PKG1 Serine/threonine protein kinase that acts as key mediator of the nitric oxide (NO)/cGMP signaling pathway. GMP binding activates PRKG1, which phosphorylates serines and threonines on many cellular proteins. Numerous protein targets for PRKG1 phosphorylation are implicated in modulating cellular calcium, but the contribution of each of these targets may vary substantially among cell types. Proteins that are phosphorylated by PRKG1 regulate platelet activation and adhesion, smooth muscle contraction, cardiac function, gene expression, feedback of the NO-signaling pathway, and other processes involved in several aspects of the CNS like axon guidance, hippocampal and cerebellar learning, circadian rhythm and nociception. Smooth muscle relaxation is mediated through lowering of intracellular free calcium, by desensitization of contractile proteins to calcium, and by decrease in the contractile state of smooth muscle or in platelet activation. Regulates intracellular calcium levels via several pathways: phosphorylates MRVI1/IRAG and inhibits IP3-induced Ca(2+) release from intracellular stores, phosphorylation of KCNMA1 (BKCa) channels decreases intracellular Ca(2+) levels, which leads to increased opening of this channel. PRKG1 phosphorylates the canonical transient receptor potential channel (TRPC) family which inactivates the associated inward calcium current. Another mode of action of NO/cGMP/PKGI signaling involves PKGI-mediated inactivation of the Ras homolog gene family member A (RhoA). Phosphorylation of RHOA by PRKG1 blocks the action of this protein in myriad processes: regulation of RHOA translocation; decreasing contraction; controlling vesicle trafficking, reduction of myosin light chain phosphorylation resulting in vasorelaxation. Activation of PRKG1 by NO signaling alters also gene expression in a number of tissues. In smooth muscle cells, increased cGMP and PRKG1 activity influence expression of smooth muscle-specific contractile proteins, levels of proteins in the NO/cGMP signaling pathway, down-regulation of the matrix proteins osteopontin and thrombospondin-1 to limit smooth muscle cell migration and phenotype. Regulates vasodilator-stimulated phosphoprotein (VASP) functions in platelets and smooth muscle. Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. cGMP subfamily. Primarily expressed in lung and placenta. 2 alternatively spliced human isoforms have been reported. Note: This description may include information from UniProtKB.

Protein type: AGC group; EC 2.7.11.12; Kinase, protein; PKG family; Protein kinase, AGC; Protein kinase, Ser/Thr (non-receptor)

Chromosomal Location of human Ortholog: 10q11.23-q21.1

Cellular Component: acrosomal vesicle; cytoplasm; cytosol; Golgi apparatus; nucleoplasm; plasma membrane; sarcolemma

Molecular Function: ATP binding; calcium channel regulator activity; cGMP binding; cGMP-dependent protein kinase activity; identical protein binding; mitogen-activated protein kinase p38 binding; protein binding; protein kinase activity; protein serine kinase activity

Biological Process: actin cytoskeleton organization; cell growth involved in cardiac muscle cell development; cerebellum development; cGMP-mediated signaling; collateral sprouting; dendrite development; forebrain development; negative regulation of glutamate secretion; negative regulation of inositol phosphate biosynthetic process; negative regulation of platelet aggregation; negative regulation of vascular associated smooth muscle cell migration; negative regulation of vascular associated smooth muscle cell proliferation; neuron migration; positive regulation of circadian rhythm; positive regulation of cytosolic calcium ion concentration; positive regulation of large conductance calcium-activated potassium channel activity; protein phosphorylation; regulation of GTPase activity; regulation of testosterone biosynthetic process; relaxation of vascular associated smooth muscle; signal transduction; spermatid development

Reference #: Q13976 (UniProtKB)

Alt. Names/Synonyms: AAT8; cGK; cGK 1; cGK1; cGKI; cGKI-alpha; cGKI-BETA; cGMP-dependent protein kinase 1; cGMP-dependent protein kinase I; DKFZp686K042; FLJ36117; KGP1; MGC71944; PGK; PKG; PKG1; PRKG1; PRKG1B; PRKGR1A; PRKGR1B; protein kinase cGMP-dependent 1; protein kinase, cGMP-dependent, regulatory, type I, beta; protein kinase, cGMP-dependent, type I

Gene Symbols: PRKG1

Molecular weight: 76,364 Da

Basal Isoelectric point: 5.74 Predict pI for various phosphorylation states

Protein-Specific Antibodies, siRNAs or Recombinant Proteins from Cell Signaling Technology^®

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PKG1

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