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Lysyl 4-aminobenzoic acid derivatives as potent small molecule mimetics of plasminogen kringle 5.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Feb 23; Vol. 14 (4), pp. 965-6. - Publication Year :
- 2004
-
Abstract
- Kringle 5, a proteolytic fragment of human plasminogen has been shown to potently inhibit angiogenesis. The tetrapeptide KLYD derived from kringle 5 has been shown to capture many activities of kringle 5 in vitro. Further simplification has been achieved by replacement of the two central amino acids with a 4-aminobenzoic acid spacer group. Molecules displaying the required recognition groups on this core show similar in vitro properties to kringle 5, and are able to displace radiolabeled protein from a high affinity binding site on endothelial cells.
- Subjects :
- Cell Migration Inhibition
Cell Movement drug effects
Endothelium, Vascular drug effects
Endothelium, Vascular metabolism
Humans
Molecular Structure
Plasminogen chemistry
Plasminogen genetics
Vascular Endothelial Growth Factor A antagonists & inhibitors
Vascular Endothelial Growth Factor A pharmacology
4-Aminobenzoic Acid chemistry
Kringles
Molecular Mimicry
Plasminogen pharmacology
para-Aminobenzoates
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 14
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15013002
- Full Text :
- https://doi.org/10.1016/j.bmcl.2003.12.034