General Information of Target

Target ID LDTP15361
Target Name Protein Aster-C (GRAMD1C)
Gene Name GRAMD1C
Gene ID 54762
Synonyms
Protein Aster-C; GRAM domain-containing protein 1C
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQKSCEENEGKPQNMPKAEEDRPLEDVPQEAEGNPQPSEEGVSQEAEGNPRGGPNQPGQG
FKEDTPVRHLDPEEMIRGVDELERLREEIRRVRNKFVMMHWKQRHSRSRPYPVCFRP
Target Bioclass
Transporter and channel
Subcellular location
Endoplasmic reticulum membrane
Function
Cholesterol transporter that mediates non-vesicular transport of cholesterol from the plasma membrane (PM) to the endoplasmic reticulum (ER). Contains unique domains for binding cholesterol and the PM, thereby serving as a molecular bridge for the transfer of cholesterol from the PM to the ER. Plays a crucial role in cholesterol homeostasis and has the unique ability to localize to the PM based on the level of membrane cholesterol. In lipid-poor conditions localizes to the ER membrane and in response to excess cholesterol in the PM is recruited to the endoplasmic reticulum-plasma membrane contact sites (EPCS) which is mediated by the GRAM domain. At the EPCS, the sterol-binding VASt/ASTER domain binds to the cholesterol in the PM and facilitates its transfer from the PM to ER.
Uniprot ID
Q8IYS0
Ensemble ID
ENST00000358160.9
HGNC ID
HGNC:25252

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
FUOV1 SNV: p.C439R .
HCC15 SNV: p.G263R .
HT115 SNV: p.K472N .
NCIH2286 SNV: p.Y71H .
OVCAR8 SNV: p.G14V .
P31FUJ SNV: p.E27G .
RL952 SNV: p.V34M .
SNU1079 SNV: p.N208H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C396(1.16)  LDD3224  [1]
CY-1
 Probe Info 
N.A.  LDD0246  [2]
YN-1
 Probe Info 
N.A.  LDD0447  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0024  KB05 ICC26 C396(1.16)  LDD3224  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
CD151 antigen (CD151) Tetraspanin (TM4SF) family P48509
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
B-cell differentiation antigen CD72 (CD72) . P21854

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.
3 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.