Target Information

Target General Infomation
Target ID
T64795
Former ID
TTDS00161
Target Name
Voltage-dependent T-type calcium channel alpha-1G subunit
Gene Name
CACNA1G
Synonyms
Cav; Cav3.1c; NBR13; Voltage-dependent T-type calcium channel; Voltage-gated calcium channel alpha subunit Cav3.1; CACNA1G
Target Type
Successful
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Epilepsy [ICD10: G40]
Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Epileptic conditions; Pancreatic cancer [ICD9:345, 140-199, 140-229, 157, 210-229; ICD10: G40, C25]
Hypertension; Angina [ICD9: 401, 413; ICD10: I10-I16, I20]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Paramethadione syndrome; Seizures [ICD9:741, 744, 745, 746, 751, 753, 345.9, 780.3; ICD10: Q05, Q17, Q20-Q28, Q60, Q79, G40, P90, R56]
Schizophrenia [ICD9: 295; ICD10: F20]
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 and gene expression.
BioChemical Class
Calcium channel
Target Validation
T64795
UniProt ID
O43497
Sequence
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
Drugs and Mode of Action
Drug(s) Ethosuximide Drug Info Approved Epilepsy [538174], [542193]
Methsuximide Drug Info Approved Epileptic seizures [538431], [542243]
Paramethadione Drug Info Approved Paramethadione syndrome; Seizures [538397], [542280], [551871]
Penfluridol Drug Info Approved Schizophrenia [551871]
Trimethadione Drug Info Approved Epileptic conditions; Pancreatic cancer [538387], [542339], [551871]
Verapamil Drug Info Approved Hypertension; Angina [536619], [539535]
PD-200390 Drug Info Phase 2 Insomnia [530573]
Blocker (channel blocker) (-)-(R)-efonidipine Drug Info [527288]
ML218 Drug Info [531818]
Blocker Alpha-methyl-alpha-phenylsuccinimide (MPS) Drug Info [535283]
Diphenylbutylpiperidines pimozide Drug Info [535338]
Ethosuximide Drug Info [535142], [535283], [536932]
Methsuximide Drug Info [535283]
Nickel chloride Drug Info [538044]
Paramethadione Drug Info [536353]
Penfluridol Drug Info [535338]
Trimethadione Drug Info [536353]
Verapamil Drug Info [536067], [538057]
Inhibitor Cis-N,5-dibenzyl-6-oxomorpholine-3-carboxamide Drug Info [528344]
KKHT-10318 Drug Info [528476]
KKHT-10608 Drug Info [528476]
KKHT-10609 Drug Info [528476]
KKHT-10613 Drug Info [528476]
KKHT-10618 Drug Info [528476]
KKHT-11018 Drug Info [528476]
KKHT-20718 Drug Info [528476]
KKHT-20818 Drug Info [528476]
KKHT-20918 Drug Info [528476]
KYS-05001 Drug Info [529044]
KYS-05040 Drug Info [527099]
KYS-05041 Drug Info [528504]
KYS-05042 Drug Info [529566]
KYS-05050 Drug Info [528495]
KYS-05055 Drug Info [529566]
KYS-05056 Drug Info [529566]
KYS-05057 Drug Info [529566]
KYS-05064 Drug Info [528504]
KYS-05065 Drug Info [529566]
KYS-05070 Drug Info [528345]
KYS-05071 Drug Info [528345]
KYS-05074 Drug Info [528345]
KYS-05077 Drug Info [528495]
KYS-05080 Drug Info [529566]
KYS-05090 Drug Info [529566]
Modulator PD-200390 Drug Info [549974]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway MAPK signaling pathway
Calcium signaling pathway
Circadian entrainment
Type II diabetes mellitus
PANTHER Pathway Endogenous cannabinoid signaling
GABA-B receptor II signaling
Nicotine pharmacodynamics pathway
Pathway Interaction Database Regulation of nuclear beta catenin signaling and target gene transcription
PathWhiz Pathway Muscle/Heart Contraction
Reactome NCAM1 interactions
WikiPathways NCAM signaling for neurite out-growth
Nicotine Activity on Chromaffin Cells
References
Ref 530573Bioorg Med Chem Lett. 2010 Jan 15;20(2):461-4. Epub 2009 Nov 27.Synthesis and in vivo evaluation of bicyclic gababutins.
Ref 536619Partial restoration of mutant enzyme homeostasis in three distinct lysosomal storage disease cell lines by altering calcium homeostasis. PLoS Biol. 2008 Feb;6(2):e26.
Ref 538174FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040253.
Ref 538387FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 005856.
Ref 538397FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006800.
Ref 538431FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010596.
Ref 539535(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2406).
Ref 542193(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7182).
Ref 542243(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7228).
Ref 542280(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7261).
Ref 542339(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7316).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 527099Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84.3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.
Ref 527288Identification of R(-)-isomer of efonidipine as a selective blocker of T-type Ca2+ channels. Br J Pharmacol. 2004 Dec;143(8):1050-7. Epub 2004 Nov 15.
Ref 528344Bioorg 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.
Ref 528345Bioorg 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.
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 528495Bioorg 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.
Ref 528504Bioorg Med Chem. 2007 Jan 15;15(2):1091-105. Epub 2006 Oct 30.3D pharmacophore based virtual screening of T-type calcium channel blockers.
Ref 529044Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. Epub 2007 Sep 1.Discovery of potent T-type calcium channel blocker.
Ref 529566Bioorg 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.
Ref 531818The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. ACS Chem Neurosci. 2011 Dec 21;2(12):730-742.
Ref 535142Effects 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.
Ref 535283Block of cloned human T-type calcium channels by succinimide antiepileptic drugs. Mol Pharmacol. 2001 Nov;60(5):1121-32.
Ref 535338Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403.
Ref 536067Mechanism of tissue-selective drug action in the cardiovascular system. Mol Interv. 2005 Apr;5(2):84-93.
Ref 536353Prophylactic 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.
Ref 536932Maladaptive 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.
Ref 538044T-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.
Ref 538057Combination therapy and target organ protection in hypertension and diabetes mellitus. Am J Hypertens. 1997 Sep;10(9 Pt 2):198S-201S.
Ref 549974Pfizer. Product Development Pipeline. March 31 2009.

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