Details of the Target

General Information of Target

Target ID LDTP06497
Target Name Voltage-dependent R-type calcium channel subunit alpha-1E (CACNA1E)
Gene Name CACNA1E
Gene ID 777
Synonyms
CACH6; CACNL1A6; Voltage-dependent R-type calcium channel subunit alpha-1E; Brain calcium channel II; BII; Calcium channel, L type, alpha-1 polypeptide, isoform 6; Voltage-gated calcium channel subunit alpha Cav2.3
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MARFGEAVVARPGSGDGDSDQSRNRQGTPVPASGQAAAYKQTKAQRARTMALYNPIPVRQ
NCFTVNRSLFIFGEDNIVRKYAKKLIDWPPFEYMILATIIANCIVLALEQHLPEDDKTPM
SRRLEKTEPYFIGIFCFEAGIKIVALGFIFHKGSYLRNGWNVMDFIVVLSGILATAGTHF
NTHVDLRTLRAVRVLRPLKLVSGIPSLQIVLKSIMKAMVPLLQIGLLLFFAILMFAIIGL
EFYSGKLHRACFMNNSGILEGFDPPHPCGVQGCPAGYECKDWIGPNDGITQFDNILFAVL
TVFQCITMEGWTTVLYNTNDALGATWNWLYFIPLIIIGSFFVLNLVLGVLSGEFAKERER
VENRRAFMKLRRQQQIERELNGYRAWIDKAEEVMLAEENKNAGTSALEVLRRATIKRSRT
EAMTRDSSDEHCVDISSVGTPLARASIKSAKVDGVSYFRHKERLLRISIRHMVKSQVFYW
IVLSLVALNTACVAIVHHNQPQWLTHLLYYAEFLFLGLFLLEMSLKMYGMGPRLYFHSSF
NCFDFGVTVGSIFEVVWAIFRPGTSFGISVLRALRLLRIFKITKYWASLRNLVVSLMSSM
KSIISLLFLLFLFIVVFALLGMQLFGGRFNFNDGTPSANFDTFPAAIMTVFQILTGEDWN
EVMYNGIRSQGGVSSGMWSAIYFIVLTLFGNYTLLNVFLAIAVDNLANAQELTKDEQEEE
EAFNQKHALQKAKEVSPMSAPNMPSIERDRRRRHHMSMWEPRSSHLRERRRRHHMSVWEQ
RTSQLRKHMQMSSQEALNREEAPTMNPLNPLNPLSSLNPLNAHPSLYRRPRAIEGLALGL
ALEKFEEERISRGGSLKGDGGDRSSALDNQRTPLSLGQREPPWLARPCHGNCDPTQQEAG
GGEAVVTFEDRARHRQSQRRSRHRRVRTEGKESSSASRSRSASQERSLDEAMPTEGEKDH
ELRGNHGAKEPTIQEERAQDLRRTNSLMVSRGSGLAGGLDEADTPLVLPHPELEVGKHVV
LTEQEPEGSSEQALLGNVQLDMGRVISQSEPDLSCITANTDKATTESTSVTVAIPDVDPL
VDSTVVHISNKTDGEASPLKEAEIREDEEEVEKKKQKKEKRETGKAMVPHSSMFIFSTTN
PIRRACHYIVNLRYFEMCILLVIAASSIALAAEDPVLTNSERNKVLRYFDYVFTGVFTFE
MVIKMIDQGLILQDGSYFRDLWNILDFVVVVGALVAFALANALGTNKGRDIKTIKSLRVL
RVLRPLKTIKRLPKLKAVFDCVVTSLKNVFNILIVYKLFMFIFAVIAVQLFKGKFFYCTD
SSKDTEKECIGNYVDHEKNKMEVKGREWKRHEFHYDNIIWALLTLFTVSTGEGWPQVLQH
SVDVTEEDRGPSRSNRMEMSIFYVVYFVVFPFFFVNIFVALIIITFQEQGDKMMEECSLE
KNERACIDFAISAKPLTRYMPQNRHTFQYRVWHFVVSPSFEYTIMAMIALNTVVLMMKYY
SAPCTYELALKYLNIAFTMVFSLECVLKVIAFGFLNYFRDTWNIFDFITVIGSITEIILT
DSKLVNTSGFNMSFLKLFRAARLIKLLRQGYTIRILLWTFVQSFKALPYVCLLIAMLFFI
YAIIGMQVFGNIKLDEESHINRHNNFRSFFGSLMLLFRSATGEAWQEIMLSCLGEKGCEP
DTTAPSGQNENERCGTDLAYVYFVSFIFFCSFLMLNLFVAVIMDNFEYLTRDSSILGPHH
LDEFVRVWAEYDRAACGRIHYTEMYEMLTLMSPPLGLGKRCPSKVAYKRLVLMNMPVAED
MTVHFTSTLMALIRTALDIKIAKGGADRQQLDSELQKETLAIWPHLSQKMLDLLVPMPKA
SDLTVGKIYAAMMIMDYYKQSKVKKQRQQLEEQKNAPMFQRMEPSSLPQEIIANAKALPY
LQQDPVSGLSGRSGYPSMSPLSPQDIFQLACMDPADDGQFQERQSLEPEVSELKSVQPSN
HGIYLPSDTQEHAGSGRASSMPRLTVDPQVVTDPSSMRRSFSTIRDKRSNSSWLEEFSME
RSSENTYKSRRRSYHSSLRLSAHRLNSDSGHKSDTHRSGGRERGRSKERKHLLSPDVSRC
NSEERGTQADWESPERRQSRSPSEGRSQTPNRQGTGSLSESSIPSVSDTSTPRRSRRQLP
PVPPKPRPLLSYSSLIRHAGSISPPADGSEEGSPLTSQALESNNACLTESSNSPHPQQSQ
HASPQRYISEPYLALHEDSHASDCGEEETLTFEAAVATSLGRSNTIGSAPPLRHSWQMPN
GHYRRRRRGGPGPGMMCGAVNNLLSDTEEDDKC
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Calcium channel alpha-1 subunit (TC 1.A.1.11) family, CACNA1E subfamily
Subcellular location
Membrane
Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells. They are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1E gives rise to R-type calcium currents. R-type calcium channels belong to the 'high-voltage activated' (HVA) group and are blocked by nickel. They are however insensitive to dihydropyridines (DHP). Calcium channels containing alpha-1E subunit could be involved in the modulation of firing patterns of neurons which is important for information processing.
TTD ID
T73977
Uniprot ID
Q15878
DrugMap ID
TTYRP0M
Ensemble ID
ENST00000367570.6
HGNC ID
HGNC:1392
ChEMBL ID
CHEMBL1687682

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
ABC1 SNV: p.V1408G .
CASKI SNV: p.G1866S .
CCK81 SNV: p.A487T .
CCSW1 SNV: p.P197H .
COLO792 SNV: p.E1743K; p.P1968S .
CORL23 SNV: p.N1151K .
DU145 SNV: p.A298T; p.T1004N; p.C1281Y; p.L1840V; p.P2161H; p.R2284Q .
G361 SNV: p.S1054F .
G415 SNV: p.P89S .
HCT15 SNV: p.R417K; p.E1386D; p.K1859E .
HEC1 SNV: p.V210A .
KASUMI2 SNV: p.R1258Q .
KMCH1 SNV: p.A1531T .
KP4 SNV: p.A978S .
KURAMOCHI SNV: p.T1815K .
LS123 SNV: p.A1993V .
LS513 SNV: p.M791I .
MCC13 SNV: p.D862N
Substitution: p.P119T		 .
MEWO SNV: p.E945K .
MFE296 Deletion: p.S855PfsTer52 .
MFE319 SNV: p.E1023K .
NALM6 SNV: p.R2059W; p.S2189R .
NCIH1299 SNV: p.P1936T .
NCIH1793 SNV: p.I1294V; p.G1994V .
NCIH1944 SNV: p.W160Ter; p.C1055Y .
NCIH2286 Deletion: p.D1635TfsTer19
SNV: p.E970Ter		 .
NUGC3 Deletion: p.D1431IfsTer3 .
PC9 SNV: p.F1426L .
PF382 SNV: p.R533H .
RL952 SNV: p.F148L .
SNGM SNV: p.R1143Q; p.K1323N .
SW403 SNV: p.P2095H .
TE4 SNV: p.P267T .
TGBC1TKB SNV: p.L1310F .
TOV21G SNV: p.P1141Q .

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
CY-1
 Probe Info  		E1636(0.00); E1637(0.00)  LDD0246  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Calcium Phosphate Small molecular drug DB11348
Calcium Phosphate Dihydrate Small molecular drug DB14481
Enflurane Small molecular drug DB00228
Ergocalciferol Small molecular drug DB00153
Lamotrigine Small molecular drug DB00555
Nicardipine Small molecular drug DB00622
Spironolactone Small molecular drug DB00421
Topiramate Small molecular drug DB00273
Verapamil Small molecular drug DB00661
Bioallethrin . DB13746
Butamben . DB11148
Calcium Citrate . DB11093
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cpu-228 Small molecular drug D09YTH
Efonidipine . DB09235
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Th-9229 . D0QQ7N

References

1 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.