Target Information

Target General Infomation
Target ID
T84316
Former ID
TTDS00415
Target Name
Voltage-dependent calcium channel subunit alpha-2/delta-1
Gene Name
CACNA2D1
Synonyms
CACNL2A; CCHL2A; MHS3; Voltage-dependent calcium channel subunit alpha-2-1; Voltage-dependent calcium channel subunit delta-1; Voltage-gated calcium channel subunit alpha-2/delta-1; CACNA2D1
Target Type
Successful
Disease Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Cardiovascular disorder [ICD10: I00-I99]
Generalized anxiety disorder [ICD9: 300, 300.02, 311; ICD10: F32, F40-F42, F41.1]
Hypertension; Angina [ICD9: 401, 413; ICD10: I10-I16, I20]
Hypertension [ICD9: 401; ICD10: I10-I16]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Function
The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel. Plays an important role in excitation-contraction coupling (By similarity).
BioChemical Class
Ca(2+) channel auxiliary subunit 2 1-4
Target Validation
T84316
UniProt ID
P54289
Sequence
MAAGCLLALTLTLFQSLLIGPSSEEPFPSAVTIKSWVDKMQEDLVTLAKTASGVNQLVDI
YEKYQDLYTVEPNNARQLVEIAARDIEKLLSNRSKALVRLALEAEKVQAAHQWREDFASN
EVVYYNAKDDLDPEKNDSEPGSQRIKPVFIEDANFGRQISYQHAAVHIPTDIYEGSTIVL
NELNWTSALDEVFKKNREEDPSLLWQVFGSATGLARYYPASPWVDNSRTPNKIDLYDVRR
RPWYIQGAASPKDMLILVDVSGSVSGLTLKLIRTSVSEMLETLSDDDFVNVASFNSNAQD
VSCFQHLVQANVRNKKVLKDAVNNITAKGITDYKKGFSFAFEQLLNYNVSRANCNKIIML
FTDGGEERAQEIFNKYNKDKKVRVFTFSVGQHNYDRGPIQWMACENKGYYYEIPSIGAIR
INTQEYLDVLGRPMVLAGDKAKQVQWTNVYLDALELGLVITGTLPVFNITGQFENKTNLK
NQLILGVMGVDVSLEDIKRLTPRFTLCPNGYYFAIDPNGYVLLHPNLQPKPIGVGIPTIN
LRKRRPNIQNPKSQEPVTLDFLDAELENDIKVEIRNKMIDGESGEKTFRTLVKSQDERYI
DKGNRTYTWTPVNGTDYSLALVLPTYSFYYIKAKLEETITQARYSETLKPDNFEESGYTF
IAPRDYCNDLKISDNNTEFLLNFNEFIDRKTPNNPSCNADLINRVLLDAGFTNELVQNYW
SKQKNIKGVKARFVVTDGGITRVYPKEAGENWQENPETYEDSFYKRSLDNDNYVFTAPYF
NKSGPGAYESGIMVSKAVEIYIQGKLLKPAVVGIKIDVNSWIENFTKTSIRDPCAGPVCD
CKRNSDVMDCVILDDGGFLLMANHDDYTNQIGRFFGEIDPSLMRHLVNISVYAFNKSYDY
QSVCEPGAAPKQGAGHRSAYVPSVADILQIGWWATAAAWSILQQFLLSLTFPRLLEAVEM
EDDDFTASLSKQSCITEQTQYFFDNDSKSFSGVLDCGNCSRIFHGEKLMNTNLIFIMVES
KGTCPCDTRLLIQAEQTSDGPNPCDMVKQPRYRKGPDVCFDNNVLEDYTDCGGVSGLNPS
LWYIIGIQFLLLWLVSGSTHRLL
Drugs and Mode of Action
Drug(s) Amlodipine Drug Info Approved Hypertension; Angina [537071], [542011]
Diltiazem Drug Info Approved Hypertension [536619], [539449]
Lercanidipine Drug Info Approved Hypertension [536336]
Nitrendipine Drug Info Approved Hypertension [539478], [550669]
Pregabalin Drug Info Approved Chronic obstructive pulmonary disease [528162], [540884]
Imagabalin Drug Info Phase 3 Generalized anxiety disorder [531511]
Mirogabalin Drug Info Phase 3 Cardiovascular disorder [543055], [549169]
Lercanidipine Drug Info Phase 2 Hypertension [548460]
Inhibitor (R)-3-(aminomethyl)-4-(furan-2-yl)butanoic acid Drug Info [527684]
(S)-2-amino-2-cyclohexylacetic acid Drug Info [527946]
(S)-2-amino-2-o-tolylacetic acid Drug Info [527946]
(S)-2-amino-2-p-tolylacetic acid Drug Info [527946]
(S)-2-amino-2-phenylpropanoic acid Drug Info [527946]
(S)-2-amino-3-(benzylthio)propanoic acid Drug Info [527946]
(S)-2-amino-3-cyclohexylpropanoic acid Drug Info [527946]
(S)-2-amino-4-(benzylthio)butanoic acid Drug Info [527946]
(S)-3-(aminomethyl)-4-(furan-2-yl)butanoic acid Drug Info [527684]
(S)-phenylglycine Drug Info [527946]
1-benzhydryl-4-(3,3-diphenylpropyl)piperazine Drug Info [530438]
1-benzhydryl-4-(4,4-diphenylbutyl)piperazine Drug Info [530438]
2-(1-(aminomethyl)-3-butylcyclopentyl)acetic acid Drug Info [530504]
2-(1-(aminomethyl)-3-ethylcyclopentyl)acetic acid Drug Info [530504]
2-amino-2-(2,3-difluorophenyl)acetic acid Drug Info [527946]
2-amino-2-(2,4-difluorophenyl)acetic acid Drug Info [527946]
2-amino-2-(2-fluorophenyl)acetic acid Drug Info [527946]
2-amino-2-(3-bromophenyl)acetic acid Drug Info [527946]
2-amino-2-(3-chloro-4-fluorophenyl)acetic acid Drug Info [527946]
2-amino-2-(3-chlorophenyl)acetic acid Drug Info [527946]
2-amino-2-(thiophen-2-yl)acetic acid Drug Info [527946]
2-amino-4-(2-methyl-benzylsulfanyl)-butyric acid Drug Info [527946]
3-(aminomethyl)-4-(furan-2-yl)butanoic acid Drug Info [527684]
3-(aminomethyl)-4-(furan-3-yl)butanoic acid Drug Info [527684]
3-(aminomethyl)-4-(thiophen-2-yl)butanoic acid Drug Info [527684]
3-(aminomethyl)-4-(thiophen-3-yl)butanoic acid Drug Info [527684]
3-Aminomethyl-5-methyl-hexanoic acid Drug Info [551273]
4-(2,3-dichlorobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(2,5-dichlorobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(2-bromobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(2-cyanobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(2-methoxybenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(2-nitrobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3,4-dichlorobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3,4-dimethylbenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3,5-dichlorobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3,5-dimethylbenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3-bromobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3-chlorobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3-cyanobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3-fluorobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3-methoxybenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(3-nitrobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(4-bromobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(4-chlorobenzylthio)-2-aminobutanoic acid Drug Info [527946]
4-(4-tert-butylbenzylthio)-2-aminobutanoic acid Drug Info [527946]
ETHIONINE Drug Info [527946]
Gababutin Drug Info [530504]
N'-Acridin-9-yl-N,N-diethyl-butane-1,4-diamine Drug Info [527016]
N,4-dibenzhydrylpiperazine-1-carboxamide Drug Info [530438]
NP-118809 Drug Info [530438]
PD-144550 Drug Info [551273]
Rac-2-amino-4-phenylbutanoic acid Drug Info [527946]
Rac-2-amino-5-cyclohexylpentanoic acid Drug Info [527946]
Trans-dimethyl gababutin Drug Info [530573]
Blocker Amlodipine Drug Info [536553], [536597]
Diltiazem Drug Info [537595]
Lercanidipine Drug Info [537620]
Nitrendipine Drug Info [537276]
Agonist Imagabalin Drug Info [528162], [531511]
Modulator Mirogabalin Drug Info [528162], [532966]
Pregabalin Drug Info [528162]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway MAPK signaling pathway
Cardiac muscle contraction
Adrenergic signaling in cardiomyocytes
Oxytocin signaling pathway
Hypertrophic cardiomyopathy (HCM)
Arrhythmogenic right ventricular cardiomyopathy (ARVC)
Dilated cardiomyopathy
PANTHER Pathway Muscarinic acetylcholine receptor 2 and 4 signaling pathway
WikiPathways Arrhythmogenic Right Ventricular Cardiomyopathy
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
References
Ref 528162Pregabalin reduces the release of synaptic vesicles from cultured hippocampal neurons. Mol Pharmacol. 2006 Aug;70(2):467-76. Epub 2006 Apr 26.
Ref 531511Methodology for rapid measures of glutamate release in rat brain slices using ceramic-based microelectrode arrays: basic characterization and drug pharmacology. Brain Res. 2011 Jul 15;1401:1-9.
Ref 536336Fixed-dose combination lercanidipine/enalapril. Drugs. 2007;67(1):95-106; discussion 107-8.
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 537071Antihypertensive efficacy of olmesartan medoxomil or valsartan in combination with amlodipine: a review of factorial-design studies. Curr Med Res Opin. 2009 Jan;25(1):177-85.
Ref 539449(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: 2298).
Ref 539478(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: 2334).
Ref 540884(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: 5484).
Ref 542011(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: 6981).
Ref 543055(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: 8303).
Ref 548460Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025674)
Ref 549169Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033181)
Ref 550669Drug information of Nitrendipine, 2008. eduDrugs.
Ref 527016Bioorg Med Chem Lett. 2004 Apr 19;14(8):1913-6.N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.
Ref 527684Bioorg Med Chem Lett. 2006 May 1;16(9):2329-32. Epub 2005 Aug 15.Heteroaromatic side-chain analogs of pregabalin.
Ref 527946Bioorg Med Chem Lett. 2006 Mar 1;16(5):1138-41. Epub 2005 Dec 27.Structure-activity relationships of alpha-amino acid ligands for the alpha2delta subunit of voltage-gated calcium channels.
Ref 528162Pregabalin reduces the release of synaptic vesicles from cultured hippocampal neurons. Mol Pharmacol. 2006 Aug;70(2):467-76. Epub 2006 Apr 26.
Ref 530438Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. Epub 2009 Sep 11.Scaffold-based design and synthesis of potent N-type calcium channel blockers.
Ref 530504Bioorg Med Chem Lett. 2010 Jan 1;20(1):362-5. Epub 2009 Oct 25.Synthesis and in vivo evaluation of 3-substituted gababutins.
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 531511Methodology for rapid measures of glutamate release in rat brain slices using ceramic-based microelectrode arrays: basic characterization and drug pharmacology. Brain Res. 2011 Jul 15;1401:1-9.
Ref 532966Efficacy and safety of mirogabalin (DS-5565) for the treatment of diabetic peripheral neuropathic pain: a randomized, double-blind, placebo- and active comparator-controlled, adaptive proof-of-concept phase 2 study. Diabetes Care. 2014 Dec;37(12):3253-61.
Ref 536553Benidipine, an anti-hypertensive drug, inhibits reactive oxygen species production in polymorphonuclear leukocytes and oxidative stress in salt-loaded stroke-prone spontaneously hypertensive rats. Eur J Pharmacol. 2008 Feb 2;580(1-2):201-13. Epub 2007 Nov 1.
Ref 536597A first drug combination for the treatment of arterial hypertension with a calcium channel antagonist (amlodipine besylate) and an angiotensin receptor blocker (valsartan): Exforge. Rev Med Liege. 2007 Nov;62(11):688-94.
Ref 537276Sulfobutyl ether-alkyl ether mixed cyclodextrin derivatives with enhanced inclusion ability. J Pharm Sci. 2009 Apr 30.
Ref 537595Egr-1, the potential target of calcium channel blockers in cardioprotection with ischemia/reperfusion injury in rats. Cell Physiol Biochem. 2009;24(1-2):17-24. Epub 2009 Jul 1.
Ref 537620Treatment of essential hypertension with calcium channel blockers: what is the place of lercanidipine? Expert Opin Drug Metab Toxicol. 2009 Aug;5(8):981-7.
Ref 551273Enantioselective synthesis of PD144723: a potent stereospecific anticonvulsant, Bioorg. Med. Chem. Lett. 4(6):823-826 (1994).

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