General Information of Target

Target ID LDTP12901
Target Name Grainyhead-like protein 1 homolog (GRHL1)
Gene Name GRHL1
Gene ID 29841
Synonyms
LBP32; MGR; TFCP2L2; Grainyhead-like protein 1 homolog; Mammalian grainyhead; NH32; Transcription factor CP2-like 2; Transcription factor LBP-32
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGAVMGTFSSLQTKQRRPSKDIAWWYYQYQRDKIEDELEMTMVCHRPEGLEQLEAQTNFT
KRELQVLYRGFKNECPSGVVNEDTFKQIYAQFFPHGDASTYAHYLFNAFDTTQTGSVKFE
DFVTALSILLRGTVHEKLRWTFNLYDINKDGYINKEEMMDIVKAIYDMMGKYTYPVLKED
TPRQHVDVFFQKMDKNKDGIVTLDEFLESCQEDDNIMRSLQLFQNVM
Target Bioclass
Transcription factor
Family
Grh/CP2 family, Grainyhead subfamily
Subcellular location
Nucleus
Function
Transcription factor involved in epithelial development. Binds directly to the consensus DNA sequence 5'-AACCGGTT-3'. Important regulator of DSG1 in the context of hair anchorage and epidermal differentiation, participates in the maintenance of the skin barrier. There is no genetic interaction with GRHL3, nor functional cooperativity due to diverse target gene selectivity during epithelia development. May play a role in regulating glucose homeostasis and insulin signaling.; [Isoform 1]: Functions as a transcription activator.; [Isoform 2]: May function as a repressor in tissues where both isoform 1 and isoform 2 are expressed.
Uniprot ID
Q9NZI5
Ensemble ID
ENST00000324907.14
HGNC ID
HGNC:17923

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 SNV: p.E597K .
HT115 SNV: p.V221A .
OVK18 Deletion: p.S610LfsTer6 .
RKO SNV: p.I560F .
RVH421 Substitution: p.G608K .
TOV21G SNV: p.D6Y .
U2OS Insertion: p.Y65WfsTer39
SNV: p.T27N
.
YSCCC SNV: p.I582M .

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 
C335(4.49)  LDD3319  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 AU565 C335(2.91)  LDD2265  [1]
 LDCM0023  KB03 AU565 C335(4.36)  LDD2682  [1]
 LDCM0024  KB05 MEWO C335(4.49)  LDD3319  [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