cAMP-dependent protein kinase catalytic subunit alpha
Also known as: PKACA, PRKACA
Function
Phosphorylates a large number of substrates in the cytoplasm and the nucleus. Phosphorylates CDC25B, ABL1, NFKB1, CLDN3, histone H1.4 (H1-4), PSMC5/RPT6, PJA2, RYR2, RORA, SLC6A6, SOX9, UHRF1 and VASP. Regulates the abundance of compartmentalized pools of its regulatory subunits through phosphorylation of PJA2 which binds and ubiquitinates these subunits, leading to their subsequent proteolysis. RORA is activated by phosphorylation. Required for glucose-mediated adipogenic differentiation increase and osteogenic differentiation inhibition from osteoblasts. Involved in chondrogenesis by mediating phosphorylation of SOX9 (By similarity). Involved in the regulation of platelets in response to thrombin and collagen; maintains circulating platelets in a resting state by phosphorylating proteins in numerous platelet inhibitory pathways when in complex with NF-kappa-B (NFKB1 and NFKB2) and I-kappa-B-alpha (NFKBIA), but thrombin and collagen disrupt these complexes and free active PRKACA stimulates platelets and leads to platelet aggregation by phosphorylating VASP. Prevents the antiproliferative and anti-invasive effects of alpha-difluoromethylornithine in breast cancer cells when activated. RYR2 channel activity is potentiated by phosphorylation in presence of luminal Ca(2+), leading to reduced amplitude and increased frequency of store overload-induced Ca(2+) release (SOICR) characterized by an increased rate of Ca(2+) release and propagation velocity of spontaneous Ca(2+) waves, despite reduced wave amplitude and resting cytosolic Ca(2+). PSMC5/RPT6 activation by phosphorylation stimulates proteasome. Negatively regulates tight junctions (TJs) in ovarian cancer cells via CLDN3 phosphorylation. NFKB1 phosphorylation promotes NF-kappa-B p50-p50 DNA binding. Acts as a key inhibitor of smoothened signaling pathway by mediating phosphorylation of GLI (GLI1, GLI2 and GLI3) transcription factors in absence of hedgehog (DHH, IHH or SHH) morphogens: GLI phosphorylation promotes their processing and prevents transcriptional activation of smoothened target genes. GLI transcription factor phosphorylation is inhibited by interaction of PRKACA with SMO which sequesters PRKACA at the cell membrane. Also inhibits the smoothened signaling pathway in embryonic development by catalyzing phosphorylation of OFD1 in ciliogenesis. Prevents meiosis resumption in prophase-arrested oocytes via CDC25B inactivation by phosphorylation (By similarity). May also regulate rapid eye movement (REM) sleep in the pedunculopontine tegmental (PPT) (By similarity). Phosphorylates APOBEC3G and AICDA. Phosphorylates HSF1; this phosphorylation promotes HSF1 nuclear localization and transcriptional activity upon heat shock. Acts as a negative regulator of mTORC1 by mediating phosphorylation of RPTOR. Phosphorylates AKAP19.
Classification
- Family (Pfam)
- PF00069 Pkinase
- InterPro
- AGC-kinase_C, Kinase-like_dom_sf, Prot_kinase_dom, Protein_kinase_ATP_BS, Ser/Thr_kinase_AS, STKc_PKA
- Functional cluster
- Protein Serine/Threonine Kinases
Experimental structures · PDB · 53
- 2GU8 X-ray 2.20A
- 3AGL X-ray 2.10A
- 3AGM X-ray 2.00A
- 3AMA X-ray 1.75A
- 3AMB X-ray 2.25A
- 3L9L X-ray 2.00A
- 3L9M X-ray 1.90A
- 3L9N X-ray 2.00A
- 3MVJ X-ray 2.49A
- 3NX8 X-ray 2.00A
- 3OOG X-ray 2.00A
- 3OVV X-ray 1.58A
- … and 41 more
A predicted model is available from AlphaFold.
Gene Ontology · 72
- GO:0001669 acrosomal vesicle
- GO:0034704 calcium channel complex
- GO:0005952 cAMP-dependent protein kinase complex
- GO:0005813 centrosome
- GO:0097546 ciliary base
- GO:0005737 cytoplasm
- GO:0005829 cytosol
- GO:0070062 extracellular exosome
- GO:0098978 glutamatergic synapse
- GO:0005811 lipid droplet
- GO:0005759 mitochondrial matrix
- GO:0031594 neuromuscular junction
- GO:0016607 nuclear speck
- GO:0005654 nucleoplasm
- GO:0031588 nucleotide-activated protein kinase complex
- GO:0005634 nucleus
- GO:0048471 perinuclear region of cytoplasm
- GO:0005886 plasma membrane
- GO:0044853 plasma membrane raft
- GO:0098794 postsynapse
- GO:0036126 sperm flagellum
- GO:0097225 sperm midpiece
- GO:0005524 ATP binding
- GO:0004691 cAMP-dependent protein kinase activity
- GO:0099103 channel activator activity
- GO:0140198 histone H1-4S35 kinase activity
- GO:0000287 magnesium ion binding
- GO:0030145 manganese ion binding
- GO:0019870 potassium channel inhibitor activity
- GO:0019904 protein domain specific binding
- GO:0034237 protein kinase A regulatory subunit binding
- GO:0019901 protein kinase binding
- GO:0106310 protein serine kinase activity
- GO:0004674 protein serine/threonine kinase activity
- GO:0004712 protein serine/threonine/tyrosine kinase activity
- GO:0007189 adenylate cyclase-activating G protein-coupled receptor signaling pathway
- GO:0007193 adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
- GO:0141156 cAMP/PKA signal transduction
- GO:0086064 cell communication by electrical coupling involved in cardiac conduction
- GO:0071872 cellular response to epinephrine stimulus
- GO:0071377 cellular response to glucagon stimulus
- GO:0071333 cellular response to glucose stimulus
- GO:0034605 cellular response to heat
- GO:0019221 cytokine-mediated signaling pathway
- GO:0034380 high-density lipoprotein particle assembly
- GO:0030007 intracellular potassium ion homeostasis
- GO:0035694 mitochondrial protein catabolic process
- GO:0006397 mRNA processing
- GO:1904539 negative regulation of glycolytic process through fructose-6-phosphate
- GO:0032703 negative regulation of interleukin-2 production
- GO:0120186 negative regulation of protein localization to chromatin
- GO:1904262 negative regulation of TORC1 signaling
- GO:0050850 positive regulation of calcium-mediated signaling
- GO:0045542 positive regulation of cholesterol biosynthetic process
- GO:0045722 positive regulation of gluconeogenesis
- GO:0032024 positive regulation of insulin secretion
- GO:0050766 positive regulation of phagocytosis
- GO:0010898 positive regulation of triglyceride catabolic process
- GO:0099170 postsynaptic modulation of chemical synaptic transmission
- GO:2000810 regulation of bicellular tight junction assembly
- GO:1903779 regulation of cardiac conduction
- GO:0055117 regulation of cardiac muscle contraction
- GO:0010881 regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ion
- GO:0051726 regulation of cell cycle
- GO:0002027 regulation of heart rate
- GO:0016241 regulation of macroautophagy
- GO:0070507 regulation of microtubule cytoskeleton organization
- GO:0045667 regulation of osteoblast differentiation
- GO:0061136 regulation of proteasomal protein catabolic process
- GO:0003091 renal water homeostasis
- GO:0048240 sperm capacitation
- GO:0097700 vascular endothelial cell response to laminar fluid shear stress
Disease associations
- pigmented nodular adrenocortical disease, primary, 4 MONDO:0014359
- cardioacrofacial dysplasia 1 MONDO:0030876
Drugs targeting this protein · 1
- GSK-690693 inhibitor
Related proteins · sequence + function similarity
- cAMP-dependent protein kinase catalytic subunit alpha 1.00
- cAMP-dependent protein kinase catalytic subunit alpha 1.00
- cAMP-dependent protein kinase catalytic subunit alpha 1.00
- cAMP-dependent protein kinase catalytic subunit alpha 1.00
- cAMP-dependent protein kinase catalytic subunit alpha 1.00
- cAMP-dependent protein kinase catalytic subunit alpha 1.00
- cAMP-dependent protein kinase catalytic subunit alpha 1.00
- cAMP-dependent protein kinase catalytic subunit beta 0.99
- cAMP-dependent protein kinase catalytic subunit beta 0.99
- cAMP-dependent protein kinase catalytic subunit beta 0.99
- cAMP-dependent protein kinase catalytic subunit 1 0.99
- cAMP-dependent protein kinase catalytic subunit beta 0.98
Co-cited proteins · studied together in the literature
- cAMP-dependent protein kinase catalytic subunit alpha 1 shared papers
- Protein smoothened 2 shared papers
- Sodium- and chloride-dependent taurine transporter 1 shared papers
- cAMP-dependent protein kinase type I-alpha regulatory subunit 4 shared papers
- cAMP-dependent protein kinase catalytic subunit beta 3 shared papers
- Ryanodine receptor 2 1 shared papers
- cAMP-dependent protein kinase type II-beta regulatory subunit 2 shared papers
- E3 ubiquitin-protein ligase UHRF1 1 shared papers
- Histone H1.4 1 shared papers
- NF-kappa-B inhibitor alpha 1 shared papers
- E3 ubiquitin-protein ligase Praja-2 2 shared papers
- Heat shock factor protein 1 1 shared papers
Literature · 52 cited papers
- SLC6A6 imports taurine into mitochondria to sustain mitochondrial translation and tumour growth. Nat. Metab. · 2026
- GRK2 kinases in the primary cilium initiate SMOOTHENED-PKA signaling in the Hedgehog cascade. PLoS Biol. · 2024
- A PKA inhibitor motif within SMOOTHENED controls Hedgehog signal transduction. Nat. Struct. Mol. Biol. · 2022
- The TBC1D31/praja2 complex controls primary ciliogenesis through PKA-directed OFD1 ubiquitylation. EMBO J. · 2021
- Germline and Mosaic Variants in PRKACA and PRKACB Cause a Multiple Congenital Malformation Syndrome. Am. J. Hum. Genet. · 2020
- GPCR signaling inhibits mTORC1 via PKA phosphorylation of Raptor. Elife · 2019
- Structure of smAKAP and its regulation by PKA-mediated phosphorylation. FEBS J. · 2016
- N-terminome analysis of the human mitochondrial proteome. Proteomics · 2015
- Multifunctional reagents for quantitative proteome-wide analysis of protein modification in human cells and dynamic profiling of protein lipidation during vertebrate development. Angew. Chem. Int. Ed. · 2015
- Global profiling of co- and post-translationally N-myristoylated proteomes in human cells. Nat. Commun. · 2014
- Recurrent somatic mutations underlie corticotropin-independent Cushing's syndrome. Science · 2014
- Recurrent activating mutation in PRKACA in cortisol-producing adrenal tumors. Nat. Genet. · 2014
- … and 40 more in the literature graph