General Information of Target

Target ID LDTP07217
Target Name Zinc finger protein Gfi-1b (GFI1B)
Gene Name GFI1B
Gene ID 8328
Synonyms
Zinc finger protein Gfi-1b; Growth factor independent protein 1B; Potential regulator of CDKN1A translocated in CML
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPRSFLVKSKKAHTYHQPRVQEDEPLWPPALTPVPRDQAPSNSPVLSTLFPNQCLDWTNL
KREPELEQDQNLARMAPAPEGPIVLSRPQDGDSPLSDSPPFYKPSFSWDTLATTYGHSYR
QAPSTMQSAFLEHSVSLYGSPLVPSTEPALDFSLRYSPGMDAYHCVKCNKVFSTPHGLEV
HVRRSHSGTRPFACDICGKTFGHAVSLEQHTHVHSQERSFECRMCGKAFKRSSTLSTHLL
IHSDTRPYPCQFCGKRFHQKSDMKKHTYIHTGEKPHKCQVCGKAFSQSSNLITHSRKHTG
FKPFSCELCTKGFQRKVDLRRHRESQHNLK
Target Bioclass
Transcription factor
Subcellular location
Nucleus
Function
Essential proto-oncogenic transcriptional regulator necessary for development and differentiation of erythroid and megakaryocytic lineages. Component of a RCOR-GFI-KDM1A-HDAC complex that suppresses, via histone deacetylase (HDAC) recruitment, a number of genes implicated in multilineage blood cell development and controls hematopoietic differentiation. Transcriptional repressor or activator depending on both promoter and cell type context; represses promoter activity of SOCS1 and SOCS3 and thus, may regulate cytokine signaling pathways. Cooperates with GATA1 to repress target gene transcription, such as the apoptosis regulator BCL2L1; GFI1B silencing in leukemic cell lines markedly increase apoptosis rate. Inhibits down-regulation of MYC and MYB as well as the cyclin-dependent kinase inhibitor CDKN1A/P21WAF1 in IL6-treated myelomonocytic cells. Represses expression of GATA3 in T-cell lymphomas and inhibits GATA1-mediated transcription; as GATA1 also mediates erythroid GFI1B transcription, both GATA1 and GFI1B participate in a feedback regulatory pathway controlling the expression of GFI1B gene in erythroid cells. Suppresses GATA1-mediated stimulation of GFI1B promoter through protein interaction. Binds to gamma-satellite DNA and to its own promoter, auto-repressing its own expression. Alters histone methylation by recruiting histone methyltransferase to target genes promoters. Plays a role in heterochromatin formation.
Uniprot ID
Q5VTD9
Ensemble ID
ENST00000339463.7
HGNC ID
HGNC:4238

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.V182M .
A375 SNV: p.T125P .
HCT116 SNV: p.G226D .
Ishikawa (Heraklio) 02 ER SNV: p.Q21R .
JURLMK1 SNV: p.H322R .
MCC13 SNV: p.H294Y .
SW1116 SNV: p.Y248S .
YSCCC SNV: p.S93C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C54(1.05); C165(1.16)  LDD2324  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 EoL-1 C54(1.05); C165(1.16)  LDD2324  [1]
 LDCM0023  KB03 EoL-1 C54(1.43); C165(1.36)  LDD2741  [1]
 LDCM0024  KB05 EoL-1 C54(1.05); C165(1.23)  LDD3158  [1]

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