Target Information

Target General Infomation
Target ID
T79694
Former ID
TTDR00048
Target Name
Voltage-dependent T-type calcium channel alpha-1I subunit
Gene Name
Cacna1i
Synonyms
Alpha1I; CaVT.3; Voltage-gated calcium channel alpha subunit Cav3.3; Cacna1i
Target Type
Discontinued
Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and 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. Isoform alpha-1I gives rise to T-type calcium currents. T-type calcium channels belong to the "low-voltage activated (LVA)" group and are strongly blocked by nickel and mibefradil. A particularity of this type of channels is an opening at quite negative potentials, and a voltage-dependent inactivation. T-type channels servepacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firingpatterns of neurons which is important for information processing as well as in cell growth processes. Gates in voltage ranges similar to, but higher than alpha 1G or alpha 1H.
BioChemical Class
Calcium channel
Target Validation
T79694
UniProt ID
Q9Z0Y8
Sequence
MADSNLPPSSAAAPAPEPGITEQPGPRSPPPSPPGLEEPLEGTNPDVPHPDLAPVAFFCL
RQTTSPRNWCIKMVCNPWFECVSMLVILLNCVTLGMYQPCDDMECLSDRCKILQVFDDFI
FIFFAMEMVLKMVALGIFGKKCYLGDTWNRLDFFIVMAGMVEYSLDLQNINLSAIRTVRV
LRPLKAINRVPSMRILVNLLLDTLPMLGNVLLLCFFVFFIFGIIGVQLWAGLLRNRCFLE
ENFTIQGDVALPPYYQPEEDDEMPFICSLTGDNGIMGCHEIPPLKEQGRECCLSKDDVYD
FGAGRQDLNASGLCVNWNRYYNVCRTGNANPHKGAINFDNIGYAWIVIFQVITLEGWVEI
MYYVMDAHSFYNFIYFILLIIVGSFFMINLCLVVIATQFSETKQREHRLMLEQRQRYLSS
STVASYAEPGDCYEEIFQYVCHILRKAKRRALGLYQALQNRRQAMGPGTPAPAKPGPHAK
EPSHCKLCPRHSPLDPTPHTLVQPISAILASDPSSCPHCQHEAGRRPSGLGSTDSGQEGS
GSGGSAEAEANGDGPQSSEDGVSSDLGKEEEQEDGAARLCGDVWRETREKLRGIVDSKYF
NRGIMMAILVNTVSMGIEHHEQPEELTNILEICNVVFTSMFALEMILKLAAFGLFDYLRN
PYNIFDSIIVIISIWEIVGQADGGLSVLRTFRLLRVLKLVRFMPALRRQLVVLMKTMDNV
ATFCMLLMLFIFIFSILGMHIFGCKFSLRTDTGDTVPDRKNFDSLLWAIVTVFQILTQED
WNVVLYNGMASTTPWASLYFVALMTFGNYVLFNLLVAILVEGFQAEGDANRSYSDEDQSS
SNLEEFDKLPEGLDNSRDLKLCPIPMTPNGHLDPSLPLGAHLGPAGTMGTAPRLSLQPDP
VLVALDSRKSSVMSLGRMSYDQRSLSSSRSSYYGPWGRSGTWASRRSSWNSLKHKPPSAE
HESLLSGEGGGSCVRACEGAREEAPTRTAPLHAPHAHHAHHGPHLAHRHRHHRRTLSLDT
RDSVDLGELVPVVGAHSRAAWRGAGQAPGHEDCNGRMPNIAKDVFTKMDDCRDRGEDEEE
IDYTLCFRVRKMIDVYKPDWCEVREDWSVYLFSPENKFRILCQTIIAHKLFDYVVLAFIF
LNCITIALERPQIEAGSTERIFLTVSNYIFTAIFVGEMTLKVVSLGLYFGEQAYLRSSWN
VLDGFLVFVSIIDIVVSVASAGGAKILGVLRVLRLLRTLRPLRVISRAPGLKLVVETLIS
SLKPIGNIVLICCAFFIIFGILGVQLFKGKFYHCLGVDTRNITNRSDCVAANYRWVHHKY
NFDNLGQALMSLFVLASKDGWVNIMYNGLDAVAVDQQPVTNHNPWMLLYFISFLLIVSFF
VLNMFVGVVVENFHKCRQHQEAEEARRREEKRLRRLEKKRRKAQRLPYYATYCPTRLLIH
SMCTSHYLDIFITFIICLNVVTMSLEHYNQPTSLETALKYCNYMFTTVFVLEAVLKLVAF
GLRRFFKDRWNQLDLAIVLLSVMGITLEEIEINAALPINPTIIRIMRVLRIARVLKLLKM
ATGMRALLDTVVQALPQVGNLGLLFMLLFFIYAALGVELFGKLVCNDENPCEGMSRHATF
ENFGMAFLTLFQVSTGDNWNGIMKDTLRDCTHDERSCLSSLQFVSPLYFVSFVLTAQFVL
INVVVAVLMKHLDDSNKEAQEDAEMDAEIELEMAHGLGPCPGPCPGPCPCPWPLAPVLAR
GCPLVLLGATGARIGRGRCWRRHRESPVPSTRYSPAQETLWLDSVSLIIKDSLEGELTII
DNLSGSVFHHYASPDGCGKCHHDKQEVQLAETEAFSLNSDRSSSILLGDDLSLEDPTACP
PGRKDSKGELDPPEPMRVGDLGECFFPLSSTAVSPDPENFLCEMEEIPFNPVQSWLKHDS
SQAPPSPFSPDGSSPLLQMPAEFFHPAVSASQKGPEKGTGTGTLPKIALQGSWASLRSPS
VNCTLLRQATGSDTSLDASPSSSAGSLQTTLEDSLTLSDSPRRALGPPVQVPGPRASLSP
ATRRRLSLRGRGLFSLRGLRAHQRSHSSGGSTSPGCTHHDSMDPSDEEGRGGAGGGGAGS
EHSETLSSLSLTSLFCLPPTLPPPGLTPARKFNSTSSLAAGPGRPGSTVSARGLVRSPSW
AADRSKDPPGQAQLVSGLGSSAPGPQPPPGESTDAASKRKR
Drugs and Mode of Action
Drug(s) U-92032 Drug Info Terminated Discovery agent [545700]
Inhibitor U-92032 Drug Info [525864]
Pathways
KEGG Pathway MAPK signaling pathway
Calcium signaling pathway
Circadian entrainment
References
Ref 545700Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004258)
Ref 525864J Med Chem. 2000 Sep 7;43(18):3372-6.Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity.

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