Details of the Target

General Information of Target

Target ID LDTP03971
Target Name Signal transducer and activator of transcription 5A (STAT5A)
Gene Name STAT5A
Gene ID 6776
Synonyms
STAT5; Signal transducer and activator of transcription 5A
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGWIQAQQLQGDALRQMQVLYGQHFPIEVRHYLAQWIESQPWDAIDLDNPQDRAQATQL
LEGLVQELQKKAEHQVGEDGFLLKIKLGHYATQLQKTYDRCPLELVRCIRHILYNEQRLV
REANNCSSPAGILVDAMSQKHLQINQTFEELRLVTQDTENELKKLQQTQEYFIIQYQESL
RIQAQFAQLAQLSPQERLSRETALQQKQVSLEAWLQREAQTLQQYRVELAEKHQKTLQLL
RKQQTIILDDELIQWKRRQQLAGNGGPPEGSLDVLQSWCEKLAEIIWQNRQQIRRAEHLC
QQLPIPGPVEEMLAEVNATITDIISALVTSTFIIEKQPPQVLKTQTKFAATVRLLVGGKL
NVHMNPPQVKATIISEQQAKSLLKNENTRNECSGEILNNCCVMEYHQATGTLSAHFRNMS
LKRIKRADRRGAESVTEEKFTVLFESQFSVGSNELVFQVKTLSLPVVVIVHGSQDHNATA
TVLWDNAFAEPGRVPFAVPDKVLWPQLCEALNMKFKAEVQSNRGLTKENLVFLAQKLFNN
SSSHLEDYSGLSVSWSQFNRENLPGWNYTFWQWFDGVMEVLKKHHKPHWNDGAILGFVNK
QQAHDLLINKPDGTFLLRFSDSEIGGITIAWKFDSPERNLWNLKPFTTRDFSIRSLADRL
GDLSYLIYVFPDRPKDEVFSKYYTPVLAKAVDGYVKPQIKQVVPEFVNASADAGGSSATY
MDQAPSPAVCPQAPYNMYPQNPDHVLDQDGEFDLDETMDVARHVEELLRRPMDSLDSRLS
PPAGLFTSARGSLS
Target Bioclass
Transcription factor
Family
Transcription factor STAT family
Subcellular location
Cytoplasm
Function
Carries out a dual signal transduction and activation of transcription. Mediates cellular responses to the cytokine KITLG/SCF and other growth factors. Mediates cellular responses to ERBB4. May mediate cellular responses to activated FGFR1, FGFR2, FGFR3 and FGFR4. Binds to the GAS element and activates PRL-induced transcription. Regulates the expression of milk proteins during lactation.
Uniprot ID
P42229
Ensemble ID
ENST00000345506.8
HGNC ID
HGNC:11366
ChEMBL ID
CHEMBL5403

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.W484C .
AN3CA Insertion: p.Q368PfsTer9 .
JURKAT Deletion: p.Q368RfsTer2 .
KATOIII Insertion: p.R769TfsTer8 DBIA    Probe Info 
KMS27 SNV: p.I38F .
LNCaP clone FGC SNV: p.I85N .
LS180 Deletion: p.Q368RfsTer2 .
MOLT4 SNV: p.C508F; p.A789T .
NCIH1155 SNV: p.Q117Ter .
NCIH196 SNV: p.G431A .
NUGC3 SNV: p.A517T .
U937 SNV: p.N642H DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-EBA
 Probe Info  		4.04  LDD0215  [1]
TH211
 Probe Info  		Y694(16.42)  LDD0260  [2]
Probe 1
 Probe Info  		Y225(15.00)  LDD3495  [3]
DBIA
 Probe Info  		C101(1.43)  LDD3316  [4]
AHL-Pu-1
 Probe Info  		C101(2.16)  LDD0171  [5]
HHS-482
 Probe Info  		Y694(1.17)  LDD0285  [6]
HHS-475
 Probe Info  		Y694(0.86)  LDD0264  [7]
IPM
 Probe Info  		C101(1.07)  LDD1701  [8]
TFBX
 Probe Info  		N.A.  LDD0148  [9]
HHS-465
 Probe Info  		Y694(0.00); Y114(0.00); K696(0.00)  LDD2240  [10]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe11
 Probe Info  		5.98  LDD0472  [11]
FFF probe13
 Probe Info  		9.37  LDD0476  [11]
FFF probe3
 Probe Info  		8.06  LDD0465  [11]
DA-2
 Probe Info  		N.A.  LDD0073  [12]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA DM93 C101(2.16)  LDD0171  [5]
 LDCM0116  HHS-0101 DM93 Y694(0.86)  LDD0264  [7]
 LDCM0117  HHS-0201 DM93 Y694(0.65)  LDD0265  [7]
 LDCM0118  HHS-0301 DM93 Y694(0.71)  LDD0266  [7]
 LDCM0119  HHS-0401 DM93 Y694(0.87)  LDD0267  [7]
 LDCM0120  HHS-0701 DM93 Y694(0.85)  LDD0268  [7]
 LDCM0123  JWB131 DM93 Y694(1.17)  LDD0285  [6]
 LDCM0124  JWB142 DM93 Y694(0.74)  LDD0286  [6]
 LDCM0125  JWB146 DM93 Y694(0.82)  LDD0287  [6]
 LDCM0126  JWB150 DM93 Y694(5.05)  LDD0288  [6]
 LDCM0127  JWB152 DM93 Y694(2.96)  LDD0289  [6]
 LDCM0128  JWB198 DM93 Y694(1.90)  LDD0290  [6]
 LDCM0129  JWB202 DM93 Y694(0.64)  LDD0291  [6]
 LDCM0130  JWB211 DM93 Y694(1.22)  LDD0292  [6]
 LDCM0022  KB02 697 C101(4.03)  LDD2245  [4]
 LDCM0023  KB03 MDA-MB-231 C101(1.07)  LDD1701  [8]
 LDCM0024  KB05 MEL167 C101(1.43)  LDD3316  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Tyrosine-protein phosphatase non-receptor type 1 (PTPN1) Protein-tyrosine phosphatase family P18031
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transcription factor 12 (TCF12) . Q99081

References

1 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
2 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
3 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
4 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
5 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
6 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
7 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
8 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
9 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
10 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
11 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
12 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.