Design, Synthesis, and Characterization of Fatty Acid Derivatives of a Dimeric Peptide-Based Postsynaptic Density-95 (PSD-95) Inhibitor
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Design, Synthesis, and Characterization of Fatty Acid Derivatives of a Dimeric Peptide-Based Postsynaptic Density-95 (PSD-95) Inhibitor. / Nissen, Klaus B; Andersen, Julie J; Haugaard-Kedström, Linda Maria; Bach, Anders; Strømgaard, Kristian.
In: Journal of Medicinal Chemistry, Vol. 58, 2015, p. 1575-1580.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Design, Synthesis, and Characterization of Fatty Acid Derivatives of a Dimeric Peptide-Based Postsynaptic Density-95 (PSD-95) Inhibitor
AU - Nissen, Klaus B
AU - Andersen, Julie J
AU - Haugaard-Kedström, Linda Maria
AU - Bach, Anders
AU - Strømgaard, Kristian
PY - 2015
Y1 - 2015
N2 - 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.
AB - 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.
U2 - 10.1021/jm501755d
DO - 10.1021/jm501755d
M3 - Journal article
C2 - 25590984
VL - 58
SP - 1575
EP - 1580
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
ER -
ID: 130178670