Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10815580 | Cellular Signalling | 2012 | 13 Pages |
Abstract
⺠Kinin B1 and B2 receptors are important in normal and pathological conditions. ⺠We tested kinin derivatives containing C-terminal Lys instead of the native Arg. ⺠Lys9-bradykinin and Lys10-kallidin effectively activated both B1 and B2 receptors. ⺠The Lys-kinin derivatives showed biased agonism for B2 receptor activation of ERK1/2. ⺠Dual activators of B1and B2 receptors might be therapeutically useful.
Keywords
GPCRdes-Arg10-kallidinKinin B2 receptorCarboxypeptidaseinositol triphosphateRIPAPBSIP3eNOSiNOSFBSHEKDMEMDes-Arg9-bradykininG protein-coupled receptorsDulbecco's modified Eagle's medium[Ca2 +]iradio-immunoprecipitation assayEndocytosisBiased agonistbradykinin B2 receptorbradykininChoChinese Hamster Ovaryfetal bovine seruminducible nitric oxide synthaseendothelial nitric oxide synthaseintracellular calcium concentrationPhosphate buffered salinePhosphoinositideNitric oxideKallidinhuman embryonic kidneyKinin B1 receptorG protein-coupled receptor
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Authors
Xianming Zhang, Jessica L. Lowry, Viktor Brovkovych, Randal A. Skidgel,