Inhibitors of pla2 Inhibitors of pla2

C - Chemistry, Metallurgy

07

K

C07K 7/04 (2006.01) A61K 38/08 (2006.01) A61K 38/12 (2006.01) C07K 7/06 (2006.01) C07K 7/64 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2266746

The present invention relates to a three-dimensional structure which inhibits the activity of PLA2. In one particular aspect the structure has a conformation and polarity such that it binds to (i) at least one amino acid in the N-terminal helix region of PLA2; and/or (ii) at least one amino acid in the region spanning residues (70-77) of PLA2. In another aspect the structure is a peptide comprising D-amino acids which has a sequence corresponding to the reverse sequence of a region between residues (69 and 75) of PLA2.

La présente invention concerne une structure tridimensionnelle inhibitrice de l'activité des PLA¿2?. Sous l'un de ses aspects, la structure présente une conformation et une polarité telles qu'elle se lie à (i) au moins un acide aminé dans la région de l'hélice N-terminale des PLA¿2?; et/ou (ii) au moins un acide aminé dans la région entre les résidus (70-77) des PLA¿2?. Sous un autre aspect, la structure est un peptide comprenant des acides D-aminés et qui présente une séquence correspondant à la séquence inverse de la région entre les résidus (69 et 75) des PLA¿2?.

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