Details of the Target

General Information of Target

Target ID LDTP09802
Target Name Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3)
Gene Name PIK3R3
Gene ID 8503
Synonyms
Phosphatidylinositol 3-kinase regulatory subunit gamma; PI3-kinase regulatory subunit gamma; PI3K regulatory subunit gamma; PtdIns-3-kinase regulatory subunit gamma; Phosphatidylinositol 3-kinase 55 kDa regulatory subunit gamma; PI3-kinase subunit p55-gamma; PtdIns-3-kinase regulatory subunit p55-gamma; p55PIK
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNPVYSPVQPGAPYGNPKNMAYTGYPTAYPAAAPAYNPSLYPTNSPSYAPEFQFLHSAYA
TLLMKQAWPQNSSSCGTEGTFHLPVDTGTENRTYQASSAAFRYTAGTPYKVPPTQSNTAP
PPYSPSPNPYQTAMYPIRSAYPQQNLYAQGAYYTQPVYAAQPHVIHHTTVVQPNSIPSAI
YPAPVAAPRTNGVAMGMVAGTTMAMSAGTLLTTPQHTAIGAHPVSMPTYRAQGTPAYSYV
PPHW
Target Bioclass
Other
Family
PI3K p85 subunit family
Function Binds to activated (phosphorylated) protein-tyrosine kinases through its SH2 domain and regulates their kinase activity. During insulin stimulation, it also binds to IRS-1.
Uniprot ID
Q92569
Ensemble ID
ENST00000262741.10
HGNC ID
HGNC:8981
ChEMBL ID
CHEMBL3559703

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT116 Deletion: p.M96CfsTer7 .
KMCH1 SNV: p.A48V .
NCIH661 SNV: p.P351A .
ONS76 SNV: p.Y240N; p.M456L .
OVK18 SNV: p.P127H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C230(1.47)  LDD3403  [1]
N1
 Probe Info  		N.A.  LDD0245  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 697 C230(1.21)  LDD2245  [1]
 LDCM0023  KB03 697 C230(1.35)  LDD2662  [1]
 LDCM0024  KB05 Reh C230(1.47)  LDD3403  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 20 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adenine nucleotide translocase lysine N-methyltransferase (ANTKMT) ANT/ATPSC lysine N-methyltransferase family Q9BQD7
Phospholipase A and acyltransferase 4 (PLAAT4) H-rev107 family Q9UL19
E3 ubiquitin-protein ligase pellino homolog 3 (PELI3) Pellino family Q8N2H9
OTU domain-containing protein 7B (OTUD7B) Peptidase C64 family Q6GQQ9
Cytosol aminopeptidase (LAP3) Peptidase M17 family P28838
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA) PI3/PI4-kinase family P42336
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PIK3CB) PI3/PI4-kinase family P42338
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PIK3CD) PI3/PI4-kinase family O00329
Hepatocyte growth factor receptor (MET) Tyr protein kinase family P08581
Mast/stem cell growth factor receptor Kit (KIT) Tyr protein kinase family P10721
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Receptor tyrosine-protein kinase erbB-2 (ERBB2) Tyr protein kinase family P04626
Receptor tyrosine-protein kinase erbB-3 (ERBB3) Tyr protein kinase family P21860
Focal adhesion kinase 1 (PTK2) Tyr protein kinase family Q05397
Proto-oncogene tyrosine-protein kinase Src (SRC) Tyr protein kinase family P12931
Tyrosine-protein kinase Blk (BLK) Tyr protein kinase family P51451
Tyrosine-protein kinase Yes (YES1) Tyr protein kinase family P07947
SPRY domain-containing SOCS box protein 2 (SPSB2) SPSB family Q99619
E3 ubiquitin-protein ligase CBL (CBL) . P22681
Methyltransferase-like protein 27 (METTL27) . Q8N6F8
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 620 (ZNF620) Krueppel C2H2-type zinc-finger protein family Q6ZNG0
Zinc finger and BTB domain-containing protein 18 (ZBTB18) Krueppel C2H2-type zinc-finger protein family Q99592
Dr1-associated corepressor (DRAP1) NC2 alpha/DRAP1 family Q14919
Androgen receptor (AR) Nuclear hormone receptor family P10275
Pre-B-cell leukemia transcription factor 4 (PBX4) TALE/PBX homeobox family Q9BYU1
Signal transducer and activator of transcription 5B (STAT5B) Transcription factor STAT family P51692
Golgin-45 (BLZF1) . Q9H2G9
Oligodendrocyte transcription factor 1 (OLIG1) . Q8TAK6
Other
Click To Hide/Show 30 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Abl interactor 1 (ABI1) ABI family Q8IZP0
Beta-crystallin A2 (CRYBA2) Beta/gamma-crystallin family P53672
Retinoid-binding protein 7 (RBP7) Fatty-acid binding protein (FABP) family Q96R05
cAMP-dependent protein kinase type I-beta regulatory subunit (PRKAR1B) CAMP-dependent kinase regulatory chain family P31321
Coiled-coil domain-containing protein 89 (CCDC89) CCDC89 family Q8N998
Centrosomal protein of 19 kDa (CEP19) CEP19 family Q96LK0
Adapter molecule crk (CRK) CRK family P46108
GRB2-associated-binding protein 1 (GAB1) GAB family Q13480
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
NGFI-A-binding protein 2 (NAB2) NAB family Q15742
Sperm microtubule inner protein 6 (SPMIP6) SMRP1 family Q8NCR6
Protein TASOR 2 (TASOR2) TASOR family Q5VWN6
Tetraspanin-2 (TSPAN2) Tetraspanin (TM4SF) family O60636
Troponin I, slow skeletal muscle (TNNI1) Troponin I family P19237
AP-4 complex accessory subunit RUSC1 (RUSC1) . Q9BVN2
Centromere protein R (ITGB3BP) . Q13352
Enkurin domain-containing protein 1 (ENKD1) . Q9H0I2
Fibroblast growth factor receptor substrate 3 (FRS3) . O43559
Fibronectin type III domain-containing protein 8 (FNDC8) . Q8TC99
Insulin receptor substrate 1 (IRS1) . P35568
Nebulette (NEBL) . O76041
Pleckstrin homology domain-containing family F member 2 (PLEKHF2) . Q9H8W4
SERTA domain-containing protein 2 (SERTAD2) . Q14140
SH2 domain-containing protein 2A (SH2D2A) . Q9NP31
Single-stranded DNA-binding protein 4 (SSBP4) . Q9BWG4
Spermatogenesis-associated protein 32 (SPATA32) . Q96LK8
Suppressor of cytokine signaling 4 (SOCS4) . Q8WXH5
Uncharacterized protein C3orf36 (C3orf36) . Q3SXR2
Uncharacterized protein KIAA0408 (KIAA0408) . Q6ZU52
WD repeat and FYVE domain-containing protein 3 (WDFY3) . Q8IZQ1

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sf1126 Small molecular drug DB05210

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.