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Showing drug card for Zonisamide (DB00909)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:03:44
Primary Accession Number DB00909
Secondary Accession Number
  • APRD00004
Name Zonisamide
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description Zonisamide is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures. Zonisamide may be a carbonic anhydrase inhibitor although this is not one of the primary mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels leading to a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may inhibit the uptake of the inhibitory neurotransmitter GABA while enhancing the uptake of the excitatory neurotransmitter glutamate.
Synonyms
  1. Zonisamida [Spanish]
  2. Zonisamidum [Latin]
  3. zonisamide
Brand Names
  1. Exceglan
  2. Excegram
  3. Excegran
  4. Zonegran
Brand Mixtures Not Available
Chemical IUPAC Name 1,2-benzoxazol-3-ylmethanesulfonamide
Chemical Formula C8H8N2O3S
Chemical Structure Structure
CAS Registry Number 68291-97-4
InChI Identifier InChI=1/C8H8N2O3S/c9-14(11,12)5-7-6-3-1-2-4-8(6)13-10-7/h1-4H,5H2,(H2,9,11,12)/f/h9H2
InChI Key UBQNRHZMVUUOMG-JSGPKCTECW
KEGG Drug D00538 Link Image
KEGG Compound C07504 Link Image
PubChem Compound 5734 Link Image
PubChem Substance 188654 Link Image
ChEBI ID Not Available
PharmGKB ID PA451978 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available
RxList Link http://www.rxlist.com/cgi/generic3/zonisamide.htm Link Image
PDRhealth Link http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zon1564.shtml Link Image
Wikipedia Link http://en.wikipedia.org/wiki/Zonisamide Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 212.2260
Monoisotopic Molecular Weight 212.0256
State Solid
Melting Point 161-163 oC
Experimental Water Solubility 0.8 mg/mL Source: PhysProp
Predicted Water Solubility 2.09e+00 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 0.5 Source: PhysProp
Predicted LogP 0.67 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -2.01 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 10.2
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES NS(=O)(=O)CC1=NOC2=CC=CC=C12
Canonical SMILES NS(=O)(=O)CC1=NOC2=CC=CC=C12
Drug Category
  • Anticonvulsants
  • Antioxidants
ATC Codes
AHFS Codes Not Available
Indication For use as adjunctive treatment of partial seizures in adults with epilepsy.
Pharmacology Zonisamide is an antiseizure drug chemically classified as a sulfonamide and unrelated to other antiseizure agents. The precise mechanism by which zonisamide exerts its antiseizure effect is unknown, although it is believed that the drug blocks sodium channels which leads to the suppression of neuronal hypersynchronization (i.e. convulsions). Likewise zonisamide has also been found not to potentiate syanptic activity by GABA (gamma amino butyric acid).
Mechanism of Action Zonisamide binds to sodium channels, voltage sensitive calcium channels and to a lesser extent carbonic anhydrase. This blocks or suppresses neuronal depolarization and hypersynchronization.
Absorption Variable, yet relatively rapid rate of absorption with a time to peak concentration of 2.8-3.9 hours. Food has no effect on the bioavailability of zonisamide.
Toxicity Symptoms of overdose include diminished breathing, loss of consciousness, low blood pressure, and slow heartbeat.
Protein Binding 40% (at concentrations of 1.0-7.0 µg/mL)
Biotransformation Primarily hepatic through cytochrome P450 isoenzyme 3A4 (CYP3A4). Undergoes acetylation and reduction, forming N-acetyl zonisamide, and the open-ring metabolite 2–sulfamoylacetyl phenol, respectively.
Half Life 63 hours
Dosage Forms
Form Route
Capsule Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Murata M, Horiuchi E, Kanazawa I: Zonisamide has beneficial effects on Parkinson's disease patients. Neurosci Res. 2001 Dec;41(4):397-9. [PubMed Link Image]
  2. Gadde KM, Franciscy DM, Wagner HR 2nd, Krishnan KR: Zonisamide for weight loss in obese adults: a randomized controlled trial. JAMA. 2003 Apr 9;289(14):1820-5. [PubMed Link Image]
  3. Ueda Y, Doi T, Tokumaru J, Willmore LJ: Effect of zonisamide on molecular regulation of glutamate and GABA transporter proteins during epileptogenesis in rats with hippocampal seizures. Brain Res Mol Brain Res. 2003 Aug 19;116(1-2):1-6. [PubMed Link Image]
  4. Hasegawa H: Utilization of zonisamide in patients with chronic pain or epilepsy refractory to other treatments: a retrospective, open label, uncontrolled study in a VA hospital. Curr Med Res Opin. 2004 May;20(5):577-80. [PubMed Link Image]
  5. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [PubMed Link Image]
  6. Drugs.com Link Image
  7. Wikipedia Link Image
  8. RxList Link Image
  9. PDRhealth Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 3A4 (CYP3A4)
  2. Aldehyde oxidase
Targets
  1. Sodium channel protein type 1 subunit alpha
  2. Carbonic anhydrase 1
  3. Voltage-dependent T-type calcium channel subunit alpha-1G
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 1 Gene Name CYP3A4
Enzyme 1 SwissProt ID P08684 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Aldehyde oxidase
Enzyme 2 Gene Name AOX1
Enzyme 2 SwissProt ID Q06278 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|Q06278|ADO_HUMAN Aldehyde oxidase (EC 1.2.3.1) 
MDRASELLFYVNGRKVIEKNVDPETMLLPYLRKKLRLTGTPYGCGGGGCGACTVMISRYN
PITKRIRHHPANACLIPICSLYGAAVTTVEGIGSTHTRIHPVQERIAKCHGTQCGFCTPG
MVMSIYPLLRNHPEPTLDQLTDALGGNLCRCHGYRPIIDACKTFCKTSGCCQSKENGVCC
LDQGINGLPEFEEGSKTSPKLFAEEEFLPLDPTQELIFPPELMIMADKQSQRTRVFGSER
MMWFSPVTLKDLLEFKFKYPQAPVIMGNTSVGPEVKFKGVFHPGYNSPDRIEEPECCKPC
IYGLTLGAGLSLAQVKDILADVVQKLPEEKTQMYHALLKHLGTLAGSQIRNMASLGGHII
SRHPDSDLNPILAVGNCTLNLLSKEGKRQIPLNEQFLSKCPNADLKPQEILVSVNIPISR
KWEFVSAFRQAQRQENALAIVNSGMRVFFGEGDGIIRELCISYGGVGPATICAKNSCQKL
IGRHWNEQMLDIACRLILNEVSLLGSAPGGKVEFKRTLIISFLFKFYLEVSQILKKMDPV
HYPSLADKYESALEDLHSKHHCSTLKYQNIGPKQHPEDPIGHPIMHLSGVKHATGEAIYC
DDMPLVDQELFLTFVTSSRAHAKIVSIDLSEALSMPGVVDIMTAEHLSDVNSFCFFTEAE
KFLATDKVFCVGQLVCAVLADSEVQAKRAAKRVKIVYQDLEPLILTIEESIQHNSSFKPE
RKLEYGNVDEAFKVVDQILEGEIHMGGQEHFYMETQSMLVVPKGEDQEMDVYVSTQFPKY
IQDIVASTLKLPANKVMCHVRRVGGAFGGKVLKTGIIAAVTAFAANKHGRAVRCVLERGE
DMLITGGRHPYLGKYKAGFMNDGRILALDMEHYSNAGASLDESLFVIEMGLLKMDNAYKF
PNLRCRGWACRTNLPSNTAFRGFGFPQAVLITESCITEVAAKCGLSPEKVRIINMYKEID
QTPYKQEINAKNLIQCWRECMAMSSYSLRKVAVEKFNAENYWKKKGLAMVPLKFPVGLAS
RAAGQAAALVHIYLDGSVLVTHGGIEMGQGVHTKMIQVVSRELRMPMSNVHLRGTSTETV
PNANISGGSVVADLNGLAVKDACQTLLKRLEPIISKNPKGTWKDWAQTAFDESINLSAVG
YFRGYESDMNWEKGEGQPFEYFVYGAACSEVEIDCLTGDHKNIRTDIVMDVGCSINPAID
IGQIEGAFIQGMGLYTIEELNYSPQGILHTRGPDQYKIPAICDMPTELHIALLPPSQNSN
TLYSSKGLGESGVFLGCSVFFAIHDAVSAARQERGLHGPLTLNSPLTPEKIRMACEDKFT
KMIPRDEPGSYVPWNVPI
Drug Target 1 [top]
Target 1 ID 158
Target 1 Name Sodium channel protein type 1 subunit alpha
Target 1 Synonyms
  1. Sodium channel protein type I subunit alpha
  2. Sodium channel protein, brain I subunit alpha
  3. Voltage-gated sodium channel subunit alpha Nav1.1
Target 1 Gene Name SCN1A
Target 1 Protein Sequence >Sodium channel protein type 1 subunit alpha 
MEQTVLVPPGPDSFNFFTRESLAAIERRIAEEKAKNPKPDKKDDDENGPKPNSDLEAGKN
LPFIYGDIPPEMVSEPLEDLDPYYINKKTFIVLNKGKAIFRFSATSALYILTPFNPLRKI
AIKILVHSLFSMLIMCTILTNCVFMTMSNPPDWTKNVEYTFTGIYTFESLIKIIARGFCL
EDFTFLRDPWNWLDFTVITFAYVTEFVDLGNVSALRTFRVLRALKTISVIPGLKTIVGAL
IQSVKKLSDVMILTVFCLSVFALIGLQLFMGNLRNKCIQWPPTNASLEEHSIEKNITVNY
NGTLINETVFEFDWKSYIQDSRYHYFLEGFLDALLCGNSSDAGQCPEGYMCVKAGRNPNY
GYTSFDTFSWAFLSLFRLMTQDFWENLYQLTLRAAGKTYMIFFVLVIFLGSFYLINLILA
VVAMAYEEQNQATLEEAEQKEAEFQQMIEQLKKQQEAAQQAATATASEHSREPSAAGRLS
DSSSEASKLSSKSAKERRNRRKKRKQKEQSGGEEKDEDEFQKSESEDSIRRKGFRFSIEG
NRLTYEKRYSSPHQSLLSIRGSLFSPRRNSRTSLFSFRGRAKDVGSENDFADDEHSTFED
NESRRDSLFVPRRHGERRNSNLSQTSRSSRMLAVFPANGKMHSTVDCNGVVSLVGGPSVP
TSPVGQLLPEVIIDKPATDDNGTTTETEMRKRRSSSFHVSMDFLEDPSQRQRAMSIASIL
TNTVEELEESRQKCPPCWYKFSNIFLIWDCSPYWLKVKHVVNLVVMDPFVDLAITICIVL
NTLFMAMEHYPMTDHFNNVLTVGNLVFTGIFTAEMFLKIIAMDPYYYFQEGWNIFDGFIV
TLSLVELGLANVEGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAII
VFIFAVVGMQLFGKSYKDCVCKIASDCQLPRWHMNDFFHSFLIVFRVLCGEWIETMWDCM
EVAGQAMCLTVFMMVMVIGNLVVLNLFLALLLSSFSADNLAATDDDNEMNNLQIAVDRMH
KGVAYVKRKIYEFIQQSFIRKQKILDEIKPLDDLNNKKDSCMSNHTAEIGKDLDYLKDVN
GTTSGIGTGSSVEKYIIDESDYMSFINNPSLTVTVPIAVGESDFENLNTEDFSSESDLEE
SKEKLNESSSSSEGSTVDIGAPVEEQPVVEPEETLEPEACFTEGCVQRFKCCQINVEEGR
GKQWWNLRRTCFRIVEHNWFETFIVFMILLSSGALAFEDIYIDQRKTIKTMLEYADKVFT
YIFILEMLLKWVAYGYQTYFTNAWCWLDFLIVDVSLVSLTANALGYSELGAIKSLRTLRA
LRPLRALSRFEGMRVVVNALLGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYHCINTT
TGDRFDIEDVNNHTDCLKLIERNETARWKNVKVNFDNVGFGYLSLLQVATFKGWMDIMYA
AVDSRNVELQPKYEESLYMYLYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKFGGQDIFM
TEEQKKYYNAMKKLGSKKPQKPIPRPGNKFQGMVFDFVTRQVFDISIMILICLNMVTMMV
ETDDQSEYVTTILSRINLVFIVLFTGECVLKLISLRHYYFTIGWNIFDFVVVILSIVGMF
LAELIEKYFVSPTLFRVIRLARIGRILRLIKGAKGIRTLLFALMMSLPALFNIGLLLFLV
MFIYAIFGMSNFAYVKREVGIDDMFNFETFGNSMICLFQITTSAGWDGLLAPILNSKPPD
CDPNKVNPGSSVKGDCGNPSVGIFFFVSYIIISFLVVVNMYIAVILENFSVATEESAEPL
SEDDFEMFYEVWEKFDPDATQFMEFEKLSQFAAALEPPLNLPQPNKLQLIAMDLPMVSGD
RIHCLDILFAFTKRVLGESGEMDALRIQMEERFMASNPSKVSYQPITTTLKRKQEEVSAV
IIQRAYRRHLLKRTVKQASFTYNKNKIKGGANLLIKEDMIIDRINENSITEKTDLTMSTA
ACPPSYDRVTKPIVEKHEQEGKDEKAKGK
Target 1 Number of Residues 2042
Target 1 Molecular Weight 228974
Target 1 Theoretical pI 5.53
Target 1 GO Classification
Function
voltage-gated ion channel activity
voltage-gated sodium channel activity
transporter activity
ion transporter activity
ion channel activity
binding
ion binding
cation binding
calcium ion binding
Process
cation transport
monovalent inorganic cation transport
sodium ion transport
physiological process
cellular physiological process
transport
ion transport
Component
protein complex
voltage-gated sodium channel complex
cell
membrane
Target 1 General Function Involved in ion channel activity
Target 1 Specific Function Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 124-147
  • 156-175
  • 189-207
  • 214-233
  • 250-273
  • 400-425
  • 763-787
  • 799-822
  • 831-850
  • 857-876
  • 893-913
  • 967-992
  • 1214-1237
  • 1251-1276
  • 1283-1304
  • 1309-1330
  • 1350-1377
  • 1457-1483
  • 1537-1560
  • 1572-1595
  • 1602-1625
  • 1636-1657
  • 1673-1695
  • 1762-1786
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 12642270 Link Image
Target 1 UniProtKB/Swiss-Prot ID P35498 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name SCN1A_HUMAN Link Image
Target 1 PDB ID 1BYY Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >6000 bp 
ATGGAGCAAACAGTGCTTGTACCACCAGGACCTGACAGCTTCAACTTCTTCACCAGAGAA
TCTCTTGCGGCTATTGAAAGACGCATTGCAGAAGAAAAGGCAAAGAATCCCAAACCAGAC
AAAAAAGATGACGACGAAAATGGCCCAAAGCCAAATAGTGACTTGGAAGCTGGAAAGAAC
CTTCCATTTATTTATGGAGACATTCCTCCAGAGATGGTGTCAGAGCCCCTGGAGGACCTG
GACCCCTACTATATCAATAAGAAAACTTTTATAGTATTGAATAAAGGGAAGGCCATCTTC
CGGTTCAGTGCCACCTCTGCCCTGTACATTTTAACTCCCTTCAATCCTCTTAGGAAAATA
GCTATTAAGATTTTGGTACATTCATTATTCAGCATGCTAATTATGTGCACTATTTTGACA
AACTGTGTGTTTATGACAATGAGTAACCCTCCTGATTGGACAAAGAATGTAGAATACACC
TTCACAGGAATATATACTTTTGAATCACTTATAAAAATTATTGCAAGGGGATTCTGTTTA
GAAGATTTTACTTTCCTTCGGGATCCATGGAACTGGCTCGATTTCACTGTCATTACATTT
GCGTACGTCACAGAGTTTGTGGACCTGGGCAATGTCTCGGCATTGAGAACATTCAGAGTT
CTCCGAGCATTGAAGACGATTTCAGTCATTCCAGGCCTGAAAACCATTGTGGGAGCCCTG
ATCCAGTCTGTGAAGAAGCTCTCAGATGTAATGATCCTGACTGTGTTCTGTCTGAGCGTA
TTTGCTCTAATTGGGCTGCAGCTGTTCATGGGCAACCTGAGGAATAAATGTATACAATGG
CCTCCCACCAATGCTTCCTTGGAGGAACATAGTATAGAAAAGAATATAACTGTGAATTAT
AATGGTACACTTATAAATGAAACTGTCTTTGAGTTTGACTGGAAGTCATATATTCAAGAT
TCAAGATATCATTATTTCCTGGAGGGTTTTTTAGATGCACTACTATGTGGAAATAGCTCT
GATGCAGGCCAATGTCCAGAGGGATATATGTGTGTGAAAGCTGGTAGAAATCCCAATTAT
GGCTACACAAGCTTTGATACCTTCAGTTGGGCTTTTCTGTCCTTGTTTCGACTAATGACT
CAGGACTTCTGGGAAAATCTTTATCAACTGACATTACGTGCTGCTGGGAAAACGTACATG
ATATTTTTTGTGTTGGTCATTTTCTTGGGCTCATTCTACCTAATAAATTTGATCCTGGCT
GTGGTGGCCATGGCCTACGAGGAACAGAATCAGGCCACCTTGGAAGAAGCAGAACAGAAA
GAGGCCGAATTTCAGCAGATGATTGAACAGCTTAAAAAGCAACAGGAGGCAGCTCAGCAG
GCAGCAACGGCAACTGCCTCAGAACATTCCAGAGAGCCCAGTGCAGCAGGCAGGCTCTCA
GACAGCTCATCTGAAGCCTCTAAGTTGAGTTCCAAGAGTGCTAAGGAAAGAAGAAATCGG
AGGAAGAAAAGAAAACAGAAAGAGCAGTCTGGTGGGGAAGAGAAAGATGAGGATGAATTC
CAAAAATCTGAATCTGAGGACAGCATCAGGAGGAAAGGTTTTCGCTTCTCCATTGAAGGG
AACCGATTGACATATGAAAAGAGGTACTCCTCCCCACACCAGTCTTTGTTGAGCATCCGT
GGCTCCCTATTTTCACCAAGGCGAAATAGCAGAACAAGCCTTTTCAGCTTTAGAGGGCGT
GCAAAGGATGTGGGATCTGAGAACGACTTCGCAGATGATGAGCACAGCACCTTTGAGGAT
AACGAGAGCCGTAGAGATTCCTTGTTTGTGCCCCGACGACACGGAGAGAGACGCAACAGC
AACCTGAGTCAGACCAGTAGGTCATCCCGGATGCTGGCAGTGTTTCCAGCGAATGGGAAG
ATGCACAGCACTGTGGATTGCAATGGTGTGGTTTCCTTGGTTGGTGGACCTTCAGTTCCT
ACATCGCCTGTTGGACAGCTTCTGCCAGGGGGAACAACCACTGAAACTGAAATGAGAAAG
AGAAGGTCAAGTTCTTTCCACGTTTCCATGGACTTTCTAGAAGATCCTTCCCAAAGGCAA
CGAGCAATGAGTATAGCCAGCATTCTAACAAATACAGTAGAAGAACTTGAAGAATCCAGG
CAGAAATGCCCACCCTGTTGGTATAAATTTTCCAACATATTCTCAATCTGGGACTGTTCT
CCATATTGGTTAAAAGTGAAACATGTTGTCAACCTGGTCGTGATGGACCCATTTGTTGAC
CTGGCCATCACCATCTGTATTGTCTTAAATACTCTTTTCATGGCCATGGAGCACTATCCA
ATGACGGACCATTTCAATAATGTGCTTACAGTAGGAAACTTGGTTTTCACTGGGATCTTT
ACAGCAGAAATGTTTCTGAAAATTATTGCCATGGATCCTTACTATTATTTCCAAGAAGGC
TGGAATATCTTTGACGGTTTTATTGTGACGCTTAGCCTGGTAGAACTTGGACTCGCCAAT
GTGGAAGGATTATCTGTTCTCCGTTCATTTCGATTGCTGCGAGTTTTCAAGTTGGCAAAA
TCTTGGCCAACGTTAAATATGCTAATAAAGATCATCGGCAATTCCGTGGGGGCTCTGGGA
AATTTAACCCTCGTCTTGGCCATCATCGTCTTCATTTTTGCCGTGGTCGGCATGCAGCTC
TTTGGTAAAAGCTACAAAGATTGTGTCTGCAAGATCGCCAGTGATTGTCAACTCCCACAA
CGCTGGCACATGAATGACTTCTTCCACTCCTTCCTGATTGTGTTCCGCGTGCTGTGTGGG
GAGTGGATAGAGACCATGTGGGACTGTATGGAGGTTGCTGGTCAAGCCATGTGCCTTACT
GTCTTCATGATGGTCATGGTGATTGGAAACCTAGTGGTCCTGAATCTCTTTCTGGCCTTG
CTTCTGAGCTCATTTAGTGCAGACAACCTTGCAGCCACTGATGATGATAATGAAATGAAT
AATCTCCAAATTGCTGTGGATAGGATGCACAAAGGAGTAGCTTATGTGAAAAGAAAAATA
TATGAATTTATTCAACAGTCCTTCATTAGGAAACAAAAGATTTTAGATGAAATTAAACCA
CTTGATGATCTAAACAACAAGAAAGACAGTTGTATGTCCAATCATACAACAGAAATTGGG
AAAGATCTTGACTATCTTAAAGATGTAAATGGAACTACAAGTGGTATAGGAACTGGCAGC
AGTGTTGAAAAATACATTATTGATGAAAGTGATTACATGTCATTCATAAACAACCCCAGT
CTTACTGTGACTGTACCAATTGCTGTAGGAGAATCTGACTTTGAAAATTTAAACACGGAA
GACTTTAGTAGTGAATCGGATCTGGAAGAAAGCAAAGAGAAACTGAATGAAAGCAGTAGC
TCATCAGAAGGTAGCACTGTGGGACATCGGCGCCCTGTAGAAGAACAGCCCGTAGTGGAA
CCTGAAGAAACTCTTGAACCAGAAGCTTGTTTCACTGAAGGCTGTGTACAAAGATTCAAG
TGTTGTCAAATCAATGTGGAAGAAGGCAGAGGAAAACAATGGTGGAACCTGAGAAGGACG
TGTTTCCGAATAGTTGAACATAACTGGTTTGAGACCTTCATTGTTTTCATGATTCTCCTT
AGTAGTGGTGCTCTGGCATTTGAAGATATATATATTGATCAGCGAAAGACGATTAAGACG
ATGTTGGAATATGCTGACAAGGTTTTCACTTACATTTTCATTCTGGAAATGCTTCTAAAA
TGGGTGGCATATGGCTATCAAACATATTTCACCAATGCCTGGTGTTGGCTGGACTTCTTA
ATTGTTGATGTTTCATTGGTCAGTTTAACAGCAAATGCCTTGGGTTACTCAGAACTTGGA
GCCATCAAATCTCTCAGGACACTAAGAGCTCTGAGACCTCTAAGAGCCTTATCTCGATTT
GAAGGGATGAGGGTGGTTGTGAATGCCCTTTTAGGAGCAATTCCATCCATCATGAATGTG
CTTCTGGTTTGTCTTATATTCTGGCTAATTTTCAGCATCATGGGCGTAAATTTGTTTGCT
GGCAAATTCTACCACTGTATTAACACCACAACTGGTGACAGGTTTGACATCGAAGACGTG
AATAATCATACTGATTGCCTAAAACTAATAGAAAGAAATGAGACTGCTCGATGGAAAAAT
GTGAAAGTAAACTTTGATAATGTAGGATTTGGGTATCTCTCTTTGCTTCAAGTTGCCACA
TTCAAAGGATGGATGGATATAATGTATGCAGCAGTTGATTCCAGAAATGTGGAACTCCAG
CCTAAGTATGAAGAAAGTCTGTACATGTATCTTTACTTTGTTATTTTCATCATCTTTGGG
TCCTTCTTCACCTTGAACCTGTTTATTGGTGTCATCATAGATAATTTCAACCAGCAGAAA
AAGAAGTTTGGAGGTCAAGACATCTTTATGACAGAAGAACAGAAGAAATACTATAATGCA
ATGAAAAAATTAGGATCGAAAAAACCGCAAAAGCCTATACCTCGACCAGGAAACAAATTT
CAAGGAATGGTCTTTGACTTCGTAACCAGACAAGTTTTTGACATAAGCATCATGATTCTC
ATCTGTCTTAACATGGTCACAATGATGGTGGAAACAGATGACCAGAGTGAATATGTGACT
ACCATTTTGTCACGCATCAATCTGGTGTTCATTGTGCTATTTACTGGAGAGTGTGTACTG
AAACTCATCTCTCTACGCCATTATTATTTTACCATTGGATGGAATATTTTTGATTTTGTG
GTTGTCATTCTCTCCATTGTAGGTATGTTTCTTGCCGAGCTGATAGAAAAGTATTTCGTG
TCCCCTACCCTGTTCCGAGTGATCCGTCTTGCTAGGATTGGCCGAATCCTACGTCTGATC
AAAGGAGCAAAGGGGATCCGCACGCTGCTCTTTGCTTTGATGATGTCCCTTCCTGCGTTG
TTTAACATCGGCCTCCTACTCTTCCTAGTCATGTTCATCTACGCCATCTTTGGGATGTCC
AACTTTGCCTATGTTAAGAGGGAAGTTGGGATCGATGACATGTTCAACTTTGAGACCTTT
GGCAACAGCATGATCTGCCTATTCCAAATTACAACCTCTGCTGGCTGGGATGGATTGCTA
GCACCCATTCTCAACAGTAAGCCACCCGACTGTGACCCTAATAAAGTTAACCCTGGAAGC
TCAGTTAAGGGAGACTGTGGGAACCCATCTGTTGGAATTTTCTTTTTTGTCAGTTACATC
ATCATATCCTTCCTGGTTGTGGTGAACATGTACATCGCGGTCATCCTGGAGAACTTCAGT
GTTGCTACTGAAGAAAGTGCAGAGCCTCTGAGTGAGGATGACTTTGAGATGTTCTATGAG
GTTTGGGAGAAGTTTGATCCCGATGCAACTCAGTTCATGGAATTTGAAAAATTATCTCAG
TTTGCAGCTGCGCTTGAACCGCCTCTCAATCTGCCACAACCAAACAAACTCCAGCTCATT
GCCATGGATTTGCCCATGGTGAGTGGTGACCGGATCCACTGTCTTGATATCTTATTTGCT
TTTACAAAGCGGGTTCTAGGAGAGAGTGGAGAGATGGATGCTCTACGAATACAGATGGAA
GAGCGATTCATGGCTTCCAATCCTTCCAAGGTCTCCTATCAGCCAATCACTACTACTTTA
AAACGAAAACAAGAGGAAGTATCTGCTGTCATTATTCAGCGTGCTTACAGACGCCACCTT
TTAAAGCGAACTGTAAAACAAGCTTCCTTTACGTACAATAAAAACAAAATCAAAGGTGGG
GCTAATCTTCTTATAAAAGAAGACATGATAATTGACAGAATAAATGAAAACTCTATTACA
GAAAAAACTGATCTGACCATGTCCACTGCAGCTTGTCCACCTTCCTATGACCGGGTGACA
AAGCCAATTGTGGAAAAACATGAGCAAGAAGGCAAAGATGAAAAAGCCAAAGGGAAATAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID SCN1A Link Image
Target 1 GenAtlas ID SCN1A Link Image
Target 1 HGNC ID HGNC:10585 Link Image
Target 1 Chromosome Location 2
Target 1 Locus 2q24.3
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Escayg A, MacDonald BT, Meisler MH, Baulac S, Huberfeld G, An-Gourfinkel I, Brice A, LeGuern E, Moulard B, Chaigne D, Buresi C, Malafosse A: Mutations of SCN1A, encoding a neuronal sodium channel, in two families with GEFS+2. Nat Genet. 2000 Apr;24(4):343-5. [PubMed Link Image]
  2. Wallace RH, Scheffer IE, Barnett S, Richards M, Dibbens L, Desai RR, Lerman-Sagie T, Lev D, Mazarib A, Brand N, Ben-Zeev B, Goikhman I, Singh R, Kremmidiotis G, Gardner A, Sutherland GR, George AL Jr, Mulley JC, Berkovic SF: Neuronal sodium-channel alpha1-subunit mutations in generalized epilepsy with febrile seizures plus. Am J Hum Genet. 2001 Apr;68(4):859-65. Epub 2001 Mar 13. [PubMed Link Image]
  3. Escayg A, Heils A, MacDonald BT, Haug K, Sander T, Meisler MH: A novel SCN1A mutation associated with generalized epilepsy with febrile seizures plus--and prevalence of variants in patients with epilepsy. Am J Hum Genet. 2001 Apr;68(4):866-73. Epub 2001 Mar 14. [PubMed Link Image]
  4. Claes L, Del-Favero J, Ceulemans B, Lagae L, Van Broeckhoven C, De Jonghe P: De novo mutations in the sodium-channel gene SCN1A cause severe myoclonic epilepsy of infancy. Am J Hum Genet. 2001 Jun;68(6):1327-32. Epub 2001 May 15. [PubMed Link Image]
  5. Abou-Khalil B, Ge Q, Desai R, Ryther R, Bazyk A, Bailey R, Haines JL, Sutcliffe JS, George AL Jr: Partial and generalized epilepsy with febrile seizures plus and a novel SCN1A mutation. Neurology. 2001 Dec 26;57(12):2265-72. [PubMed Link Image]
  6. Lu CM, Han J, Rado TA, Brown GB: Differential expression of two sodium channel subtypes in human brain. FEBS Lett. 1992 May 25;303(1):53-8. [PubMed Link Image]
  7. Malo MS, Blanchard BJ, Andresen JM, Srivastava K, Chen XN, Li X, Jabs EW, Korenberg JR, Ingram VM: Localization of a putative human brain sodium channel gene (SCN1A) to chromosome band 2q24. Cytogenet Cell Genet. 1994;67(3):178-86. [PubMed Link Image]
Target 1 Drug References
  1. Kanazawa O: Refractory grand mal seizures with onset during infancy including severe myoclonic epilepsy in infancy. Brain Dev. 2001 Nov;23(7):749-56. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 295
Target 2 Name Carbonic anhydrase 1
Target 2 Synonyms
  1. CA-I
  2. Carbonate dehydratase I
  3. Carbonic anhydrase I
  4. EC 4.2.1.1
Target 2 Gene Name CA1
Target 2 Protein Sequence >Carbonic anhydrase 1 
ASPDWGYDDKNGPEQWSKLYPIANGNNQSPVDIKTSETKHDTSLKPISVSYNPATAKEII
NVGHSFHVNFEDNDNRSVLKGGPFSDSYRLFQFHFHWGSTNEHGSEHTVDGVKYSAELHV
AHWNSAKYSSLAEAASKADGLAVIGVLMKVGEANPKLQKVLDALQAIKTKGKRAPFTNFD
PSTLLPSSLDFWTYPGSLTHPPLYESVTWIICKESISVSSEQLAQFRSLLSNVEGDNAVP
MQHNNRPTQPLKGRTVRASF
Target 2 Number of Residues 264
Target 2 Molecular Weight 28739
Target 2 Theoretical pI 7.14
Target 2 GO Classification
Function
binding
ion binding
cation binding
transition metal ion binding
zinc ion binding
catalytic activity
lyase activity
carbon-oxygen lyase activity
hydro-lyase activity
carbonate dehydratase activity
Process
physiological process
metabolism
cellular metabolism
one-carbon compound metabolism
Component
Not Available
Target 2 General Function Inorganic ion transport and metabolism
Target 2 Specific Function Reversible hydration of carbon dioxide
Target 2 Pathways
Name SMPDB Link KEGG Link
Nitrogen metabolism map00910 Link Image
Target 2 Reactions
  • H2CO3 = CO2 + H2O
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 29600 Link Image
Target 2 UniProtKB/Swiss-Prot ID P00915 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name CAH1_HUMAN Link Image
Target 2 PDB ID 1CZM Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Cytoplasm
Target 2 Gene Sequence >786 bp 
ATGGCAAGTCCAGACTGGGGATATGATGACAAAAATGGTCCTGAACAATGGAGCAAGCTG
TATCCCATTGCCAATGGAAATAACCAATCCCCTGTTGATATTAAAACCAGTGAAACCAAA
CATGACACCTCTCTGAAACCTATTAGTGTCTCCTACAACCCAGCCACAGCCAAAGAAATT
ATCAATGTGGGGCATTCTTTCCATGTAAATTTTGAGGACAACGATAACCGATCAGTGCTG
AAAGGTGGTCCTTTCTCTGACAGCTACAGGCTCTTTCAGTTTCATTTTCACTGGGGCAGT
ACAAATGAGCATGGTTCAGAACATACAGTGGATGGAGTCAAATATTCTGCCGAGCTTCAC
GTAGCTCACTGGAATTCTGCAAAGTACTCCAGCCTTGCTGAAGCTGCCTCAAAGGCTGAT
GGTTTGGCAGTTATTGGTGTTTTGATGAAGGTTGGTGAGGCCAACCCAAAGCTGCAGAAA
GTACTTGATGCCCTCCAAGCAATTAAAACCAAGGGCAAACGAGCCCCATTCACAAATTTT
GACCCCTCTACTCTCCTTCCTTCATCCCTGGATTTCTGGACCTACCCTGGCTCTCTGACT
CATCCTCCTCTTTATGAGAGTGTAACTTGGATCATCTGTAAGGAGAGCATCAGTGTCAGC
TCAGAGCAGCTGGCACAATTCCGCAGCCTTCTATCAAATGTTGAAGGTGATAACGCTGTC
CCCATGCAGCACAACAACCGCCCAACCCAACCTCTGAAGGGCAGAACAGTGAGAGCTTCA
TTTTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID CA1 Link Image
Target 2 GenAtlas ID CA1 Link Image
Target 2 HGNC ID HGNC:1368 Link Image
Target 2 Chromosome Location 8
Target 2 Locus 8q13-q22.1
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Lowe N, Brady HJ, Barlow JH, Sowden JC, Edwards M, Butterworth PH: Structure and methylation patterns of the gene encoding human carbonic anhydrase I. Gene. 1990 Sep 14;93(2):277-83. [PubMed Link Image]
  2. Barlow JH, Lowe N, Edwards YH, Butterworth PH: Human carbonic anhydrase I cDNA. Nucleic Acids Res. 1987 Mar 11;15(5):2386. [PubMed Link Image]
  3. Lin KT, Deutsch HF: Human carbonic anhydrases. XII. The complete primary structure of the C isozyme. J Biol Chem. 1974 Apr 25;249(8):2329-37. [PubMed Link Image]
  4. Giraud N, Marriq C, Laurent-Tabusse G: [Primary structure of human B erythrocyte carbonic anhydrase. 3. Sequence of CNBr fragment I and III (residues 149-260)] Biochimie. 1974;56(8):1031-43. [PubMed Link Image]
  5. Andersson B, Nyman PO, Strid L: Amino acid sequence of human erythrocyte carbonic anhydrase B. Biochem Biophys Res Commun. 1972 Aug 7;48(3):670-7. [PubMed Link Image]
  6. Lin KT, Deutsch HF: Human carbonic anhydrases. XI. The complete primary structure of carbonic anhydrase B. J Biol Chem. 1973 Mar 25;248(6):1885-93. [PubMed Link Image]
  7. Omoto K, Ueda S, Goriki K, Takahashi N, Misawa S, Pagaran IG: Population genetic studies of the Philippine Negritos. III. Identification of the carbonic anhydrase-1 variant with CA1 Guam. Am J Hum Genet. 1981 Jan;33(1):105-11. [PubMed Link Image]
  8. Chegwidden WR, Wagner LE, Venta PJ, Bergenhem NC, Yu YS, Tashian RE: Marked zinc activation of ester hydrolysis by a mutation, 67-His (CAT) to Arg (CGT), in the active site of human carbonic anhydrase I. Hum Mutat. 1994;4(4):294-6. [PubMed Link Image]
  9. Kannan KK, Notstrand B, Fridborg K, Lovgren S, Ohlsson A, Petef M: Crystal structure of human erythrocyte carbonic anhydrase B. Three-dimensional structure at a nominal 2.2-A resolution. Proc Natl Acad Sci U S A. 1975 Jan;72(1):51-5. [PubMed Link Image]
Target 2 Drug References
  1. Kitano Y, Komiyama C, Makino M, Takasuna K, Satoh H, Aoki T, Kinoshita M, Takazawa A, Yamauchi T, Sakurada S: Anticonvulsant and neuroprotective effects of the novel nootropic agent nefiracetam on kainic acid-induced seizures in rats. Brain Res. 2005 Sep 28;1057(1-2):168-76. [PubMed Link Image]
  2. Hayakawa T, Higuchi Y, Nigami H, Hattori H: Zonisamide reduces hypoxic-ischemic brain damage in neonatal rats irrespective of its anticonvulsive effect. Eur J Pharmacol. 1994 May 12;257(1-2):131-6. [PubMed Link Image]
  3. Masuda Y, Karasawa T: Inhibitory effect of zonisamide on human carbonic anhydrase in vitro. Arzneimittelforschung. 1993 Apr;43(4):416-8. [PubMed Link Image]
  4. Owen AJ, Ijaz S, Miyashita H, Wishart T, Howlett W, Shuaib A: Zonisamide as a neuroprotective agent in an adult gerbil model of global forebrain ischemia: a histological, in vivo microdialysis and behavioral study. Brain Res. 1997 Oct 3;770(1-2):115-22. [PubMed Link Image]
  5. Nagatomo I, Akasaki Y, Uchida M, Kuchiiwa S, Nakagawa S, Takigawa M: Influence of dietary zinc on convulsive seizures and hippocampal NADPH diaphorase-positive neurons in seizure susceptible EL mouse. Brain Res. 1998 Apr 13;789(2):213-20. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 535
Target 3 Name Voltage-dependent T-type calcium channel subunit alpha-1G
Target 3 Synonyms
  1. Cav3.1c
  2. NBR13
  3. Voltage- gated calcium channel subunit alpha Cav3.1
Target 3 Gene Name CACNA1G
Target 3 Protein Sequence >Voltage-dependent T-type calcium channel subunit alpha-1G 
MDEEEDGAGAEESGQPRSFMRLNDLSGAGGRPGPGSAEKDPGSADSEAEGLPYPALAPVV
FFYLSQDSRPRSWCLRTVCNPWFERISMLVILLNCVTLGMFRPCEDIACDSQRCRILQAF
DDFIFAFFAVEMVVKMVALGIFGKKCYLGDTWNRLDFFIVIAGMLEYSLDLQNVSFSAVR
TVRVLRPLRAINRVPSMRILVTLLLDTLPMLGNVLLLCFFVFFIFGIVGVQLWAGLLRNR
CFLPENFSLPLSVDLERYYQTENEDESPFICSQPRENGMRSCRSVPTLRGDGGGGPPCGL
DYEAYNSSSNTTCVNWNQYYTNCSAGEHNPFKGAINFDNIGYAWIAIFQVITLEGWVDIM
YFVMDAHSFYNFIYFILLIIVGSFFMINLCLVVIATQFSETKQRESQLMREQRVRFLSNA
STLASFSEPGSCYEELLKYLVYILRKAARRLAQVSRAAGVRVGLLSSPAPLGGQETQPSS
SCSRSHRRLSVHHLVHHHHHHHHHYHLGNGTLRAPRASPEIQDRDANGSRRLMLPPPSTP
ALSGAPPGGAESVHSFYHADCHLEPVRCQAPPPRSPSEASGRTVGSGKVYPTVHTSPPPE
TLKEKALVEVAASSGPPTLTSLNIPPGPYSSMHKLLETQSTGACQSSCKISSPCLKADSG
ACGPDSCPYCARAGAGEVELADREMPDSDSEAVYEFTQDAQHSDLRDPHSRRQRSLGPDA
EPSSVLAFWRLICDTFRKIVDSKYFGRGIMIAILVNTLSMGIEYHEQPEELTNALEISNI
VFTSLFALEMLLKLLVYGPFGYIKNPYNIFDGVIVVISVWEIVGQQGGGLSVLRTFRLMR
VLKLVRFLPALQRQLVVLMKTMDNVATFCMLLMLFIFIFSILGMHLFGCKFASERDGDTL
PDRKNFDSLLWAIVTVFQILTQEDWNKVLYNGMASTSSWAALYFIALMTFGNYVLFNLLV
AILVEGFQAEEISKREDASGQLSCIQLPVDSQGGDANKSESEPDFFSPSLDGDGDRKKCL
ALVSLGEHPELRKSLLPPLIIHTAATPMSLPKSTSTGLGEALGPASRRTSSSGSAEPGAA
HEMKSPPSARSSPHSPWSAASSWTSRRSSRNSLGRAPSLKRRSPSGERRSLLSGEGQESQ
DEEESSEEERASPAGSDHRHRGSLEREAKSSFDLPDTLQVPGLHRTASGRGSASEHQDCN
GKSASGRLARALRPDDPPLDGDDADDEGNLSKGERVRAWIRARLPACCLERDSWSAYIFP
PQSRFRLLCHRIITHKMFDHVVLVIIFLNCITIAMERPKIDPHSAERIFLTLSNYIFTAV
FLAEMTVKVVALGWCFGEQAYLRSSWNVLDGLLVLISVIDILVSMVSDSGTKILGMLRVL
RLLRTLRPLRVISRAQGLKLVVETLMSSLKPIGNIVVICCAFFIIFGILGVQLFKGKFFV
CQGEDTRNITNKSDCAEASYRWVRHKYNFDNLGQALMSLFVLASKDGWVDIMYDGLDAVG
VDQQPIMNHNPWMLLYFISFLLIVAFFVLNMFVGVVVENFHKCRQHQEEEEARRREEKRL
RRLEKKRRNLMLDDVIASGSSASAASEAQCKPYYSDYSRFRLLVHHLCTSHYLDLFITGV
IGLNVVTMAMEHYQQPQILDEALKICNYIFTVIFVLESVFKLVAFGFRRFFQDRWNQLDL
AIVLLSIMGITLEEIEVNASLPINPTIIRIMRVLRIARVLKLLKMAVGMRALLDTVMQAL
PQVGNLGLLFMLLFFIFAALGVELFGDLECDETHPCEGLGRHATFRNFGMAFLTLFRVST
GDNWNGIMKDTLRDCDQESTCYNTVISPIYFVSFVLTAQFVLVNVVIAVLMKHLEESNKE
AKEEAELEAELELEMKTLSPQPHSPLGSPFLWPGVEGPDSPDSPKPGALHPAAHARSASH
FSLEHPTDRQLFDTISLLIQGSLEWELKLMDELAGPGGQPSAFPSAPSLGGSDPQIPLAE
MEALSLTSEIVSEPSCSLALTDDSLPDDMHTLLLSALESNMQPHPTELPGPDLLTVRKSG
VSRTHSLPNDSYMCRHGSTAEGPLGHRGWGLPKAQSGSVLSVHSQPADTSYILQLPKDAP
HLLQPHSAPTWGTIPKLPPPGRSPLAQRPLRRQAAIRTDSLDVQGLGSREDLLAEVSGPS
PPLARAYSFWGQSSTQAQQHSRSHSKISKHMTPPAPCPGPEPNWGKGPPETRSSLELDTE
LSWISGDLLPPGGQEEPPSPRDLKKCYSVEAQSCQRRPTSWLDEQRRHSIAVSCLDSGSQ
PHLGTDPSNLGGQPLGGPGSRPKKKLSPPSITIDPPESQGPRTPPSPGICLRRRAPSSDS
KDPLASGPPDSMAASPSPKKDVLSLSGLSSDPADLDP
Target 3 Number of Residues 2416
Target 3 Molecular Weight 262474
Target 3 Theoretical pI 6.57
Target 3 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
voltage-gated ion channel activity
voltage-gated calcium channel activity
Process
physiological process
cellular physiological process
transport
ion transport
cation transport
di-, tri-valent inorganic cation transport
calcium ion transport
Component
intrinsic to membrane
integral to membrane
cell
membrane
protein complex
voltage-gated calcium channel complex
Target 3 General Function Involved in voltage-gated calcium channel activity
Target 3 Specific 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. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the "low-voltage activated (LVA)" group and are strongly blocked by mibefradil. A particularity of this type of channels is an opening at quite negative potentials and a voltage-dependent inactivation. T-type channels serve pacemaking 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 firing patterns of neurons which is important for information processing as well as in cell growth processes
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 81-101
  • 120-141
  • 151-170
  • 176-193
  • 214-234
  • 371-395
  • 744-764
  • 778-799
  • 806-824
  • 833-856
  • 868-888
  • 940-964
  • 1273-1295
  • 1314-1334
  • 1345-1364
  • 1379-1400
  • 1411-1434
  • 1512-1537
  • 1611-1631
  • 1646-1667
  • 1675-1693
  • 1708-1731
  • 1746-1766
  • 1827-1854
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 6625659 Link Image
Target 3 UniProtKB/Swiss-Prot ID O43497 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name CAC1G_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >7134 bp 
ATGGACGAGGAGGAGGATGGAGCGGGCGCCGAGGAGTCGGGACAGCCCCGGAGCTTCATG
CGGCTCAACGACCTGTCGGGGGCCGGGGGCCGGCCGGGGCCGGGGTCAGCAGAAAAGGAC
CCGGGCAGCGCGGACTCCGAGGCGGAGGGGCTGCCGTACCCGGCGCTGGCCCCGGTGGTT
TTCTTCTACTTGAGCCAGGACAGCCGCCCGCGGAGCTGGTGTCTCCGCACGGTCTGTAAC
CCCTGGTTTGAGCGCATCAGCATGTTGGTCATCCTTCTCAACTGCGTGACCCTGGGCATG
TTCCGGCCATGCGAGGACATCGCCTGTGACTCCCAGCGCTGCCGGATCCTGCAGGCCTTT
GATGACTTCATCTTTGCCTTCTTTGCCGTGGAGATGGTGGTGAAGATGGTGGCCTTGGGC
ATCTTTGGGAAAAAGTGTTACCTGGGAGACACTTGGAACCGGCTTGACTTTTTCATCGTC
ATCGCAGGGATGCTGGAGTACTCGCTGGACCTGCAGAACGTCAGCTTCTCAGCTGTCAGG
ACAGTCCGTGTGCTGCGACCGCTCAGGGCCATTAACCGGGTGCCCAGCATGCGCATCCTT
GTCACGTTGCTGCTGGATACGCTGCCCATGCTGGGCAACGTCCTGCTGCTCTGCTTCTTC
GTCTTCTTCATCTTCGGCATCGTCGGCGTCCAGCTGTGGGCAGGGCTGCTTCGGAACCGA
TGCTTCCTACCTGAGAATTTCAGCCTCCCCCTGAGCGTGGACCTGGAGCGCTATTACCAG
ACAGAGAACGAGGATGAGAGCCCCTTCATCTGCTCCCAGCCACGCGAGAACGGCATGCGG
TCCTGCAGAAGCGTGCCCACGCTGCGCGGGGACGGGGGCGGTGGCCCACCTTGCGGTCTG
GACTATGAGGCCTACAACAGCTCCAGCAACACCACCTGTGTCAACTGGAACCAGTACTAC
ACCAACTGCTCAGCGGGGGAGCACAACCCCTTCAAGGGCGCCATCAACTTTGACAACATT
GGCTATGCCTGGATCGCCATCTTCCAGGTCATCACGCTGGAGGGCTGGGTCGACATCATG
TACTTTGTGATGGATGCTCATTCCTTCTACAATTTCATCTACTTCATCCTCCTCATCATC
GTGGGCTCCTTCTTCATGATCAACCTGTGCCTGGTGGTGATTGCCACGCAGTTCTCAGAG
ACCAAGCAGCGGGAAAGCCAGCTGATGCGGGAGCAGCGTGTGCGGTTCCTGTCCAACGCC
AGCACCCTGGCTAGCTTCTCTGAGCCCGGCAGCTGCTATGAGGAGCTGCTCAAGTACCTG
GTGTACATCCTTCGTAAGGCAGCCCGCAGGCTGGCTCAGGTCTCTCGGGCAGCAGGTGTG
CGGGTTGGGCTGCTCAGCAGCCCAGCACCCCTCGGGGGCCAGGAGACCCAGCCCAGCAGC
AGCTGCTCTCGCTCCCACCGCCGCCTATCCGTCCACCACCTGGTGCACCACCACCACCAC
CATCACCACCACTACCACCTGGGCAATGGGACGCTCAGGGCCCCCCGGGCCAGCCCGGAG
ATCCAGGACAGGGATGCCAATGGGTCCCGCAGGCTCATGCTGCCACCACCCTCGACGCCT
GCCCTCTCCGGGGCCCCCCCTGGTGGCGCAGAGTCTGTGCACAGCTTCTACCATGCCGAC
TGCCACTTAGAGCCAGTCCGCTGCCAGGCGCCCCCTCCCAGGTCCCCATCTGAGGCATCC
GGCAGGACTGTGGGCAGCGGGAAGGTGTATCCCACCGTGCACACCAGCCCTCCACCGGAG
ACGCTGAAGGAGAAGGCACTAGTAGAGGTGGCTGCCAGCTCTGGGCCCCCAACCCTCACC
AGCCTCAACATCCCACCCGGGCCCTACAGCTCCATGCACAAGCTGCTGGAGACACAGAGT
ACAGGTGCCTGCCAAAGCTCTTGCAAGATCTCCAGCCCTTGCTTGAAAGCAGACAGTGGA
GCCTGTGGTCCAGACAGCTGCCCCTACTGTGCCCGGGCCGGGGCAGGGGAGGTGGAGCTC
GCCGACCGTGAAATGCCTGACTCAGACAGCGAGGCAGTTTATGAGTTCACACAGGATGCC
CAGCACAGCGACCTCCGGGACCCCCACAGCCGGCGGCAACGGAGCCTGGGCCCAGATGCA
GAGCCCAGCTCTGTGCTGGCCTTCTGGAGGCTAATCTGTGACACCTTCCGAAAGATTGTG
GACAGCAAGTACTTTGGCCGGGGAATCATGATCGCCATCCTGGTCAACACACTCAGCATG
GGCATCGAATACCACGAGCAGCCCGAGGAGCTTACCAACGCCCTAGAAATCAGCAACATC
GTCTTCACCAGCCTCTTTGCCCTGGAGATGCTGCTGAAGCTGCTTGTGTATGGTCCCTTT
GGCTACATCAAGAATCCCTACAACATCTTCGATGGTGTCATTGTGGTCATCAGCGTGTGG
GAGATCGTGGGCCAGCAGGGGGGCGGCCTGTCGGTGCTGCGGACCTTCCGCCTGATGCGT
GTGCTGAAGCTGGTGCGCTTCCTGCCGGCGCTGCAGCGGCAGCTGGTGGTGCTCATGAAG
ACCATGGACAACGTGGCCACCTTCTGCATGCTGCTTATGCTCTTCATCTTCATCTTCAGC
ATCCTGGGCATGCATCTCTTCGGCTGCAAGTTTGCCTCTGAGCGGGATGGGGACACCCTG
CCAGACCGGAAGAATTTTGACTCCTTGCTCTGGGCCATCGTCACTGTCTTTCAGATCCTG
ACCCAGGAGGACTGGAACAAAGTCCTCTACAATGGTATGGCCTCCACGTCGTCCTGGGCG
GCCCTTTATTTCATTGCCCTCATGACCTTCGGCAACTACGTGCTCTTCAATTTGCTGGTC
GCCATTCTGGTGGAGGGCTTCCAGGCGGAGGAAATCAGCAAACGGGAAGATGCGAGTGGA
CAGTTAAGCTGTATTCAGCTGCCTGTCGACTCCCAGGGGGGAGATGCCAACAAGTCCGAA
TCAGAGCCCGATTTCTTCTCACCCAGCCTGGATGGTGATGGGGACAGGAAGAAGTGCTTG
GCCTTGGTGTCCCTGGGAGAGCACCCGGAGCTGCGGAAGAGCCTGCTGCCGCCTCTCATC
ATCCACACGGCCGCCACACCCATGTCGCTGCCCAAGAGCACCAGCACGGGCCTGGGCGAG
GCGCTGGGCCCTGCGTCGCGCCGCACCAGCAGCAGCGGGTCGGCAGAGCCTGGGGCGGCC
CACGAGATGAAGTCACCGCCCAGCGCCCGCAGCTCTCCGCACAGCCCCTGGAGCGCTGCA
AGCAGCTGGACCAGCAGGCGCTCCAGCCGGAACAGCCTCGGCCGTGCACCCAGCCTGAAG
CGGAGAAGCCCAAGTGGAGAGCGGCGGTCCCTGTTGTCGGGAGAAGGCCAGGAGAGCCAG
GATGAAGAGGAGAGCTCAGAAGAGGAGCGGGCCAGCCCTGCGGGCAGTGACCATCGCCAC
AGGGGGTCCCTGGAGCGGGAGGCCAAGAGTTCCTTTGACCTGCCAGACACACTGCAGGTG
CCAGGGCTGCATCGCACTGCCAGTGGCCGAGGGTCTGCTTCTGAGCACCAGGACTGCAAT
GGCAAGTCGGCTTCAGGGCGCCTGGCCCGGGCCCTGCGGCCTGATGACCCCCCACTGGAT
GGGGATGACGCCGATGACGAGGGCAACCTGAGCAAAGGGGAACGGGTCCGCGCGTGGATC
CGAGCCCGACTCCCTGCCTGCTGCCTCGAGCGAGACTCCTGGTCAGCCTACATCTTCCCT
CCTCAGTCCAGGTTCCGCCTCCTGTGTCACCGGATCATCACCCACAAGATGTTCGACCAC
GTGGTCCTTGTCATCATCTTCCTTAACTGCATCACCATCGCCATGGAGCGCCCCAAAATT
GACCCCCACAGCGCTGAACGCATCTTCCTGACCCTCTCCAATTACATCTTCACCGCAGTC
TTTCTGGCTGAAATGACAGTGAAGGTGGTGGCACTGGGCTGGTGCTTCGGGGAGCAGGCG
TACCTGCGGAGCAGTTGGAACGTGCTGGACGGGCTGTTGGTGCTCATCTCCGTCATCGAC
ATTCTGGTGTCCATGGTCTCTGACAGCGGCACCAAGATCCTGGGCATGCTGAGGGTGCTG
CGGCTGCTGCGGACCCTGCGCCCGCTCAGGGTGATCAGCCGGGCGCAGGGGCTGAAGCTG
GTGGTGGAGACGCTGATGTCCTCACTGAAACCCATCGGCAACATTGTAGTCATCTGCTGT
GCCTTCTTCATCATTTTCGGCATCTTGGGGGTGCAGCTCTTCAAAGGGAAGTTTTTCGTG
TGCCAGGGCGAGGATACCAGGAACATCACCAATAAATCGGACTGTGCCGAGGCCAGTTAC
CGGTGGGTCCGGCACAAGTACAACTTTGACAACCTTGGCCAGGCCCTGATGTCCCTGTTC
GTTTTGGCCTCCAAGGATGGTTGGGTGGACATCATGTACGATGGGCTGGATGCTGTGGGC
GTGGACCAGCAGCCCATCATGAACCACAACCCCTGGATGCTGCTGTACTTCATCTCGTTC
CTGCTCATTGTGGCCTTCTTTGTCCTGAACATGTTTGTGGGTGTGGTGGTGGAGAACTTC
CACAAGTGTCGGCAGCACCAGGAGGAAGAGGAGGCCCGGCGGCGGGAGGAGAAGCGCCTA
CGAAGACTGGAGAAAAAGAGAAGGAATCTAATGCTGGACGATGTAATTGCTTCCGGCAGC
TCAGCCAGCGCTGCGTCAGAAGCCCAGTGCAAACCTTACTACTCCGACTACTCCCGCTTC
CGGCTCCTCGTCCACCACTTGTGCACCAGCCACTACCTGGACCTCTTCATCACAGGTGTC
ATCGGGCTGAACGTGGTCACCATGGCCATGGAGCACTACCAGCAGCCCCAGATTCTGGAT
GAGGCTCTGAAGATCTGCAACTACATCTTCACTGTCATCTTTGTCTTGGAGTCAGTTTTC
AAACTTGTGGCCTTTGGTTTCCGTCGGTTCTTCCAGGACAGGTGGAACCAGCTGGACCTG
GCCATTGTGCTGCTGTCCATCATGGGCATCACGCTGGAGGAAATCGAGGTCAACGCCTCG
CTGCCCATCAACCCCACCATCATCCGCATCATGAGGGTGCTGCGCATTGCCCGAGTGCTG
AAGCTGCTGAAGATGGCTGTGGGCATGCGGGCGCTGCTGGACACGGTGATGCAGGCCCTG
CCCCAGGTGGGGAACCTGGGACTTCTCTTCATGTTGTTGTTTTTCATCTTTGCAGCTCTG
GGCGTGGAGCTCTTTGGAGACCTGGAGTGTGACGAGACACACCCCTGTGAGGGCCTGGGC
CGTCATGCCACCTTTCGGAACTTTGGCATGGCCTTCCTAACCCTCTTCCGAGTCTCCACA
GGTGACAATTGGAATGGCATTATGAAGGACACCCTCCGGGACTGTGACCAGGAGTCCACC
TGCTACAACACGGTCATCTCGCCTATCTACTTTGTGTCCTTCGTGCTGACGGCCCAGTTC
GTGCTAGTCAACGTGGTGATCGCCGTGCTGATGAAGCACCTGGAGGAGAGCAACAAGGAG
GCCAAGGAGGAGGCCGAGCTAGAGGCTGAGCTGGAGCTGGAGATGAAGACCCTCAGCCCC
CAGCCCCACTCGCCACTGGGCAGCCCCTTCCTCTGGCCTGGGGTCGAGGGCCCCGACAGC
CCCGACAGCCCCAAGCCTGGGGCTCTGCACCCAGCGGCCCACGCGAGATCAGCCTCCCAC
TTTTCCCTGGAGCACCCCACGGACAGGCAGCTGTTTGACACCATATCCCTGCTGATCCAG
GGCTCCCTGGAGTGGGAGCTGAAGCTGATGGACGAGCTGGCAGGCCCAGGGGGCCAGCCC
TCTGCCTTCCCTTCTGCCCCCAGCCTGGGAGGCTCCGACCCACAGATCCCTCTAGCTGAG
ATGGAGGCTCTGTCTCTGACGTCAGAGATTGTGTCTGAACCGTCCTGCTCTCTAGCTCTG
ACGGATGACTCTTTGCCTGATGACATGCACACACTCTTACTTAGTGCCCTGGAGAGCAAT
ATGCAGCCCCACCCCACGGAGCTGCCAGGACCAGACTTACTGACTGTGCGGAAGTCTGGG
GTCAGCCGAACGCACTCTCTGCCCAATGACAGCTACATGTGTCGGCATGGGAGCACTGCC
GAGGGGCCCCTGGGACACAGGGGCTGGGGGCTCCCCAAAGCTCAGTCAGGCTCCGTCTTG
TCCGTTCACTCCCAGCCAGCAGATACCAGCTACATCCTGCAGCTTCCCAAAGATGCACCT
CATCTGCTCCAGCCCCACAGCGCCCCAACCTGGGGCACCATCCCCAAACTGCCCCCACCA
GGACGCTCCCCTTTGGCTCAGAGGCCACTCAGGCGCCAGGCAGCAATAAGGACTGACTCC
TTGGACGTTCAGGGTCTGGGCAGCCGGGAAGACCTGCTGGCAGAGGTGAGTGGGCCCTCC
CCGCCCCTGGCCCGGGCCTACTCTTTCTGGGGCCAGTCAAGTACCCAGGCACAGCAGCAC
TCCCGCAGCCACAGCAAGATCTCCAAGCACATGACCCCGCCAGCCCCTTGCCCAGGCCCA
GAACCCAACTGGGGCAAGGGCCCTCCAGAGACCAGAAGCAGCTTAGAGTTGGACACGGAG
CTGAGCTGGATTTCAGGAGACCTCCTGCCCCCTGGCGGCCAGGAGGAGCCCCCATCCCCA
CGGGACCTGAAGAAGTGCTACAGCGTGGAGGCCCAGAGCTGCCAGCGCCGGCCTACGTCC
TGGCTGGATGAGCAGAGGAGACACTCTATCGCCGTCAGCTGCCTGGACAGCGGCTCCCAA
CCCCACCTGGGCACAGACCCCTCTAACCTTGGGGGCCAGCCTCTTGGGGGGCCTGGGAGC
CGGCCCAAGAAAAAACTCAGCCCGCCTAGTATCACCATAGACCCCCCCGAGAGCCAAGGT
CCTCGGACCCCGCCCAGCCCTGGTATCTGCCTCCGGAGGAGGGCTCCGTCCAGCGACTCC
AAGGATCCCTTGGCCTCTGGCCCCCCTGACAGCATGGCTGCCTCGCCCTCCCCAAAGAAA
GATGTGCTGAGTCTCTCCGGTTTATCCTCTGACCCAGCAGACCTGGACCCCTGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID CACNA1G Link Image
Target 3 GenAtlas ID CACNA1G Link Image
Target 3 HGNC ID HGNC:1394 Link Image
Target 3 Chromosome Location 17
Target 3 Locus 17q22
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Toyota M, Ho C, Ohe-Toyota M, Baylin SB, Issa JP: Inactivation of CACNA1G, a T-type calcium channel gene, by aberrant methylation of its 5' CpG island in human tumors. Cancer Res. 1999 Sep 15;59(18):4535-41. [PubMed Link Image]
  2. Mittman S, Guo J, Agnew WS: Structure and alternative splicing of the gene encoding alpha1G, a human brain T calcium channel alpha1 subunit. Neurosci Lett. 1999 Oct 29;274(3):143-6. [PubMed Link Image]
  3. Hirosawa M, Nagase T, Ishikawa K, Kikuno R, Nomura N, Ohara O: Characterization of cDNA clones selected by the GeneMark analysis from size-fractionated cDNA libraries from human brain. DNA Res. 1999 Oct 29;6(5):329-36. [PubMed Link Image]
  4. Cribbs LL, Gomora JC, Daud AN, Lee JH, Perez-Reyes E: Molecular cloning and functional expression of Ca(v)3.1c, a T-type calcium channel from human brain. FEBS Lett. 2000 Jan 21;466(1):54-8. [PubMed Link Image]
  5. Monteil A, Chemin J, Bourinet E, Mennessier G, Lory P, Nargeot J: Molecular and functional properties of the human alpha(1G) subunit that forms T-type calcium channels. J Biol Chem. 2000 Mar 3;275(9):6090-100. [PubMed Link Image]
  6. Nakajima D, Okazaki N, Yamakawa H, Kikuno R, Ohara O, Nagase T: Construction of expression-ready cDNA clones for KIAA genes: manual curation of 330 KIAA cDNA clones. DNA Res. 2002 Jun 30;9(3):99-106. [PubMed Link Image]
  7. Perez-Reyes E, Cribbs LL, Daud A, Lacerda AE, Barclay J, Williamson MP, Fox M, Rees M, Lee JH: Molecular characterization of a neuronal low-voltage-activated T-type calcium channel. Nature. 1998 Feb 26;391(6670):896-900. [PubMed Link Image]
Target 3 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.