| Autor: |
Nissen KB; Department of Drug Design and Pharmacology, University of Copenhagen , Universitetsparken 2, DK-2100 Copenhagen, Denmark., Andersen JJ, Haugaard-Kedström LM, Bach A, Strømgaard K |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2015 Feb 12; Vol. 58 (3), pp. 1575-80. Date of Electronic Publication: 2015 Jan 30. |
| DOI: |
10.1021/jm501755d |
| Abstrakt: |
Dimeric peptide-based inhibitors of postsynaptic density-95 (PSD-95) can reduce ischemic brain damage and inflammatory pain in rodents. To modify the pharmacokinetic profile, we designed a series of fatty acid linked dimeric ligands, which potently inhibits PSD-95 and shows improved in vitro blood plasma stability. Subcutaneous administration in rats showed extended stability and sustained release of these ligands. This can facilitate new pharmacological uses of PSD-95 inhibitors and further exploration of PSD-95 as a drug target. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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