C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/705 (2006.01) A61K 38/06 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/17 (2006.01) C07K 5/08 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2104099
-54- PEPTIDE INHIBITORS OF INFLAMMATION MEDIATED BY SELECTINS Abstract of the Invention Peptides derived from three regions of the lectin domain of GMP-140 (P-selectin) and the related selectins, ELAM-1 (E-selectin) and the lymphocyte homing receptor (L-selectin), have been found to inhibit neutrophil adhesion to GMP-140. These and additional peptides have been synthesized, having as their core region portions of the 74-76 amino acid sequence of GMP-140, with residue 1 defined as the N- terminus of the mature protein after the cleavage of the signal peptide. Examples demonstrate the inhibition of the binding of neutrophils to GMP-140 of peptides in concentrations ranging from 30 to 1500 µmol. It has been found that alterations within the core sequence, as well as N-terminal and C-terminal flanking regions, do not result in loss of biological activity. The peptides are useful as diagnostics and, in combination with a suitable pharmaceutical carrier, for clinical applications in the modulation or inhibition of coagulation processes or inflammatory processes.
Epps Leon A.
Geng Jian-Guo
Heavner George A.
Kruszynski Marion
Mcever Roger P.
Bereskin & Parr
Centecor Inc.
The Board Of Regents Of The University Of Oklahoma
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