PKG
cGMP-dependent protein kinase
PKG is a cyclic guanosine monophosphate (cGMP) -dependent serine/threonine kinase, which is activated by cGMP, phosphorylates the substrates, and regulates intracellular signal transduction. PKG inhibits β-catenin and cyclin D1 and regulates cell growth and apoptosis. PKG phosphorylates myosin light chains in smooth muscle cells, causing smooth muscle relaxation, thereby regulating vasodilation and blood pressure. PKG phosphorylates calcium channels for calcium homeostasis regulation. PKG regulates gene expression by phosphorylating transcription factors, thereby affecting cell differentiation and proliferation. PKG also regulates circadian rhythm, anxiety and fear memory. PKG has 2 subtypes, PKG I and PKG II. PKG I is mainly expressed in smooth muscle, platelets and specific neuronal areas, participates in vascular smooth muscle relaxation and cardiac function regulation. PKG II is mainly expressed in intestinal secretory epithelial cells, juxtaglomerular cells, adrenal cortex, chondrocytes and suprachiasmatic nucleus, which is mainly involved in the regulation of kidney and adrenal function, as well as bone growth and development. PKG dysfunction could lead to cancer, neurological or cardiovascular diseases[1][2][3].
References:
- [1]. Francis SH, et al., cGMP-dependent protein kinases and cGMP phosphodiesterases in nitric oxide and cGMP action. Pharmacol Rev. 2010 Sep;62(3):525-63. [Content Brief]
- [2]. Hofmann F, et al., cGMP-dependent protein kinases (cGK). Methods Mol Biol. 2013;1020:17-50. [Content Brief]
- [3]. Karami-Tehrani F, et al., Expression of cGMP-dependent protein kinase, PKGIα, PKGIβ, and PKGII in malignant and benign breast tumors. Tumour Biol. 2012 Dec;33(6):1927-32. [Content Brief]
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Sp-8-Br-PET-cGMPS
0 ImagesCat. No.: HY-137633CAS No.: 172806-21-2Sp-8-Br-PET-cGMPS is a membrane-permeable PKG agonist and a membrane-permeable inhibitor of retinal-type cGMP-gated ion channels, as well as an activator of cGMP-dependent protein kinases I α and I β. Sp-8-Br-PET-cGMPS is resistant to mammalian cyclic nucleotide-dependent phosphodiesterases, has no metabolic side effects, and is more lipophilic and permeable than Sp-8-pCPT-cGMPS. Sp-8-Br-PET-cGMPS can be used to study the role of cGMP signaling pathways in the nervous system. -
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