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TargetEnzymes

cAMP-dependent protein kinase catalytic subunit alpha

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
4
Compounds
4
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

KAPCA_HUMANPRKACAHomo sapiens

cAMP-dependent protein kinase catalytic subunit alpha

Phosphorylates a large number of substrates in the cytoplasm and the nucleus15642694,15905176,16387847,17333334,17565987,17693412,18836454,19949837,20356841,21085490,21514275,21812984,21852232,31112131,41652173. Phosphorylates CDC25B, ABL1, NFKB1, CLDN3, histone H1.4 (H1-4), PSMC5/RPT6, PJA2, RYR2, RORA, SLC6A6, SOX9, UHRF1 and VASP15178447,15642694,15905176,16387847,17333334,17565987,17693412,18836454,19949837,20356841,21085490,21514275,21812984,41652173. Regulates the abundance of compartmentalized pools of its regulatory subunits through phosphorylation of PJA2 which binds and ubiquitinates these subunits, leading to their subsequent proteolysis21423175. RORA is activated by phosphorylation21514275. Required for glucose-mediated adipogenic differentiation increase and osteogenic differentiation inhibition from osteoblasts19949837. 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 VASP15642694,20356841. Prevents the antiproliferative and anti-invasive effects of alpha-difluoromethylornithine in breast cancer cells when activated17333334. 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+)17693412. PSMC5/RPT6 activation by phosphorylation stimulates proteasome17565987. Negatively regulates tight junctions (TJs) in ovarian cancer cells via CLDN3 phosphorylation15905176. NFKB1 phosphorylation promotes NF-kappa-B p50-p50 DNA binding15642694. 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 genes16705181. GLI transcription factor phosphorylation is inhibited by interaction of PRKACA with SMO which sequesters PRKACA at the cell membrane36202993,39138140. Also inhibits the smoothened signaling pathway in embryonic development by catalyzing phosphorylation of OFD1 in ciliogenesis33934390. 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 AICDA16387847,18836454. Phosphorylates HSF1; this phosphorylation promotes HSF1 nuclear localization and transcriptional activity upon heat shock21085490. Acts as a negative regulator of mTORC1 by mediating phosphorylation of RPTOR31112131. Phosphorylates AKAP1927028580
Phosphorylates and activates ABL1 in sperm flagellum to promote spermatozoa capacitation

Quoted from UniProt’s FUNCTION annotation for P17612 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
PRKAR2A0.9990.8990.9000.901
PRKAR2B0.9990.9520.9000.931
PRKAR1B0.9990.9890.9000.700
AKAP10.9990.8370.5000.998
PRKAR1A0.9990.9530.9000.955
EZR0.9980.0000.9000.982
AKAP50.9980.7800.5000.985
PKIA0.9980.9730.9000.591
CREB10.9960.5100.9000.940
RYR20.9940.5710.9000.871

Where it sits in the cell

  • Cytosol
  • Microtubulesadditional
  • Cytokinetic bridgeadditional
  • Primary ciliumadditional
  • Basal bodyadditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm · Cell membrane · Membrane · Nucleus · Mitochondrion · Cell projection, cilium, flagellum · Cytoplasmic vesicle, secretory vesicle, acrosome

Expression by cell type

Single cell type RNA, the 12 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Other brain neurons42.7 nCPM
  • Microglia36.8 nCPM
  • Brain excitatory neurons34.9 nCPM
  • Brain inhibitory neurons32 nCPM
  • Bergmann glia25.2 nCPM
  • Astrocytes23.8 nCPM
  • Distal convoluted tubule cells21.8 nCPM
  • Oligodendrocyte progenitor cells21.7 nCPM
  • Oligodendrocytes20.8 nCPM
  • Ependymal cells20.2 nCPM
  • Renal connecting tubule cells19.8 nCPM
  • Renal collecting duct principal cells18.9 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • skeletal muscle276.2 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 4

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
cAMP-dependent protein kinase catalytic subunit alphaEnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1062854
cAMP-dependent protein kinase catalytic subunit alphaEnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1062854
cAMP-dependent protein kinase catalytic subunit alphaEnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1062854
cAMP-dependent protein kinase catalytic subunit alphaEnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1062854