Therapeutic Targets Database
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TTD Target ID: TTDS00161

Target Information
NameVoltage-dependent T-type calcium channel alpha-1G subunit    
Type of targetSuccessful target    
SynonymsCav    
Cav3.1c    
NBR13    
Voltage-dependent T-type calcium channel    
Voltage-gated calcium channel alpha subunit Cav3.1    
DiseaseAnalgesics    [1]
Angina pectoris    [2]
Cardiac dysrhythmias    [3]
Cardiovascular disease, unspecified    [4]
Epilepsy    [5]
Heart failure    [3]
Hypertension    [6]
Hypoinsulinemia    [7]
Neuropathic pain    [1]
Drug(s)EthosuximideApprovedEpilepsy[8][9][10]
MethsuximideApprovedEpileptic seizures[9]
ParamethadioneApprovedParamethadione syndrome[11]
PregabalinApprovedNeuropathic pain [1]
TrimethadioneApprovedEpileptic conditions[11]
VerapamilApprovedHypertension and angina[12][13]
Gabapentin enacarbilPhase IIMigraine prophylaxis and neuropathic pain[14]
MibefradilWithdrawalHypertension[4][6][15][3]
PD-200390DiscontinuedInsomnia[16]
BioChemical ClassVoltage-gated channel    
PathwayCalcium signaling pathway
MAPK signaling pathway
Type II diabetes mellitus
UniProt IDO43497
Q9P0X4
FunctionVoltage-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 and gene expression.    
SequenceMDEEEDGAGAEESGQPRSFMRLNDLSGAGGRPGPGSAEKDPGSADSEAEGLPYPALAPVV 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 ValidationClick to Find Target Validation Information.    
InhibitorKKHT-10318[17]
KKHT-10608[17]
KKHT-10609[17]
KKHT-10613[17]
KKHT-10618[17]
KKHT-11018[17]
KKHT-20718[17]
KKHT-20818[17]
KKHT-20918[17]
KYS-05001[18]
KYS-05040[19]
KYS-05041[20]
KYS-05041[21]
KYS-05042[21]
KYS-05042[22]
KYS-05050[23]
KYS-05055[22]
KYS-05056[22]
KYS-05057[22]
KYS-05064[20]
KYS-05065[22]
KYS-05070[24]
KYS-05071[24]
KYS-05074[24]
KYS-05077[23]
KYS-05080[22]
KYS-05090[22]
cis-N,5-dibenzyl-6-oxomorpholine-3-carboxamide[25]
BlockerAlpha-methyl-alpha-phenylsuccinimide (MPS)[9]
Diphenylbutylpiperidines pimozide[26]
Ethosuximide[8][9][10]
Methsuximide[9]
Mibefradil[4][6][15][3]
Nickel chloride[7]
Paramethadione[11]
Penfluridol[26]
Trimethadione[11]
Verapamil[12][13]
ModulatorGabapentin enacarbil[14]
PD-200390[16]
Pregabalin[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The P/Q-type voltage-dependent calcium channel as pharmacological target in spinocerebellar ataxia type 6: gabapentin and pregabalin may be of therapeutic benefit. Med Hypotheses. 2007;68(1):131-6. Epub 2006 Aug 8. To Reference
Ref 2Management of chronic stable angina pectoris. Bol Asoc Med P R. 2008 Oct-Dec;100(4):39-47. To Reference
Ref 3Voltage-gated T-type Ca2+ channels and heart failure. Proc Assoc Am Physicians. 1999 Sep-Oct;111(5):429-37. To Reference
Ref 4T-type calcium channel blockade in the management of chronic ischemic heart disease. Cardiovasc Drugs Ther. 2000 Oct;14(5):459-61. To Reference
Ref 5A fluorescence-based high-throughput screening assay for the identification of T-type calcium channel blockers. Assay Drug Dev Technol. 2009 Jun;7(3):266-80. To Reference
Ref 6Comparison of the efficacy and safety of losartan (50-100 mg) with the T-type calcium channel blocker mibefradil (50-100 mg) in mild to moderate hypertension. Fundam Clin Pharmacol. 2000 Jan-Feb;14(1):31-41. To Reference
Ref 7T-type calcium channels facilitate insulin secretion by enhancing general excitability in the insulin-secreting beta-cell line, INS-1. Endocrinology. 1997 Sep;138(9):3735-40. To Reference
Ref 8Maladaptive homeostatic plasticity in a rodent model of central pain syndrome: thalamic hyperexcitability after spinothalamic tract lesions. J Neurosci. 2008 Nov 12;28(46):11959-69. To Reference
Ref 9Block of cloned human T-type calcium channels by succinimide antiepileptic drugs. Mol Pharmacol. 2001 Nov;60(5):1121-32. To Reference
Ref 10Effects of ethosuximide, a T-type Ca(2+) channel blocker, on dorsal horn neuronal responses in rats. Eur J Pharmacol. 2001 Mar;415(2-3):141-9. To Reference
Ref 11Prophylactic and therapeutic functions of T-type calcium blockers against noise-induced hearing loss. Hear Res. 2007 Apr;226(1-2):52-60. Epub 2006 Dec 31. To Reference
Ref 12Mechanism of tissue-selective drug action in the cardiovascular system. Mol Interv. 2005 Apr;5(2):84-93. To Reference
Ref 13Combination therapy and target organ protection in hypertension and diabetes mellitus. Am J Hypertens. 1997 Sep;10(9 Pt 2):198S-201S. To Reference
Ref 14GSK. Product Development Pipeline. February 2009. To Reference
Ref 15Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. To Reference
Ref 16Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 17Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. To Reference
Ref 18Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. Epub 2007 Sep 1.Discovery of potent T-type calcium channel blocker. To Reference
Ref 19Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84.3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers. To Reference
Ref 20Bioorg Med Chem. 2007 Jan 15;15(2):1091-105. Epub 2006 Oct 30.3D pharmacophore based virtual screening of T-type calcium channel blockers. To Reference
Ref 21Bioorg Med Chem Lett. 2005 Jan 17;15(2):283-6.Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers. To Reference
Ref 22Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. Epub 2008 Jun 14.T-type Ca2+ channel blockers suppress the growth of human cancer cells. To Reference
Ref 23Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5. Epub 2006 Oct 12.Synthesis and biological evaluation of novel T-type calcium channel blockers. To Reference
Ref 24Bioorg Med Chem Lett. 2006 Oct 1;16(19):5014-7. Epub 2006 Jul 28.Growth inhibition of human cancer cells in vitro by T-type calcium channel blockers. To Reference
Ref 25Bioorg Med Chem Lett. 2006 Oct 1;16(19):5244-8. Epub 2006 Jul 28.Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers. To Reference
Ref 26Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. To Reference



 

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