C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/52 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/17 (2006.01) A61K 38/19 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C07K 14/715 (2006.01) G01N 33/566 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2245224
Peptides corresponding to the N-terminal 9 residues of stromal cell derived factor-1 (SDF-1) have SDF-1 activity. SDF-1, 1-8, 1-9, 1-9 dimer and 1-17 induced intracellular calcium and chemotaxis in T lymphocytes and CEM cells, and bound to CXC chemokine receptor 4 (CXCR4). The peptides had similar activities to SDF-1, but were less potent. Whereas native SDF-1 had half maximal chemoattractant activity at 5 nM, the 1-9 dimer required 500 nM and was therefore 100 fold less potent. The 1-17 and a 1-9 monomer analog were 4- and 36-fold, respectively less potent than the 1-9 dimer. Both the chemotactic and calcium response of the 1-9 dimer was inhibited by an antibody to CXCR4. The basis for the enhanced activity of the dimer form of SDF-1, 1-9 is uncertain but it could involve an additional fortuitous binding site on the 1-9 peptide in addition to the normal SDF-1, 1-9 site. A 1-9 analog, 1-9[P2G] dimer, was found to be a CXCR4 antagonist. Overall this study shows that the N-terminal peptides are CXCR4 agonists or antagonist and these could be leads for high affinity ligands.
Clark-Lewis Ian
Giong Jiang-Hong
Clark-Lewis Ian
Giong Jiang-Hong
Smart & Biggar
University Of British Columbia
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