Details of the Target

General Information of Target

Target ID LDTP05594
Target Name ATP-binding cassette sub-family C member 8 (ABCC8)
Gene Name ABCC8
Gene ID 6833
Synonyms
HRINS; SUR; SUR1; ATP-binding cassette sub-family C member 8; Sulfonylurea receptor 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPLAFCGSENHSAAYRVDQGVLNNGCFVDALNVVPHVFLLFITFPILFIGWGSQSSKVHI
HHSTWLHFPGHNLRWILTFMLLFVLVCEIAEGILSDGVTESHHLHLYMPAGMAFMAAVTS
VVYYHNIETSNFPKLLIALLVYWTLAFITKTIKFVKFLDHAIGFSQLRFCLTGLLVILYG
MLLLVEVNVIRVRRYIFFKTPREVKPPEDLQDLGVRFLQPFVNLLSKGTYWWMNAFIKTA
HKKPIDLRAIGKLPIAMRALTNYQRLCEAFDAQVRKDIQGTQGARAIWQALSHAFGRRLV
LSSTFRILADLLGFAGPLCIFGIVDHLGKENDVFQPKTQFLGVYFVSSQEFLANAYVLAV
LLFLALLLQRTFLQASYYVAIETGINLRGAIQTKIYNKIMHLSTSNLSMGEMTAGQICNL
VAIDTNQLMWFFFLCPNLWAMPVQIIVGVILLYYILGVSALIGAAVIILLAPVQYFVATK
LSQAQRSTLEYSNERLKQTNEMLRGIKLLKLYAWENIFRTRVETTRRKEMTSLRAFAIYT
SISIFMNTAIPIAAVLITFVGHVSFFKEADFSPSVAFASLSLFHILVTPLFLLSSVVRST
VKALVSVQKLSEFLSSAEIREEQCAPHEPTPQGPASKYQAVPLRVVNRKRPAREDCRGLT
GPLQSLVPSADGDADNCCVQIMGGYFTWTPDGIPTLSNITIRIPRGQLTMIVGQVGCGKS
SLLLAALGEMQKVSGAVFWSSLPDSEIGEDPSPERETATDLDIRKRGPVAYASQKPWLLN
ATVEENIIFESPFNKQRYKMVIEACSLQPDIDILPHGDQTQIGERGINLSGGQRQRISVA
RALYQHANVVFLDDPFSALDIHLSDHLMQAGILELLRDDKRTVVLVTHKLQYLPHADWII
AMKDGTIQREGTLKDFQRSECQLFEHWKTLMNRQDQELEKETVTERKATEPPQGLSRAMS
SRDGLLQDEEEEEEEAAESEEDDNLSSMLHQRAEIPWRACAKYLSSAGILLLSLLVFSQL
LKHMVLVAIDYWLAKWTDSALTLTPAARNCSLSQECTLDQTVYAMVFTVLCSLGIVLCLV
TSVTVEWTGLKVAKRLHRSLLNRIILAPMRFFETTPLGSILNRFSSDCNTIDQHIPSTLE
CLSRSTLLCVSALAVISYVTPVFLVALLPLAIVCYFIQKYFRVASRDLQQLDDTTQLPLL
SHFAETVEGLTTIRAFRYEARFQQKLLEYTDSNNIASLFLTAANRWLEVRMEYIGACVVL
IAAVTSISNSLHRELSAGLVGLGLTYALMVSNYLNWMVRNLADMELQLGAVKRIHGLLKT
EAESYEGLLAPSLIPKNWPDQGKIQIQNLSVRYDSSLKPVLKHVNALIAPGQKIGICGRT
GSGKSSFSLAFFRMVDTFEGHIIIDGIDIAKLPLHTLRSRLSIILQDPVLFSGTIRFNLD
PERKCSDSTLWEALEIAQLKLVVKALPGGLDAIITEGGENFSQGQRQLFCLARAFVRKTS
IFIMDEATASIDMATENILQKVVMTAFADRTVVTIAHRVHTILSADLVIVLKRGAILEFD
KPEKLLSRKDSVFASFVRADK
Target Type
Successful
Target Bioclass
Transporter and channel
Family
ABC transporter superfamily, ABCC family, Conjugate transporter (TC 3.A.1.208) subfamily
Subcellular location
Cell membrane
Function Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release.
TTD ID
T91480
Uniprot ID
Q09428
DrugMap ID
TTP835K
Ensemble ID
ENST00000302539.9
HGNC ID
HGNC:59
ChEMBL ID
CHEMBL2071

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
ABC1 SNV: p.S960P .
CAL78 SNV: p.Q967Ter .
COLO320 SNV: p.A725P .
COLO678 SNV: p.R486W .
COLO792 SNV: p.E203K .
HCT116 SNV: p.R388S; p.M682I .
HCT15 Deletion: p.L1052PfsTer39
SNV: p.M730V		 .
HT115 SNV: p.T820I; p.A1536V .
KYSE510 SNV: p.I148F .
MCC13 Substitution: p.G683K .
MINO SNV: p.F1239L .
NCIH146 SNV: p.P317L .
NCIH1975 SNV: p.R598L .
NCIH446 SNV: p.A161S; p.P1441A .
ONS76 SNV: p.P751H .
SKMEL5 SNV: p.E1455K .
YSCCC SNV: p.E978D .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C922(4.00)  LDD2268  [1]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 BRX211 C922(4.00)  LDD2268  [1]
 LDCM0023  KB03 BRX211 C922(4.25)  LDD2685  [1]
 LDCM0024  KB05 BRX211 C922(2.81)  LDD3102  [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
ATP-sensitive inward rectifier potassium channel 11 (KCNJ11) Inward rectifier-type potassium channel family Q14654

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
Acetohexamide Small molecular drug D07WFK
Chlorpropamide Small molecular drug DB00672
Glibenclamide Small molecular drug D05LYX
Gliclazide Small molecular drug D0M2MR
Glimepiride Small molecular drug D0B2GI
Glipizide Small molecular drug DB01067
Gliquidone Small molecular drug DB01251
Glyburide Small molecular drug DB01016
Glymidine Small molecular drug DB01382
Nateglinide Small molecular drug DB00731
Repaglinide Small molecular drug D0N5YA
Tolbutamide Small molecular drug D06OIV
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nn-414 Small molecular drug D02ZPN
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Atp Small molecular drug DB00171
Hbr-985 Small molecular drug D0U1XJ
Mitiglinide Small molecular drug DB01252
Ns-11757 Small molecular drug D0H4BF

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 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060