Details of the Target

General Information of Target

Target ID LDTP00774
Target Name Krueppel-like factor 4 (KLF4)
Gene Name KLF4
Gene ID 9314
Synonyms
EZF; GKLF; Krueppel-like factor 4; Epithelial zinc finger protein EZF; Gut-enriched krueppel-like factor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRQPPGESDMAVSDALLPSFSTFASGPAGREKTLRQAGAPNNRWREELSHMKRLPPVLPG
RPYDLAAATVATDLESGGAGAACGGSNLAPLPRRETEEFNDLLDLDFILSNSLTHPPESV
AATVSSSASASSSSSPSSSGPASAPSTCSFTYPIRAGNDPGVAPGGTGGGLLYGRESAPP
PTAPFNLADINDVSPSGGFVAELLRPELDPVYIPPQQPQPPGGGLMGKFVLKASLSAPGS
EYGSPSVISVSKGSPDGSHPVVVAPYNGGPPRTCPKIKQEAVSSCTHLGAGPPLSNGHRP
AAHDFPLGRQLPSRTTPTLGLEEVLSSRDCHPALPLPPGFHPHPGPNYPSFLPDQMQPQV
PPLHYQGQSRGFVARAGEPCVCWPHFGTHGMMLTPPSSPLELMPPGSCMPEEPKPKRGRR
SWPRKRTATHTCDYAGCGKTYTKSSHLKAHLRTHTGEKPYHCDWDGCGWKFARSDELTRH
YRKHTGHRPFQCQKCDRAFSRSDHLALHMKRHF
Target Type
Clinical trial
Target Bioclass
Transcription factor
Family
Krueppel C2H2-type zinc-finger protein family
Subcellular location
Nucleus
Function
Transcription factor; can act both as activator and as repressor. Binds the 5'-CACCC-3' core sequence. Binds to the promoter region of its own gene and can activate its own transcription. Regulates the expression of key transcription factors during embryonic development. Plays an important role in maintaining embryonic stem cells, and in preventing their differentiation. Required for establishing the barrier function of the skin and for postnatal maturation and maintenance of the ocular surface. Involved in the differentiation of epithelial cells and may also function in skeletal and kidney development. Contributes to the down-regulation of p53/TP53 transcription.
TTD ID
T81916
Uniprot ID
O43474
DrugMap ID
TTTI53X
Ensemble ID
ENST00000374672.5
HGNC ID
HGNC:6348

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 Substitution: p.L172F .
DU145 SNV: p.P312H; p.D441Y .
HCT116 SNV: p.N347S .
HT29 SNV: p.Y348S .
ICC9 SNV: p.K409Q .
IGROV1 SNV: p.S468L .
MELJUSO SNV: p.R390W .
MFE319 SNV: p.G26D .
SNGM SNV: p.A68T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Probe 1
 Probe Info  		Y173(9.68)  LDD3495  [1]
NAIA_5
 Probe Info  		C83(0.79)  LDD2227  [2]
IA-alkyne
 Probe Info  		C432(10.99)  LDD1705  [3]
IPM
 Probe Info  		N.A.  LDD0147  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0632  CL-Sc Hep-G2 C83(0.79)  LDD2227  [2]
 LDCM0024  KB05 T cell C432(10.99)  LDD1705  [3]

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
C-terminal-binding protein 1 (CTBP1) D-isomer specific 2-hydroxyacid dehydrogenase family Q13363
Glycogen [starch] synthase, muscle (GYS1) Glycosyltransferase 3 family P13807
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Paired box protein Pax-9 (PAX9) . P55771
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Segment polarity protein dishevelled homolog DVL-3 (DVL3) DSH family Q92997
Heat shock factor 2-binding protein (HSF2BP) . O75031
Hepatocyte growth factor-regulated tyrosine kinase substrate (HGS) . O14964
Methyl-CpG-binding domain protein 3 (MBD3) . O95983

The Drug(s) Related To This Target

Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Apto-253 . D07TRP

References

1 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.
2 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
3 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
4 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