Regular ArticleMAPKK-Dependent Growth Factor-Induced Upregulation of P2Y2Receptors in Vascular Smooth Muscle Cells
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2021, Biochemical PharmacologyCitation Excerpt :Lie et al. [184] identified P2Y1R antagonists as potential therapeutic agents for neointima (scar tissue) formation after acute vascular injury. Inhibition of P2Y2R has been also proposed as an option to help prevent the proliferation of endothelial and smooth muscle cells during vascular remodeling in restenosis after angioplasty [185,186]. Clouet et al. indicated that selective P2Y6R agonists could be of therapeutic value in reducing cardiac hypertrophy and associated damages [187].
Calcium mobilization and spontaneous transient outward current characteristics upon agonist activation of P2Y<inf>2</inf> receptors in smooth muscle cells
2005, Biophysical JournalCitation Excerpt :P2Y2 receptors are clearly distinguished from P2Y1 because of the specific actions on the P2Y2 receptor of uridine 5′-triphosphate (UTP), ED50 of 1 μM (see Bultmann et al., 1998), which can be released by endothelial cells (Saiag et al., 1998). Activation of P2Y2 receptors, which like other P2Y receptors are coupled to phospholipase C (von Kugelgen and Wetter, 2000), releases calcium from intracellular stores (Hou et al., 1999), after which receptor phosphorylation appears to regulate desensitization of the P2Y2 receptor through the action of a protein kinase (Otero et al., 2000). The wild-type P2Y2 receptor sequesters in a time-dependent manner, as do other G-protein coupled receptors (Wilkinson et al., 1994; Koenig and Edwardson, 1996).
Cellular distribution and functions of P2 receptor subtypes in different systems
2004, International Review of CytologyCitation Excerpt :In the synthetic phenotype, the mitogenic P2Y1 and P2Y2 receptors are upregulated, while the P2X1 receptor is totally downregulated. The same group later showed that MAPKK-dependent growth factor can induce upregulation of P2Y2 receptors in vascular smooth muscle cells (Hou et al., 1999a) and speculated that this may be of importance in atherosclerosis and neointima formation after balloon angioplasty. The inflammatory cytokine IL-1β induced a time- and dose-dependent upregulation of P2Y2 receptor mRNA in vascular smooth muscle cells, which was greatly enhanced when combined with interferin-γ or TNF-α; lipopolysaccharide also significantly increased the expression of P2Y2 receptor mRNA (Hou et al., 2000).
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