PPP1R1A

gene
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Summary

PPP1R1A (protein phosphatase 1 regulatory inhibitor subunit 1A, HGNC:9286) is a protein-coding gene on chromosome 12q13.2, encoding Protein phosphatase 1 regulatory subunit 1A (Q13522). Inhibitor of protein-phosphatase 1.

Predicted to enable protein serine/threonine phosphatase inhibitor activity. Predicted to be involved in intracellular signal transduction. Predicted to be active in cytoplasm.

Source: NCBI Gene 5502 — RefSeq curated summary.

At a glance

  • GWAS associations: 4
  • Clinical variants (ClinVar): 32 total
  • MANE Select transcript: NM_006741

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:9286
Approved symbolPPP1R1A
Nameprotein phosphatase 1 regulatory inhibitor subunit 1A
Location12q13.2
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000135447
Ensembl biotypeprotein_coding
OMIM613246
Entrez5502

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 7 protein_coding, 1 nonsense_mediated_decay

ENST00000257905, ENST00000547431, ENST00000547826, ENST00000553113, ENST00000854646, ENST00000854647, ENST00000854648, ENST00000968383

RefSeq mRNA: 1 — MANE Select: NM_006741 NM_006741

CCDS: CCDS44912

Canonical transcript exons

ENST00000257905 — 7 exons

ExonStartEnd
ENSE000009200625458273254582795
ENSE000011472545458840554588659
ENSE000015322255457924654580392
ENSE000033014655458321154583248
ENSE000033575225458426054584320
ENSE000035035735458197654582131
ENSE000035956695458094454581050

Expression profiles

Bgee: expression breadth ubiquitous, 253 present calls, max score 99.65.

FANTOM5 (CAGE): breadth broad, TPM avg 20.1124 / max 1217.8638, expressed in 503 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter IDTPM avgSamples expressed
13136312.4198483
1313626.7505419
1313610.4808181
1313640.3919134
1313660.042418
1313650.026915

Top tissues by expression

294 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
triceps brachiiUBERON:000150999.65gold quality
diaphragmUBERON:000110399.47gold quality
hindlimb stylopod muscleUBERON:000425299.41gold quality
skeletal muscle tissue of rectus abdominisUBERON:000451199.35gold quality
gastrocnemiusUBERON:000138899.23gold quality
skeletal muscle tissue of biceps brachiiUBERON:000450299.18gold quality
gluteal muscleUBERON:000200099.10gold quality
vastus lateralisUBERON:000137999.03gold quality
biceps brachiiUBERON:000150799.01gold quality
skeletal muscle tissueUBERON:000113498.99gold quality
body of tongueUBERON:001187698.84gold quality
quadriceps femorisUBERON:000137798.79gold quality
renal medullaUBERON:000036298.70gold quality
caudate nucleusUBERON:000187398.34gold quality
putamenUBERON:000187498.32gold quality
type B pancreatic cellCL:000016998.23gold quality
islet of LangerhansUBERON:000000698.19gold quality
muscle organUBERON:000163098.18gold quality
muscle of legUBERON:000138397.86gold quality
middle frontal gyrusUBERON:000270297.76gold quality
apex of heartUBERON:000209897.71gold quality
adipose tissueUBERON:000101397.69gold quality
lateral globus pallidusUBERON:000247697.64gold quality
subcutaneous adipose tissueUBERON:000219097.61gold quality
nucleus accumbensUBERON:000188297.60gold quality
deltoidUBERON:000147697.49gold quality
medial globus pallidusUBERON:000247797.18gold quality
right lobe of liverUBERON:000111497.01gold quality
right atrium auricular regionUBERON:000663196.82gold quality
globus pallidusUBERON:000187596.74gold quality

Single-cell (SCXA)

Detected in 10 experiment(s), a significant marker in 8.

ExperimentMarker?Max mean expression
E-MTAB-11121yes848.57
E-MTAB-5061yes28.48
E-HCAD-31yes24.43
E-GEOD-81547yes16.39
E-MTAB-9388yes12.16
E-GEOD-83139yes9.00
E-HCAD-5yes8.68
E-ANND-3yes7.37
E-GEOD-81608no166.45
E-CURD-10no28.32

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

74 targeting PPP1R1A, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-190A-3P100.0080.355520
HSA-MIR-5011-5P100.0083.465820
HSA-MIR-1252-5P100.0069.802774
HSA-MIR-6867-5P100.0082.213464
HSA-MIR-188-3P100.0068.761240
HSA-MIR-314899.9775.066478
HSA-MIR-548AJ-3P99.9673.385345
HSA-MIR-548X-3P99.9673.385345
HSA-MIR-548J-3P99.9472.614881
HSA-MIR-6721-5P99.9368.922981
HSA-MIR-548AE-3P99.9372.664867
HSA-MIR-548AH-3P99.9372.544872
HSA-MIR-548AM-3P99.9372.544872
HSA-MIR-548AQ-3P99.9372.664867
HSA-MIR-464899.9167.00710
HSA-MIR-612499.8769.783551
HSA-MIR-548D-3P99.8770.674362
HSA-MIR-548BB-3P99.8670.584354
HSA-MIR-629-3P99.8567.991875
HSA-MIR-548AC99.8470.774351
HSA-MIR-548H-3P99.8470.804349
HSA-MIR-548Z99.8470.804349
HSA-MIR-6875-3P99.8270.262983
HSA-MIR-4659A-3P99.8072.624248
HSA-MIR-4659B-3P99.8072.624248
HSA-MIR-4668-5P99.7970.583782
HSA-MIR-4713-5P99.7867.801794
HSA-MIR-4446-5P99.7269.192544
HSA-MIR-453099.6966.471509
HSA-MIR-360999.5269.892587

Literature-anchored findings (GeneRIF, showing 10)

  • multiple domains in I-1 target cellular PP1 complexes, and I-1 has a role as a cellular regulator of eIF2alpha phosphorylation (PMID:15345721)
  • G147D PPI-1 can attenuate responses of cardiomyocytes to beta-adrenergic agonists by decreasing PLN phosphorylation and therefore may contribute to deteriorated function in heart failure. (PMID:18192322)
  • the human inhibitor-1 G147D polymorphism, found almost exclusively in blacks, may act as a modifier rather than risk factor in heart failure development (PMID:18698139)
  • I-1 and sarco/endoplasmic reticulum Ca2+ -ATPase synergistically induce the vascular smooth muscle cell contractile phenotype. (PMID:24249716)
  • These findings suggest that the human G109E inhibitor-1 variant impairs sarcoplasmic reticulum Ca-cycling and promotes arrhythmogenesis under stress conditions. (PMID:26455482)
  • High PPP1R1A expression is associated with ewing sarcoma tumorigenesis and metastasis. (PMID:29059150)
  • HOXC-AS3 is aberrantly overexpressed in breast cancers especially the HER2+ type. High expression of HOXC-AS3 has a relationship with poor clinical outcomes of breast cancer. HOXC-AS3 regulates cell invasion and migration both in vitro and in vivo. Results demonstrated that miR-3922-5p was a direct target of HOXC-AS3, and PPP1R1A was a target of miR-3922-5p in breast cancer. (PMID:31797701)
  • The MafA-target gene PPP1R1A regulates GLP1R-mediated amplification of glucose-stimulated insulin secretion in beta-cells. (PMID:33631146)
  • Exploring prognostic value and regulation network of PPP1R1A in hepatocellular carcinoma. (PMID:36018458)
  • Unraveling the significance of PPP1R1A gene in pancreatic beta-cell function: A study in INS-1 cells and human pancreatic islets. (PMID:38574885)

Cross-species orthologs

2 orthologs

OrganismSymbolGene ID
mus_musculusPpp1r1aENSMUSG00000022490
rattus_norvegicusPpp1r1aENSRNOG00000036827

Paralogs (2): PPP1R1B (ENSG00000131771), PPP1R1C (ENSG00000150722)

Protein

Protein identifiers

Protein phosphatase 1 regulatory subunit 1AQ13522 (reviewed: Q13522)

Alternative names: Protein phosphatase inhibitor 1

All UniProt accessions (4): Q13522, F8VR76, H0YIU4, R4GMQ8

UniProt curated annotations — full annotation on UniProt →

Function. Inhibitor of protein-phosphatase 1. This protein may be important in hormonal control of glycogen metabolism. Hormones that elevate intracellular cAMP increase I-1 activity in many tissues. I-1 activation may impose cAMP control over proteins that are not directly phosphorylated by PKA. Following a rise in intracellular calcium, I-1 is inactivated by calcineurin (or PP2B). Does not inhibit type-2 phosphatases.

Subunit / interactions. Interacts with PPP1R15A.

Post-translational modifications. Phosphorylation of Thr-35 is required for activity.

Similarity. Belongs to the protein phosphatase inhibitor 1 family.

RefSeq proteins (1): NP_006732* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR008466PPP1R1A/B/CFamily

Pfam: PF05395

UniProt features (19 total): modified residue 6, region of interest 4, sequence variant 2, mutagenesis site 2, sequence conflict 2, compositionally biased region 2, chain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q13522-F167.330.09

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (6): 46, 47, 67, 1, 35, 43

Mutagenesis-validated functional residues (2):

PositionPhenotype
35no activity.
351000-fold reduction in activity, inhibits equally pp1 and pp2a.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 122 (showing top): GSE18804_SPLEEN_MACROPHAGE_VS_COLON_TUMORAL_MACROPHAGE_DN, MORF_MSH3, MORF_BRCA1, SMID_BREAST_CANCER_RELAPSE_IN_LIVER_UP, SMID_BREAST_CANCER_RELAPSE_IN_LUNG_DN, MORF_RAD51L3, XU_HGF_SIGNALING_NOT_VIA_AKT1_48HR_UP, GOBP_GENERATION_OF_PRECURSOR_METABOLITES_AND_ENERGY, WEI_MYCN_TARGETS_WITH_E_BOX, BLALOCK_ALZHEIMERS_DISEASE_UP, CAIRO_HEPATOBLASTOMA_DN, GOBP_CARBOHYDRATE_METABOLIC_PROCESS, HOSHIDA_LIVER_CANCER_LATE_RECURRENCE_DN, NAKAYAMA_SOFT_TISSUE_TUMORS_PCA2_DN, DOUGLAS_BMI1_TARGETS_UP

GO Biological Process (3): glycogen metabolic process (GO:0005977), intracellular signal transduction (GO:0035556), signal transduction (GO:0007165)

GO Molecular Function (3): protein serine/threonine phosphatase inhibitor activity (GO:0004865), protein phosphatase inhibitor activity (GO:0004864), protein binding (GO:0005515)

GO Cellular Component (1): cytoplasm (GO:0005737)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
intracellular anatomical structure2
energy reserve metabolic process1
glucan metabolic process1
signal transduction1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
protein serine/threonine phosphatase activity1
protein phosphatase inhibitor activity1
phosphoprotein phosphatase activity1
phosphatase inhibitor activity1
protein phosphatase regulator activity1
binding1
cellular anatomical structure1

Protein interactions and networks

STRING

794 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
PPP1R1APPP1R2P41236887
PPP1R1APPP1CCP36873764
PPP1R1APPP1R3AQ16821669
PPP1R1APRKCIP41743649
PPP1R1APPP1CAP08129617
PPP1R1APPP1CBP37140607
PPP1R1ACSRP3P50461567
PPP1R1AGYS1P13807543
PPP1R1AAKAP7O43687540
PPP1R1APRKCAP17252477
PPP1R1ALRATD1Q96KN4467
PPP1R1APPP2CAP05323463
PPP1R1APPP1R15AO75807458
PPP1R1ANAP1L2Q9ULW6427
PPP1R1APNPLA4P41247425

IntAct

20 interactions, top by confidence:

ABTypeScore
SPEM1PPP1R1Apsi-mi:“MI:0915”(physical association)0.560
RRAGANPC2psi-mi:“MI:0914”(association)0.530
SLC25A11POTEIpsi-mi:“MI:0914”(association)0.530
PPP1R1AACTA1psi-mi:“MI:0914”(association)0.530
PPP1R1APPP1R15Apsi-mi:“MI:0915”(physical association)0.510
PPP1R15APPP1R1Apsi-mi:“MI:0915”(physical association)0.510
PPP1R1AGLC7psi-mi:“MI:0915”(physical association)0.370
FGL1DNM1Lpsi-mi:“MI:0914”(association)0.350
ZPBP2PROS1psi-mi:“MI:0914”(association)0.350
SLC25A11YES1psi-mi:“MI:0914”(association)0.350
SPEM1PRG2psi-mi:“MI:0914”(association)0.350
PPP1R1AACTA2psi-mi:“MI:0914”(association)0.350
PRMT6TFCP2psi-mi:“MI:0914”(association)0.350
PRMT6TP73psi-mi:“MI:0914”(association)0.350
ZPBP2PPP1R1Apsi-mi:“MI:0914”(association)0.350

BioGRID (33): PPP1R15A (Two-hybrid), PPP1R15A (Reconstituted Complex), PPP1CA (Reconstituted Complex), PPP1CB (Reconstituted Complex), PPP1CC (Reconstituted Complex), PPP1R15A (Affinity Capture-Western), PPP1R1A (Affinity Capture-MS), PPP1R1A (Affinity Capture-MS), PPP1R1A (Affinity Capture-MS), PPP1R1A (Affinity Capture-MS), PPP1R1A (Affinity Capture-MS), PPP1R1A (Affinity Capture-MS), PPP1R1A (Affinity Capture-MS), ACTA2 (Affinity Capture-MS), ACTA1 (Affinity Capture-MS)

ESM2 similar proteins: A0A1B0GUA9, A0A1B0GV96, A4IFJ0, B3DGJ2, O43687, O55074, O70139, O75167, P04370, P0C8S0, P0C913, P0C914, P0CD96, P19103, P27775, P49342, P61925, P61926, P62025, P63248, P63249, Q04758, Q13522, Q29026, Q3SX13, Q3T0A6, Q3ZB98, Q4VC05, Q5FVI4, Q5R6X9, Q64256, Q6P3A1, Q71U53, Q7M2N1, Q7YQJ3, Q7YQJ4, Q8N111, Q8R409, Q8TAD7, Q8WMS3

Diamond homologs: P01099, P07516, P19103, Q13522, Q29277, Q5R853, Q60829, Q6J4I0, Q8BKK4, Q8WMS3, Q8WVI7, Q9ERT9, Q9UD71

SIGNOR signaling

8 interactions.

AEffectBMechanism
PPP3CBunknownPPP1R1Adephosphorylation
PPP3CCunknownPPP1R1Adephosphorylation
PPP2CBunknownPPP1R1Adephosphorylation
PPP2CAunknownPPP1R1Adephosphorylation
PPP3CAunknownPPP1R1Adephosphorylation
CDK5unknownPPP1R1Aphosphorylation
CalcineurinunknownPPP1R1Adephosphorylation
PP2BunknownPPP1R1Adephosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

32 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance21
Likely benign1
Benign1

Top pathogenic / likely-pathogenic (0)

SpliceAI

1287 predictions. Top by Δscore:

VariantEffectΔscore
12:54575628:GATAG:Gdonor_gain1.0000
12:54575985:A:AGacceptor_gain1.0000
12:54575985:ACT:Aacceptor_gain1.0000
12:54575986:C:Gacceptor_gain1.0000
12:54575987:T:Aacceptor_gain1.0000
12:54575988:GCAGG:Gacceptor_loss1.0000
12:54575990:A:AGacceptor_gain1.0000
12:54575990:AG:Aacceptor_gain1.0000
12:54575991:G:GGacceptor_gain1.0000
12:54575991:GG:Gacceptor_gain1.0000
12:54576099:AGG:Adonor_loss1.0000
12:54576100:GGT:Gdonor_loss1.0000
12:54576101:G:GGdonor_gain1.0000
12:54576102:T:Gdonor_loss1.0000
12:54576665:GAGAA:Gdonor_gain1.0000
12:54576682:G:GTdonor_gain1.0000
12:54576687:A:Tdonor_gain1.0000
12:54576699:GTG:Gdonor_gain1.0000
12:54577212:T:Gacceptor_gain1.0000
12:54577212:T:TAacceptor_gain1.0000
12:54577221:A:AGacceptor_gain1.0000
12:54577221:ACAG:Aacceptor_gain1.0000
12:54577222:C:Gacceptor_gain1.0000
12:54577223:A:AGacceptor_gain1.0000
12:54577223:AG:Aacceptor_gain1.0000
12:54577224:G:GCacceptor_gain1.0000
12:54577224:GG:Gacceptor_gain1.0000
12:54577224:GGC:Gacceptor_gain1.0000
12:54577224:GGCA:Gacceptor_gain1.0000
12:54577224:GGCAT:Gacceptor_gain1.0000

AlphaMissense

1110 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
12:54588453:G:CF12L1.000
12:54588453:G:TF12L1.000
12:54588455:A:GF12L1.000
12:54584308:G:TR33S0.999
12:54584311:G:TR32S0.999
12:54584319:A:GI29T0.999
12:54588454:A:CF12C0.999
12:54588454:A:GF12S0.999
12:54588460:A:GI10T0.999
12:54584295:G:TA37D0.998
12:54584305:G:AP34S0.998
12:54588460:A:CI10S0.998
12:54584305:G:TP34T0.997
12:54584308:G:CR33G0.997
12:54584319:A:CI29S0.997
12:54584304:G:TP34H0.996
12:54584310:C:GR32P0.996
12:54584311:G:CR32G0.996
12:54588455:A:CF12V0.996
12:54588460:A:TI10N0.996
12:54584319:A:TI29N0.995
12:54588416:C:GA25P0.994
12:54588455:A:TF12I0.994
12:54584298:G:TP36H0.993
12:54584312:C:AR31S0.993
12:54584312:C:GR31S0.993
12:54584316:C:GR30P0.993
12:54584317:G:CR30G0.993
12:54584289:A:GL39P0.991
12:54588413:C:GA26P0.991

dbSNP variants (sampled 300 via entrez): RS1000213696 (12:54578918 T>A), RS1000269044 (12:54585543 C>T), RS1000689083 (12:54584381 C>A), RS1000883350 (12:54584796 C>A,T), RS1001010961 (12:54590335 A>AC), RS1001545188 (12:54585008 T>C), RS1001645081 (12:54581351 C>A,T), RS1001826802 (12:54585252 C>A,T), RS1002437358 (12:54585898 A>C,G), RS1002604772 (12:54589742 A>G), RS1002622049 (12:54589519 A>C), RS1003096630 (12:54589155 C>G), RS1003315632 (12:54582871 C>T), RS1003334727 (12:54588263 C>G,T), RS1003618226 (12:54588590 G>C,T)

Disease associations

OMIM: gene MIM:613246 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): rosette-forming glioneuronal tumor of fourth ventricule (MONDO:0016736)

Orphanet (1): Rosette-forming glioneuronal tumor (Orphanet:251975)

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

4 associations (top):

StudyTraitp-value
GCST008151_10Waist circumference6.000000e-06
GCST008157_23Body fat mass8.000000e-06
GCST008160_55Waist circumference6.000000e-06
GCST008162_15Hip circumference3.000000e-06

Drugs & pharmacology

Drug and pharmacology data

Is drug target: no

PharmGKB: 1 entry (VIP=true, CPIC=false)

Binding affinities (BindingDB)

8 measured of 12 human assays (12 total across all organisms); most potent 8 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
Calyculinamide A (18)IC505 nM
C1/C34-Calyculin A (15)IC509 nM
Des-N-methylcalyculin A (20)IC5011 nM
Calyculin A 21-acetate (13)IC5013 nM
Hemicalyculin A (5)IC5014 nM
Calyculin C (24)IC5029 nM
Calyculin J (14)IC50105 nM
Calyculin A (4)IC50112 nM

PubChem BioAssay actives

11 with measured affinity, of 15 total; 8 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
[(2R,3R,7R,8S)-2-[(1S,3S,5R,7E,9E,11E,13E)-15-amino-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyl-15-oxopentadeca-7,9,11,13-tetraenyl]-9-[(E)-3-[2-[4-[[(2S,4S)-4-(dimethylamino)-2,3-dihydroxy-5-methoxypentanoyl]amino]butan-2-yl]-1,3-oxazol-4-yl]prop-2-enyl]-7-hydroxy-4,4,8-trimethyl-1,10-dioxaspiro[4.5]decan-3-yl] dihydrogen phosphate1799476: Inhibition Assay from Article 10.1016/S1074-5521(02)00118-7: “Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.”ic500.0050uM
[(2R,3R,7R,8S)-2-[(1S,3S,5R,7E,9E,11E,13E)-14-cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyltetradeca-7,9,11,13-tetraenyl]-9-[(E)-3-[2-[4-[[(2S,4S)-4-(dimethylamino)-2,3-dihydroxy-5-methoxypentanoyl]amino]butan-2-yl]-1,3-oxazol-4-yl]prop-2-enyl]-7-hydroxy-4,4,8-trimethyl-1,10-dioxaspiro[4.5]decan-3-yl] dihydrogen phosphate1799476: Inhibition Assay from Article 10.1016/S1074-5521(02)00118-7: “Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.”ic500.0082uM
[(2R,3R,7R,8S)-2-[(1S,3S,5R,7E,9E,11E,13E)-14-cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyltetradeca-7,9,11,13-tetraenyl]-7-hydroxy-9-[(E)-3-[2-[4-[(2-hydroxyacetyl)amino]butan-2-yl]-1,3-oxazol-4-yl]prop-2-enyl]-4,4,8-trimethyl-1,10-dioxaspiro[4.5]decan-3-yl] dihydrogen phosphate1799476: Inhibition Assay from Article 10.1016/S1074-5521(02)00118-7: “Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.”ic500.0090uM
[(2R,3R,7R,8S)-2-[(1S,3S,5R,7E,9E,11E,13E)-14-cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyltetradeca-7,9,11,13-tetraenyl]-9-[(E)-3-[2-[4-[[(2S,4S)-2,3-dihydroxy-5-methoxy-4-(methylamino)pentanoyl]amino]butan-2-yl]-1,3-oxazol-4-yl]prop-2-enyl]-7-hydroxy-4,4,8-trimethyl-1,10-dioxaspiro[4.5]decan-3-yl] dihydrogen phosphate1799476: Inhibition Assay from Article 10.1016/S1074-5521(02)00118-7: “Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.”ic500.0110uM
[(2R,3R,7R,8R)-2-[(1S,3S,5R,7E,9E,11E,13E)-14-cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyltetradeca-7,9,11,13-tetraenyl]-9-[(E)-3-[2-[4-[[(2S,4S)-4-(dimethylamino)-2,3-dihydroxy-5-methoxypentanoyl]amino]butan-2-yl]-1,3-oxazol-4-yl]prop-2-enyl]-4,4,8-trimethyl-3-phosphonooxy-1,10-dioxaspiro[4.5]decan-7-yl] acetate1799476: Inhibition Assay from Article 10.1016/S1074-5521(02)00118-7: “Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.”ic500.0130uM
[(2R,3R,7R,8S)-2-[(1S,3S,5R,7E,9E,11E,13E)-14-cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyltetradeca-7,9,11,13-tetraenyl]-9-[(E)-3-cyanoprop-2-enyl]-7-hydroxy-4,4,8-trimethyl-1,10-dioxaspiro[4.5]decan-3-yl] dihydrogen phosphate1799476: Inhibition Assay from Article 10.1016/S1074-5521(02)00118-7: “Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.”ic500.0140uM
[(2R,3R,7R,8S)-2-[(1S,3S,5R,7E,9E,11E,13E)-14-cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyltetradeca-7,9,11,13-tetraenyl]-9-[(E)-3-[2-[4-[[(2S,4S)-4-(dimethylamino)-2,3-dihydroxy-5-methoxypentanoyl]amino]pentan-2-yl]-1,3-oxazol-4-yl]prop-2-enyl]-7-hydroxy-4,4,8-trimethyl-1,10-dioxaspiro[4.5]decan-3-yl] dihydrogen phosphate1799476: Inhibition Assay from Article 10.1016/S1074-5521(02)00118-7: “Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.”ic500.0290uM
[(2R,3R)-2-[(1S,3S)-4-[(3S,4R)-4-bromo-5-[(2E,4E,6E)-7-cyano-6-methylhepta-2,4,6-trien-2-yl]-3,5-dimethyloxolan-2-yl]-3-hydroxy-1-methoxypentyl]-5-[(E)-4-[2-[4-[[(2S,4S)-4-(dimethylamino)-2,3-dihydroxy-5-methoxypentanoyl]amino]butan-2-yl]-1,3-oxazol-4-yl]but-3-enoxy]-5-[(2S)-2-hydroxybutyl]-4,4-dimethyloxolan-3-yl] dihydrogen phosphate1799476: Inhibition Assay from Article 10.1016/S1074-5521(02)00118-7: “Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.”ic500.1050uM

CTD chemical–gene interactions

55 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Benzo(a)pyrenedecreases expression, increases methylation4
Valproic Acidaffects cotreatment, increases expression, affects expression4
bisphenol Aaffects cotreatment, increases methylation, increases expression3
Acetaminophendecreases expression, increases expression3
Aflatoxin B1affects expression, decreases expression, decreases methylation3
mercuric bromideaffects cotreatment, decreases expression2
Panobinostataffects cotreatment, increases expression2
Dexamethasoneincreases expression, affects cotreatment2
Estradiolincreases expression, decreases expression2
Phenylmercuric Acetateaffects cotreatment, decreases expression2
Triclosanaffects cotreatment, decreases expression2
Cyclosporinedecreases expression, increases expression2
methylmercuric chloridedecreases expression1
methyleugenoldecreases expression1
triphenyl phosphateincreases expression1
terbufosincreases methylation1
trichostatin Aincreases expression1
sodium arsenitedecreases expression1
perfluoro-n-nonanoic aciddecreases expression1
entinostatincreases expression, affects cotreatment1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamidedecreases expression, affects cotreatment, increases expression1
dorsomorphinaffects cotreatment, increases expression, decreases expression1
bisphenol Sdecreases methylation1
(+)-JQ1 compounddecreases expression1
Rosiglitazonedecreases expression1
Resveratrolaffects cotreatment, decreases expression1
Sunitinibdecreases expression1
Zoledronic Aciddecreases expression1
Fulvestrantaffects cotreatment, increases methylation1
Troglitazoneincreases expression1

Cellosaurus cell lines

4 cell lines: 4 cancer cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_TF70HAP1 PPP1R1A (-) 1Cancer cell lineMale
CVCL_TF71HAP1 PPP1R1A (-) 2Cancer cell lineMale
CVCL_TF72HAP1 PPP1R1A (-) 3Cancer cell lineMale
CVCL_TF73HAP1 PPP1R1A (-) 4Cancer cell lineMale

Clinical trials (associated diseases)

1 trials via MONDO — disease-level, not drug-specific.

TrialPhaseStatusTitle
NCT03975829PHASE4RECRUITINGPediatric Long-Term Follow-up and Rollover Study