Therapeutic Targets Database
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TTD Target ID: TTDS00415

Target Information
NameVoltage-dependent calcium channel subunit alpha-2/delta-1    
Type of targetSuccessful target    
SynonymsCACNA2D1    
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    
DiseaseAnalgesics    [1]
Chronic stable angina    [1]
Heart transplant    [2]
Hypertension    [3]
Vasospastic angina    [1]
Drug(s)AmlodipineApprovedHypertension and angina[4][5]
DiltiazemApprovedHypertension[6]
IsradipineApprovedHypertension[7]
LercanidipineApprovedHypertension[8]
NifedipineApprovedAngina pectoris[9]
NitrendipineApprovedHypertension[10]
BioChemical ClassVoltage-gated channel    
UniProt IDP54289
Q06432
SequenceMAAGCLLALTLTLFQSLLIGPSSEEPFPSAVTIKSWVDKMQEDLVTLAKTASGVNQLVDI YEKYQDLYTVEPNNARQLVEIAARDIEKLLSNRSKALVRLALEAEKVQAAHQWREDFASN EVVYYNAKDDLDPEKNDSEPGSQRIKPVFIEDANFGRQISYQHAAVHIPTDIYEGSTIVL NELNWTSALDEVFKKNREEDPSLLWQVFGSATGLARYYPASPWVDNSRTPNKIDLYDVRR RPWYIQGAASPKDMLILVDVSGSVSGLTLKLIRTSVSEMLETLSDDDFVNVASFNSNAQD VSCFQHLVQANVRNKKVLKDAVNNITAKGITDYKKGFSFAFEQLLNYNVSRANCNKIIML FTDGGEERAQEIFNKYNKDKKVRVFTFSVGQHNYDRGPIQWMACENKGYYYEIPSIGAIR INTQEYLDVLGRPMVLAGDKAKQVQWTNVYLDALELGLVITGTLPVFNITGQFENKTNLK NQLILGVMGVDVSLEDIKRLTPRFTLCPNGYYFAIDPNGYVLLHPNLQPKNPKSQEPVTL DFLDAELENDIKVEIRNKMIDGESGEKTFRTLVKSQDERYIDKGNRTYTWTPVNGTDYSL ALVLPTYSFYYIKAKLEETITQARSKKGKMKDSETLKPDNFEESGYTFIAPRDYCNDLKI SDNNTEFLLNFNEFIDRKTPNNPSCNADLINRVLLDAGFTNELVQNYWSKQKNIKGVKAR FVVTDGGITRVYPKEAGENWQENPETYEDSFYKRSLDNDNYVFTAPYFNKSGPGAYESGI MVSKAVEIYIQGKLLKPAVVGIKIDVNSWIENFTKTSIRDPCAGPVCDCKRNSDVMDCVI LDDGGFLLMANHDDYTNQIGRFFGEIDPSLMRHLVNISVYAFNKSYDYQSVCEPGAAPKQ GAGHRSAYVPSVADILQIGWWATAAAWSILQQFLLSLTFPRLLEAVEMEDDDFTASLSKQ SCITEQTQYFFDNDSKSFSGVLDCGNCSRIFHGEKLMNTNLIFIMVESKGTCPCDTRLLI QAEQTSDGPNPCDMVKQPRYRKGPDVCFDNNVLEDYTDCGGVSGLNPSLWYIIGIQFLLL WLVSGSTHRLL
Target ValidationClick to Find Target Validation Information.    
Inhibitor (R)-3-[11]
(S)-2-amino-2-cyclohexylacetic acid[12]
(S)-2-amino-2-o-tolylacetic acid[12]
(S)-2-amino-2-p-tolylacetic acid[12]
(S)-2-amino-2-phenylpropanoic acid[12]
(S)-2-amino-3-[12]
(S)-2-amino-3-cyclohexylpropanoic acid[12]
(S)-2-amino-4-[12]
(S)-3-[11]
(S)-phenylglycine[12]
1-benzhydryl-4- (3,3-diphenylpropyl)piperazine[13]
1-benzhydryl-4- (4,4-diphenylbutyl)piperazine[13]
2- (1-[14]
2- (1-[14]
2-amino-2- (2,3-difluorophenyl)acetic acid[12]
2-amino-2- (2,4-difluorophenyl)acetic acid[12]
2-amino-2- (2-fluorophenyl)acetic acid[12]
2-amino-2- (3-bromophenyl)acetic acid[12]
2-amino-2- (3-chloro-4-fluorophenyl)acetic acid[12]
2-amino-2- (3-chlorophenyl)acetic acid[12]
2-amino-2- (thiophen-2-yl)acetic acid[12]
2-amino-4- (2-methyl-benzylsulfanyl)-butyric acid[12]
3- (aminomethyl)-4-[11]
3- (aminomethyl)-4-[11]
3- (aminomethyl)-4-[11]
3- (aminomethyl)-4-[11]
3-Aminomethyl-5-methyl-hexanoic acid[15]
4- (2,3-dichlorobenzylthio)-2-aminobutanoic acid[12]
4- (2,5-dichlorobenzylthio)-2-aminobutanoic acid[12]
4- (2-bromobenzylthio)-2-aminobutanoic acid[12]
4- (2-cyanobenzylthio)-2-aminobutanoic acid[12]
4- (2-methoxybenzylthio)-2-aminobutanoic acid[12]
4- (2-nitrobenzylthio)-2-aminobutanoic acid[12]
4- (3,4-dichlorobenzylthio)-2-aminobutanoic acid[12]
4- (3,4-dimethylbenzylthio)-2-aminobutanoic acid[12]
4- (3,5-dichlorobenzylthio)-2-aminobutanoic acid[12]
4- (3,5-dimethylbenzylthio)-2-aminobutanoic acid[12]
4- (3-bromobenzylthio)-2-aminobutanoic acid[12]
4- (3-chlorobenzylthio)-2-aminobutanoic acid[12]
4- (3-cyanobenzylthio)-2-aminobutanoic acid[12]
4- (3-fluorobenzylthio)-2-aminobutanoic acid[12]
4- (3-methoxybenzylthio)-2-aminobutanoic acid[12]
4- (3-nitrobenzylthio)-2-aminobutanoic acid[12]
4- (4-bromobenzylthio)-2-aminobutanoic acid[12]
4- (4-chlorobenzylthio)-2-aminobutanoic acid[12]
4- (4-tert-butylbenzylthio)-2-aminobutanoic acid[12]
ETHIONINE[12]
Gababutin[14]
LOMERIZINE[13]
N'-Acridin-9-yl-N,N-diethyl-butane-1,4-diamine[16]
N,4-dibenzhydrylpiperazine-1-carboxamide[13]
NP-118809[13]
PD-144550[15]
PHENYLALANINE[12]
rac-2-amino-4-phenylbutanoic acid[12]
rac-2-amino-5-cyclohexylpentanoic acid[12]
trans-dimethyl gababutin[17]
BlockerAmlodipine[4][5]
Diltiazem[6]
Isradipine[7]
Lercanidipine[8]
Nifedipine[9]
Nitrendipine[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Correlates of coronary angiography in patients with stable angina and geographical differences in its utilisation: The ACTION experience. Int J Cardiol. 2008 Oct 7. [Epub ahead of print] To Reference
Ref 2Safety and efficacy of ibutilide in heart transplant recipients. J Heart Lung Transplant. 2009 May;28(5):505-7. To Reference
Ref 3Compiled report on clinical efficacy and safety of nifedipine retard 10/20/nifedipine CD 30, as a first-line/add-on therapy in patients of hypertension: ENHANS trial. J Indian Med Assoc. 2009 Feb;107(2):114-6. To Reference
Ref 4A 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. To Reference
Ref 5Benidipine, 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. To Reference
Ref 6Egr-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. To Reference
Ref 7Calcium channel blockers: pharmacology and place in therapy of pediatric hypertension. Pediatr Nephrol. 2000 Dec;15(3-4):302-16. To Reference
Ref 8Treatment of essential hypertension with calcium channel blockers: what is the place of lercanidipine? Expert Opin Drug Metab Toxicol. 2009 Aug;5(8):981-7. To Reference
Ref 9Calcium-dependent and endothelium-dependent mechanisms for a constrictor response of the saphenous vein. Bull Exp Biol Med. 2009 Feb;147(2):170-2. To Reference
Ref 10Sulfobutyl ether-alkyl ether mixed cyclodextrin derivatives with enhanced inclusion ability. J Pharm Sci. 2009 Apr 30. [Epub ahead of print] To Reference
Ref 11Bioorg Med Chem Lett. 2006 May 1;16(9):2329-32. Epub 2005 Aug 15.Heteroaromatic side-chain analogs of pregabalin. To Reference
Ref 12Bioorg 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. To Reference
Ref 13Bioorg 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. To Reference
Ref 14Bioorg Med Chem Lett. 2010 Jan 1;20(1):362-5. Epub 2009 Oct 25.Synthesis and in vivo evaluation of 3-substituted gababutins. To Reference
Ref 15Bioorg. Med. Chem. Lett. 4(6):823-826 (1994) To Reference
Ref 16Bioorg 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. To Reference
Ref 17Bioorg Med Chem Lett. 2010 Jan 15;20(2):461-4. Epub 2009 Nov 27.Synthesis and in vivo evaluation of bicyclic gababutins. To Reference



 

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