Details of the Target
General Information of Target
| Target ID | LDTP05649 | |||||
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| Target Name | Calcium-activated potassium channel subunit alpha-1 (KCNMA1) | |||||
| Gene Name | KCNMA1 | |||||
| Gene ID | 3778 | |||||
| Synonyms |
KCNMA; SLO; Calcium-activated potassium channel subunit alpha-1; BK channel; BKCA alpha; Calcium-activated potassium channel, subfamily M subunit alpha-1; K(VCA)alpha; KCa1.1; Maxi K channel; MaxiK; Slo-alpha; Slo1; Slowpoke homolog; Slo homolog; hSlo
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| 3D Structure | ||||||
| Sequence |
MANGGGGGGGSSGGGGGGGGSSLRMSSNIHANHLSLDASSSSSSSSSSSSSSSSSSSSSS
VHEPKMDALIIPVTMEVPCDSRGQRMWWAFLASSMVTFFGGLFIILLWRTLKYLWTVCCH CGGKTKEAQKINNGSSQADGTLKPVDEKEEAVAAEVGWMTSVKDWAGVMISAQTLTGRVL VVLVFALSIGALVIYFIDSSNPIESCQNFYKDFTLQIDMAFNVFFLLYFGLRFIAANDKL WFWLEVNSVVDFFTVPPVFVSVYLNRSWLGLRFLRALRLIQFSEILQFLNILKTSNSIKL VNLLSIFISTWLTAAGFIHLVENSGDPWENFQNNQALTYWECVYLLMVTMSTVGYGDVYA KTTLGRLFMVFFILGGLAMFASYVPEIIELIGNRKKYGGSYSAVSGRKHIVVCGHITLES VSNFLKDFLHKDRDDVNVEIVFLHNISPNLELEALFKRHFTQVEFYQGSVLNPHDLARVK IESADACLILANKYCADPDAEDASNIMRVISIKNYHPKIRIITQMLQYHNKAHLLNIPSW NWKEGDDAICLAELKLGFIAQSCLAQGLSTMLANLFSMRSFIKIEEDTWQKYYLEGVSNE MYTEYLSSAFVGLSFPTVCELCFVKLKLLMIAIEYKSANRESRILINPGNHLKIQEGTLG FFIASDAKEVKRAFFYCKACHDDITDPKRIKKCGCKRPKMSIYKRMRRACCFDCGRSERD CSCMSGRVRGNVDTLERAFPLSSVSVNDCSTSFRAFEDEQPSTLSPKKKQRNGGMRNSPN TSPKLMRHDPLLIPGNDQIDNMDSNVKKYDSTGMFHWCAPKEIEKVILTRSEAAMTVLSG HVVVCIFGDVSSALIGLRNLVMPLRASNFHYHELKHIVFVGSIEYLKREWETLHNFPKVS ILPGTPLSRADLRAVNINLCDMCVILSANQNNIDDTSLQDKECILASLNIKSMQFDDSIG VLQANSQGFTPPGMDRSSPDNSPVHGMLRQPSITTGVNIPIITELVNDTNVQFLDQDDDD DPDTELYLTQPFACGTAFAVSVLDSLMSATYFNDNILTLIRTLVTGGATPELEALIAEEN ALRGGYSTPQTLANRDRCRVAQLALLDGPFADLGDGGCYGDLFCKALKTYNMLCFGIYRL RDAHLSTPSQCTKRYVITNPPYEFELVPTDLIFCLMQFDHNAGQSRASLSHSSHSSQSSS KKSSSVHSIPSTANRQNRPKSRESRDKQKYVQEERL |
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| Target Type |
Clinical trial
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| Target Bioclass |
Transporter and channel
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| Family |
Potassium channel family, Calcium-activated (TC 1.A.1.3) subfamily, KCa1.1/KCNMA1 sub-subfamily
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| Subcellular location |
Cell membrane
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| Function |
Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key role in controlling excitability in a number of systems, such as regulation of the contraction of smooth muscle, the tuning of hair cells in the cochlea, regulation of transmitter release, and innate immunity. In smooth muscles, its activation by high level of Ca(2+), caused by ryanodine receptors in the sarcoplasmic reticulum, regulates the membrane potential. In cochlea cells, its number and kinetic properties partly determine the characteristic frequency of each hair cell and thereby helps to establish a tonotopic map. Kinetics of KCNMA1 channels are determined by alternative splicing, phosphorylation status and its combination with modulating beta subunits. Highly sensitive to both iberiotoxin (IbTx) and charybdotoxin (CTX).
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Target Site Mutations in Different Cell Lines
| Cell line | Mutation details | Probe for labeling this protein in this cell | |||
|---|---|---|---|---|---|
| A498 | SNV: p.T1147N | DBIA Probe Info | |||
| AGS | SNV: p.L390F | . | |||
| AN3CA | SNV: p.L277P | . | |||
| CCK81 | Insertion: p.Y676LfsTer7 | . | |||
| DU145 | SNV: p.T658I | DBIA Probe Info | |||
| HCC15 | SNV: p.Q1016K | . | |||
| HCT116 | Deletion: p.Y676TfsTer15 | . | |||
| HEC1 | SNV: p.N1010D | . | |||
| HT115 | SNV: p.S958N | . | |||
| IPC298 | SNV: p.V861M | . | |||
| JHH7 | SNV: p.D733N | . | |||
| MCC13 | SNV: p.E889K | DBIA Probe Info | |||
| MEWO | SNV: p.E822K | . | |||
| MOLT4 | Deletion: p.Y676TfsTer15 | . | |||
| NALM6 | SNV: p.V117M | . | |||
| NCIH1793 | SNV: p.I633M | DBIA Probe Info | |||
| RKO | Deletion: p.K692NfsTer15 | . | |||
| TE4 | SNV: p.D547H | . | |||
| WM793 | SNV: p.F317L | . | |||
Probe(s) Labeling This Target
ABPP Probe
| Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
|---|---|---|---|---|---|
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DBIA Probe Info |
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C947(3.21) | LDD3337 | [1] | |
Competitor(s) Related to This Target