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PL-3994   Click here for help

GtoPdb Ligand ID: 9067

Compound class: Peptide
Comment: PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist, with potential as a bronchodilating therapeutic. It is a cyclo-peptide with sequence Hept-cyclo(Cys-His-Phe-d-Ala-Gly-Arg-d-Nle-Asp-Arg-Ile-Ser-Cys)-Tyr-[Arg mimetic]-NH2 [1]. This peptide benefits from being resistant to enzymatic degradation by neutral endopeptidase (a.k.a. NEP or neprilysin), the metabolic enzyme of endogenous natriuretic peptides.
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References
1. Edelson JD, Makhlina M, Silvester KR, Vengurlekar SS, Chen X, Zhang J, Koziol-White CJ, Cooper PR, Hallam TJ, Hay DW et al.. (2013)
In vitro and in vivo pharmacological profile of PL-3994, a novel cyclic peptide (Hept-cyclo(Cys-His-Phe-d-Ala-Gly-Arg-d-Nle-Asp-Arg-Ile-Ser-Cys)-Tyr-[Arg mimetic]-NH(2)) natriuretic peptide receptor-A agonist that is resistant to neutral endopeptidase and acts as a bronchodilator.
Pulm Pharmacol Ther, 26 (2): 229-38. [PMID:23154072]