Details of the Target

General Information of Target

Target ID LDTP07460
Target Name Volume-regulated anion channel subunit LRRC8E (LRRC8E)
Gene Name LRRC8E
Gene ID 80131
Synonyms
Volume-regulated anion channel subunit LRRC8E; Leucine-rich repeat-containing protein 8E
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MIPVAEFKQFTEQQPAFKVLKPWWDVLAEYLTVAMLMIGVFGCTLQVTQDKIICLPNHEL
QENLSEAPCQQLLPRGIPEQIGALQEVKGLKNNLDLQQYSFINQLCYETALHWYAKYFPY
LVVIHTLIFMVCTSFWFKFPGTSSKIEHFISILGKCFDSPWTTRALSEVSGENQKGPAAT
ERAAATIVAMAGTGPGKAGEGEKEKVLAEPEKVVTEPPVVTLLDKKEGEQAKALFEKVKK
FRMHVEEGDILYTMYIRQTVLKVCKFLAILVYNLVYVEKISFLVACRVETSEVTGYASFC
CNHTKAHLFSKLAFCYISFVCIYGLTCIYTLYWLFHRPLKEYSFRSVREETGMGDIPDVK
NDFAFMLHLIDQYDSLYSKRFAVFLSEVSESRLKQLNLNHEWTPEKLRQKLQRNAAGRLE
LALCMLPGLPDTVFELSEVESLRLEAICDITFPPGLSQLVHLQELSLLHSPARLPFSLQV
FLRDHLKVMRVKCEELREVPLWVFGLRGLEELHLEGLFPQELARAATLESLRELKQLKVL
SLRSNAGKVPASVTDVAGHLQRLSLHNDGARLVALNSLKKLAALRELELVACGLERIPHA
VFSLGALQELDLKDNHLRSIEEILSFQHCRKLVTLRLWHNQIAYVPEHVRKLRSLEQLYL
SYNKLETLPSQLGLCSGLRLLDVSHNGLHSLPPEVGLLQNLQHLALSYNALEALPEELFF
CRKLRTLLLGDNQLSQLSPHVGALRALSRLELKGNRLEALPEELGNCGGLKKAGLLVEDT
LYQGLPAEVRDKMEEE
Target Bioclass
Transporter and channel
Family
LRRC8 family
Subcellular location
Cell membrane
Function
Non-essential component of the volume-regulated anion channel (VRAC, also named VSOAC channel), an anion channel required to maintain a constant cell volume in response to extracellular or intracellular osmotic changes. The VRAC channel conducts iodide better than chloride and can also conduct organic osmolytes like taurine. Mediates efflux of amino acids, such as aspartate, in response to osmotic stress. The VRAC channel also mediates transport of immunoreactive cyclic dinucleotide GMP-AMP (2'-3'-cGAMP), an immune messenger produced in response to DNA virus in the cytosol. Channel activity requires LRRC8A plus at least one other family member (LRRC8B, LRRC8C, LRRC8D or LRRC8E); channel characteristics depend on the precise subunit composition. Also plays a role in lysosome homeostasis by forming functional lysosomal VRAC channels in response to low cytoplasmic ionic strength condition: lysosomal VRAC channels are necessary for the formation of large lysosome-derived vacuoles, which store and then expel excess water to maintain cytosolic water homeostasis.
Uniprot ID
Q6NSJ5
Ensemble ID
ENST00000306708.11
HGNC ID
HGNC:26272

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K237(1.79)  LDD0277  [1]
DBIA
 Probe Info  		C675(2.23)  LDD3346  [2]
BTD
 Probe Info  		C493(2.15)  LDD1700  [3]
NAIA_5
 Probe Info  		N.A.  LDD2223  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C493(0.94)  LDD2117  [3]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C493(1.19)  LDD2152  [3]
 LDCM0214  AC1 HEK-293T C448(1.05)  LDD1507  [5]
 LDCM0215  AC10 HEK-293T C448(1.08)  LDD1508  [5]
 LDCM0226  AC11 HEK-293T C448(0.90); C629(1.05)  LDD1509  [5]
 LDCM0237  AC12 HEK-293T C448(1.09)  LDD1510  [5]
 LDCM0259  AC14 HEK-293T C448(0.91)  LDD1512  [5]
 LDCM0270  AC15 HEK-293T C448(1.29)  LDD1513  [5]
 LDCM0276  AC17 HEK-293T C448(1.43)  LDD1515  [5]
 LDCM0277  AC18 HEK-293T C448(0.80)  LDD1516  [5]
 LDCM0278  AC19 HEK-293T C448(0.93); C629(1.03)  LDD1517  [5]
 LDCM0279  AC2 HEK-293T C448(1.01)  LDD1518  [5]
 LDCM0280  AC20 HEK-293T C448(1.07)  LDD1519  [5]
 LDCM0281  AC21 HEK-293T C448(1.20)  LDD1520  [5]
 LDCM0282  AC22 HEK-293T C448(1.13)  LDD1521  [5]
 LDCM0283  AC23 HEK-293T C448(1.09)  LDD1522  [5]
 LDCM0285  AC25 HEK-293T C448(1.09)  LDD1524  [5]
 LDCM0286  AC26 HEK-293T C448(1.05)  LDD1525  [5]
 LDCM0287  AC27 HEK-293T C448(0.89); C629(1.22)  LDD1526  [5]
 LDCM0288  AC28 HEK-293T C448(0.99)  LDD1527  [5]
 LDCM0289  AC29 HEK-293T C448(1.25)  LDD1528  [5]
 LDCM0290  AC3 HEK-293T C448(1.05); C629(1.11)  LDD1529  [5]
 LDCM0291  AC30 HEK-293T C448(1.14)  LDD1530  [5]
 LDCM0292  AC31 HEK-293T C448(1.02)  LDD1531  [5]
 LDCM0294  AC33 HEK-293T C448(1.20)  LDD1533  [5]
 LDCM0295  AC34 HEK-293T C448(0.90)  LDD1534  [5]
 LDCM0296  AC35 HEK-293T C448(1.26); C629(1.16)  LDD1535  [5]
 LDCM0297  AC36 HEK-293T C448(0.94)  LDD1536  [5]
 LDCM0298  AC37 HEK-293T C448(1.11)  LDD1537  [5]
 LDCM0299  AC38 HEK-293T C448(0.77)  LDD1538  [5]
 LDCM0300  AC39 HEK-293T C448(1.09)  LDD1539  [5]
 LDCM0301  AC4 HEK-293T C448(1.06)  LDD1540  [5]
 LDCM0303  AC41 HEK-293T C448(1.18)  LDD1542  [5]
 LDCM0304  AC42 HEK-293T C448(1.09)  LDD1543  [5]
 LDCM0305  AC43 HEK-293T C448(1.14); C629(1.00)  LDD1544  [5]
 LDCM0306  AC44 HEK-293T C448(1.07)  LDD1545  [5]
 LDCM0307  AC45 HEK-293T C448(1.68)  LDD1546  [5]
 LDCM0308  AC46 HEK-293T C448(1.09)  LDD1547  [5]
 LDCM0309  AC47 HEK-293T C448(0.92)  LDD1548  [5]
 LDCM0311  AC49 HEK-293T C448(1.21)  LDD1550  [5]
 LDCM0312  AC5 HEK-293T C448(0.95)  LDD1551  [5]
 LDCM0313  AC50 HEK-293T C448(0.98)  LDD1552  [5]
 LDCM0314  AC51 HEK-293T C448(1.28); C629(0.85)  LDD1553  [5]
 LDCM0315  AC52 HEK-293T C448(1.17)  LDD1554  [5]
 LDCM0316  AC53 HEK-293T C448(1.33)  LDD1555  [5]
 LDCM0317  AC54 HEK-293T C448(1.05)  LDD1556  [5]
 LDCM0318  AC55 HEK-293T C448(0.93)  LDD1557  [5]
 LDCM0320  AC57 HEK-293T C448(1.97)  LDD1559  [5]
 LDCM0321  AC58 HEK-293T C448(0.95)  LDD1560  [5]
 LDCM0322  AC59 HEK-293T C448(0.89); C629(1.13)  LDD1561  [5]
 LDCM0323  AC6 HEK-293T C448(0.77)  LDD1562  [5]
 LDCM0324  AC60 HEK-293T C448(1.23)  LDD1563  [5]
 LDCM0325  AC61 HEK-293T C448(1.19)  LDD1564  [5]
 LDCM0326  AC62 HEK-293T C448(1.01)  LDD1565  [5]
 LDCM0327  AC63 HEK-293T C448(1.00)  LDD1566  [5]
 LDCM0334  AC7 HEK-293T C448(0.93)  LDD1568  [5]
 LDCM0248  AKOS034007472 HEK-293T C448(1.21)  LDD1511  [5]
 LDCM0356  AKOS034007680 HEK-293T C448(1.41)  LDD1570  [5]
 LDCM0368  CL10 HEK-293T C448(1.18)  LDD1572  [5]
 LDCM0371  CL102 HEK-293T C448(1.08)  LDD1575  [5]
 LDCM0372  CL103 HEK-293T C448(0.92)  LDD1576  [5]
 LDCM0375  CL106 HEK-293T C448(1.21)  LDD1579  [5]
 LDCM0376  CL107 HEK-293T C448(0.80)  LDD1580  [5]
 LDCM0379  CL11 HEK-293T C448(2.21)  LDD1583  [5]
 LDCM0380  CL110 HEK-293T C448(0.90)  LDD1584  [5]
 LDCM0381  CL111 HEK-293T C448(1.07)  LDD1585  [5]
 LDCM0384  CL114 HEK-293T C448(1.16)  LDD1588  [5]
 LDCM0385  CL115 HEK-293T C448(1.04)  LDD1589  [5]
 LDCM0388  CL118 HEK-293T C448(0.90)  LDD1592  [5]
 LDCM0389  CL119 HEK-293T C448(1.03)  LDD1593  [5]
 LDCM0393  CL122 HEK-293T C448(0.96)  LDD1597  [5]
 LDCM0394  CL123 HEK-293T C448(0.99)  LDD1598  [5]
 LDCM0397  CL126 HEK-293T C448(0.75)  LDD1601  [5]
 LDCM0398  CL127 HEK-293T C448(0.88)  LDD1602  [5]
 LDCM0401  CL14 HEK-293T C448(0.90)  LDD1605  [5]
 LDCM0402  CL15 HEK-293T C448(0.94)  LDD1606  [5]
 LDCM0404  CL17 HEK-293T C448(1.36)  LDD1608  [5]
 LDCM0405  CL18 HEK-293T C448(1.20)  LDD1609  [5]
 LDCM0406  CL19 HEK-293T C448(1.33); C629(1.12)  LDD1610  [5]
 LDCM0407  CL2 HEK-293T C448(1.17)  LDD1611  [5]
 LDCM0408  CL20 HEK-293T C448(1.58)  LDD1612  [5]
 LDCM0409  CL21 HEK-293T C448(1.51)  LDD1613  [5]
 LDCM0410  CL22 HEK-293T C448(1.23)  LDD1614  [5]
 LDCM0411  CL23 HEK-293T C448(1.99)  LDD1615  [5]
 LDCM0414  CL26 HEK-293T C448(0.96)  LDD1618  [5]
 LDCM0415  CL27 HEK-293T C448(1.03)  LDD1619  [5]
 LDCM0417  CL29 HEK-293T C448(1.35)  LDD1621  [5]
 LDCM0418  CL3 HEK-293T C448(1.49)  LDD1622  [5]
 LDCM0419  CL30 HEK-293T C448(1.03)  LDD1623  [5]
 LDCM0420  CL31 HEK-293T C448(0.97); C629(0.86)  LDD1624  [5]
 LDCM0421  CL32 HEK-293T C448(1.31)  LDD1625  [5]
 LDCM0422  CL33 HEK-293T C448(1.44)  LDD1626  [5]
 LDCM0423  CL34 HEK-293T C448(1.33)  LDD1627  [5]
 LDCM0424  CL35 HEK-293T C448(1.96)  LDD1628  [5]
 LDCM0428  CL39 HEK-293T C448(0.95)  LDD1632  [5]
 LDCM0431  CL41 HEK-293T C448(1.39)  LDD1635  [5]
 LDCM0432  CL42 HEK-293T C448(0.93)  LDD1636  [5]
 LDCM0433  CL43 HEK-293T C448(1.09); C629(1.01)  LDD1637  [5]
 LDCM0434  CL44 HEK-293T C448(1.28)  LDD1638  [5]
 LDCM0435  CL45 HEK-293T C448(1.62)  LDD1639  [5]
 LDCM0436  CL46 HEK-293T C448(1.16)  LDD1640  [5]
 LDCM0437  CL47 HEK-293T C448(1.48)  LDD1641  [5]
 LDCM0440  CL5 HEK-293T C448(1.18)  LDD1644  [5]
 LDCM0441  CL50 HEK-293T C448(1.06)  LDD1645  [5]
 LDCM0444  CL53 HEK-293T C448(1.44)  LDD1647  [5]
 LDCM0445  CL54 HEK-293T C448(1.20)  LDD1648  [5]
 LDCM0446  CL55 HEK-293T C448(1.17); C629(1.05)  LDD1649  [5]
 LDCM0447  CL56 HEK-293T C448(1.36)  LDD1650  [5]
 LDCM0448  CL57 HEK-293T C448(1.22)  LDD1651  [5]
 LDCM0449  CL58 HEK-293T C448(1.41)  LDD1652  [5]
 LDCM0450  CL59 HEK-293T C448(1.75)  LDD1653  [5]
 LDCM0451  CL6 HEK-293T C448(1.15)  LDD1654  [5]
 LDCM0454  CL62 HEK-293T C448(0.92)  LDD1657  [5]
 LDCM0455  CL63 HEK-293T C448(1.08)  LDD1658  [5]
 LDCM0457  CL65 HEK-293T C448(1.12)  LDD1660  [5]
 LDCM0458  CL66 HEK-293T C448(0.96)  LDD1661  [5]
 LDCM0459  CL67 HEK-293T C448(1.16); C629(0.96)  LDD1662  [5]
 LDCM0460  CL68 HEK-293T C448(1.38)  LDD1663  [5]
 LDCM0461  CL69 HEK-293T C448(1.93)  LDD1664  [5]
 LDCM0462  CL7 HEK-293T C448(1.41); C629(1.14)  LDD1665  [5]
 LDCM0463  CL70 HEK-293T C448(1.10)  LDD1666  [5]
 LDCM0464  CL71 HEK-293T C448(1.47)  LDD1667  [5]
 LDCM0467  CL74 HEK-293T C448(0.82)  LDD1670  [5]
 LDCM0470  CL77 HEK-293T C448(1.78)  LDD1673  [5]
 LDCM0471  CL78 HEK-293T C448(1.05)  LDD1674  [5]
 LDCM0472  CL79 HEK-293T C448(1.03); C629(1.03)  LDD1675  [5]
 LDCM0473  CL8 HEK-293T C448(1.28)  LDD1676  [5]
 LDCM0474  CL80 HEK-293T C448(1.17)  LDD1677  [5]
 LDCM0475  CL81 HEK-293T C448(1.69)  LDD1678  [5]
 LDCM0476  CL82 HEK-293T C448(1.29)  LDD1679  [5]
 LDCM0477  CL83 HEK-293T C448(1.12)  LDD1680  [5]
 LDCM0480  CL86 HEK-293T C448(0.83)  LDD1683  [5]
 LDCM0481  CL87 HEK-293T C448(0.90)  LDD1684  [5]
 LDCM0483  CL89 HEK-293T C448(1.16)  LDD1686  [5]
 LDCM0484  CL9 HEK-293T C448(1.84)  LDD1687  [5]
 LDCM0485  CL90 HEK-293T C448(0.95)  LDD1688  [5]
 LDCM0486  CL91 HEK-293T C448(0.83); C629(1.17)  LDD1689  [5]
 LDCM0487  CL92 HEK-293T C448(1.05)  LDD1690  [5]
 LDCM0488  CL93 HEK-293T C448(1.19)  LDD1691  [5]
 LDCM0489  CL94 HEK-293T C448(1.33)  LDD1692  [5]
 LDCM0490  CL95 HEK-293T C448(1.29)  LDD1693  [5]
 LDCM0493  CL98 HEK-293T C448(0.77)  LDD1696  [5]
 LDCM0494  CL99 HEK-293T C448(1.19)  LDD1697  [5]
 LDCM0495  E2913 HEK-293T C448(1.04)  LDD1698  [5]
 LDCM0468  Fragment33 HEK-293T C448(0.95)  LDD1671  [5]
 LDCM0427  Fragment51 HEK-293T C448(0.88)  LDD1631  [5]
 LDCM0022  KB02 769-P C675(1.83)  LDD2246  [2]
 LDCM0023  KB03 769-P C675(2.46)  LDD2663  [2]
 LDCM0024  KB05 NCI-H1666 C675(2.23)  LDD3346  [2]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C493(0.92)  LDD2093  [3]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C493(1.04)  LDD2099  [3]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C493(0.82)  LDD2107  [3]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C493(0.63)  LDD2109  [3]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C493(1.04)  LDD2111  [3]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C493(1.86)  LDD2119  [3]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C493(1.07)  LDD2123  [3]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C493(1.08)  LDD2127  [3]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C493(1.00)  LDD2129  [3]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C493(1.23)  LDD2135  [3]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C493(0.95)  LDD2137  [3]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C493(2.15)  LDD1700  [3]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C493(0.88)  LDD2140  [3]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C493(2.40)  LDD2144  [3]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C493(0.80)  LDD2146  [3]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C493(0.49)  LDD2150  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tripartite motif-containing protein 2 (TRIM2) TRIM/RBCC family Q9C040
Tripartite motif-containing protein 3 (TRIM3) TRIM/RBCC family O75382
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Volume-regulated anion channel subunit LRRC8A (LRRC8A) LRRC8 family Q8IWT6
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
G-protein-signaling modulator 2 (GPSM2) GPSM family P81274
Protein Smaug homolog 2 (SAMD4B) SMAUG family Q5PRF9

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 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
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
5 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402