General Information of Target

Target ID LDTP03645
Target Name Sodium/calcium exchanger 1 (SLC8A1)
Gene Name SLC8A1
Gene ID 6546
Synonyms
CNC; NCX1; Sodium/calcium exchanger 1; Na(+)/Ca(2+)-exchange protein 1; Solute carrier family 8 member 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MYNMRRLSLSPTFSMGFHLLVTVSLLFSHVDHVIAETEMEGEGNETGECTGSYYCKKGVI
LPIWEPQDPSFGDKIARATVYFVAMVYMFLGVSIIADRFMSSIEVITSQEKEITIKKPNG
ETTKTTVRIWNETVSNLTLMALGSSAPEILLSVIEVCGHNFTAGDLGPSTIVGSAAFNMF
IIIALCVYVVPDGETRKIKHLRVFFVTAAWSIFAYTWLYIILSVISPGVVEVWEGLLTFF
FFPICVVFAWVADRRLLFYKYVYKRYRAGKQRGMIIEHEGDRPSSKTEIEMDGKVVNSHV
ENFLDGALVLEVDERDQDDEEARREMARILKELKQKHPDKEIEQLIELANYQVLSQQQKS
RAFYRIQATRLMTGAGNILKRHAADQARKAVSMHEVNTEVTENDPVSKIFFEQGTYQCLE
NCGTVALTIIRRGGDLTNTVFVDFRTEDGTANAGSDYEFTEGTVVFKPGDTQKEIRVGII
DDDIFEEDENFLVHLSNVKVSSEASEDGILEANHVSTLACLGSPSTATVTIFDDDHAGIF
TFEEPVTHVSESIGIMEVKVLRTSGARGNVIVPYKTIEGTARGGGEDFEDTCGELEFQND
EIVKTISVKVIDDEEYEKNKTFFLEIGEPRLVEMSEKKALLLNELGGFTITGKYLFGQPV
FRKVHAREHPILSTVITIADEYDDKQPLTSKEEEERRIAEMGRPILGEHTKLEVIIEESY
EFKSTVDKLIKKTNLALVVGTNSWREQFIEAITVSAGEDDDDDECGEEKLPSCFDYVMHF
LTVFWKVLFAFVPPTEYWNGWACFIVSILMIGLLTAFIGDLASHFGCTIGLKDSVTAVVF
VALGTSVPDTFASKVAATQDQYADASIGNVTGSNAVNVFLGIGVAWSIAAIYHAANGEQF
KVSPGTLAFSVTLFTIFAFINVGVLLYRRRPEIGGELGGPRTAKLLTSCLFVLLWLLYIF
FSSLEAYCHIKGF
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Ca(2+):cation antiporter (CaCA) (TC 2.A.19) family, SLC8 subfamily
Subcellular location
Cell membrane
Function
Mediates the exchange of one Ca(2+) ion against three to four Na(+) ions across the cell membrane, and thereby contributes to the regulation of cytoplasmic Ca(2+) levels and Ca(2+)-dependent cellular processes. Contributes to Ca(2+) transport during excitation-contraction coupling in muscle. In a first phase, voltage-gated channels mediate the rapid increase of cytoplasmic Ca(2+) levels due to release of Ca(2+) stores from the endoplasmic reticulum. SLC8A1 mediates the export of Ca(2+) from the cell during the next phase, so that cytoplasmic Ca(2+) levels rapidly return to baseline. Required for normal embryonic heart development and the onset of heart contractions.
TTD ID
T07775
Uniprot ID
P32418
DrugMap ID
TTCF82X
Ensemble ID
ENST00000332839.9
HGNC ID
HGNC:11068
ChEMBL ID
CHEMBL4076

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
42MGBA SNV: p.V21L .
A375 SNV: p.G193E .
CAL51 SNV: p.E694G .
CALU1 SNV: p.T836I .
CHL1 SNV: p.G934E .
COLO792 SNV: p.A512V .
DEL SNV: p.S211R .
EFO27 SNV: p.F27L .
HCT15 SNV: p.P793S .
HKGZCC SNV: p.C765W .
HUH1 SNV: p.D292Y .
LN229 SNV: p.E148D .
LNCaP clone FGC SNV: p.A666V .
LS123 SNV: p.A857G .
MCC13 SNV: p.G881Ter .
NALM6 SNV: p.Q335H .
NCIH2172 SNV: p.K408Ter; p.Y654C .
NCIH23 SNV: p.G800C .
NUGC3 SNV: p.T912I .
OE33 Deletion: p.E695del .
RKO SNV: p.E321K; p.G568E .
SW1573 SNV: p.K620R .
SW620 SNV: p.T906I .
T98G SNV: p.Q747H .
YSCCC SNV: p.D488N .

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
YN-1
 Probe Info 
N.A.  LDD0446  [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
Protein S100-A1 (S100A1) S-100 family P23297
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein S100-A5 (S100A5) S-100 family P33763

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alpha-linolenic Acid Small molecular drug DB00132
Calcium Phosphate Small molecular drug DB11348
Calcium Phosphate Dihydrate Small molecular drug DB14481
Dronedarone Small molecular drug DB04855
Icosapent Small molecular drug DB00159
Calcium Citrate . DB11093
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Caldaret . DB06231

References

1 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.