Target Information
| Target General Information | Top | |||||
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| Target ID |
T84316
(Former ID: TTDS00415)
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| Target Name |
Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1)
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| Synonyms |
Voltage-gated calcium channel subunit alpha-2/delta-1; Voltage-dependent calcium channel subunit delta-1; Voltage-dependent calcium channel subunit alpha-2-1; MHS3; CCHL2A; CACNL2A; CACNA2D1
Click to Show/Hide
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| Gene Name |
CACNA2D1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Chronic obstructive pulmonary disease [ICD-11: CA22] | |||||
| 2 | Hypertension [ICD-11: BA00-BA04] | |||||
| 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.
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| BioChemical Class |
Voltage-gated ion channel
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| UniProt ID | ||||||
| Sequence |
MAAGCLLALTLTLFQSLLIGPSSEEPFPSAVTIKSWVDKMQEDLVTLAKTASGVNQLVDI
YEKYQDLYTVEPNNARQLVEIAARDIEKLLSNRSKALVRLALEAEKVQAAHQWREDFASN EVVYYNAKDDLDPEKNDSEPGSQRIKPVFIEDANFGRQISYQHAAVHIPTDIYEGSTIVL NELNWTSALDEVFKKNREEDPSLLWQVFGSATGLARYYPASPWVDNSRTPNKIDLYDVRR RPWYIQGAASPKDMLILVDVSGSVSGLTLKLIRTSVSEMLETLSDDDFVNVASFNSNAQD VSCFQHLVQANVRNKKVLKDAVNNITAKGITDYKKGFSFAFEQLLNYNVSRANCNKIIML FTDGGEERAQEIFNKYNKDKKVRVFTFSVGQHNYDRGPIQWMACENKGYYYEIPSIGAIR INTQEYLDVLGRPMVLAGDKAKQVQWTNVYLDALELGLVITGTLPVFNITGQFENKTNLK NQLILGVMGVDVSLEDIKRLTPRFTLCPNGYYFAIDPNGYVLLHPNLQPKPIGVGIPTIN LRKRRPNIQNPKSQEPVTLDFLDAELENDIKVEIRNKMIDGESGEKTFRTLVKSQDERYI DKGNRTYTWTPVNGTDYSLALVLPTYSFYYIKAKLEETITQARYSETLKPDNFEESGYTF IAPRDYCNDLKISDNNTEFLLNFNEFIDRKTPNNPSCNADLINRVLLDAGFTNELVQNYW SKQKNIKGVKARFVVTDGGITRVYPKEAGENWQENPETYEDSFYKRSLDNDNYVFTAPYF NKSGPGAYESGIMVSKAVEIYIQGKLLKPAVVGIKIDVNSWIENFTKTSIRDPCAGPVCD CKRNSDVMDCVILDDGGFLLMANHDDYTNQIGRFFGEIDPSLMRHLVNISVYAFNKSYDY QSVCEPGAAPKQGAGHRSAYVPSVADILQIGWWATAAAWSILQQFLLSLTFPRLLEAVEM EDDDFTASLSKQSCITEQTQYFFDNDSKSFSGVLDCGNCSRIFHGEKLMNTNLIFIMVES KGTCPCDTRLLIQAEQTSDGPNPCDMVKQPRYRKGPDVCFDNNVLEDYTDCGGVSGLNPS LWYIIGIQFLLLWLVSGSTHRLL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T50UMR | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 6 Approved Drugs | + | ||||
| 1 | Amlodipine | Drug Info | Approved | Hypertension | [2], [3] | |
| 2 | Diltiazem | Drug Info | Approved | Hypertension | [4], [5] | |
| 3 | Lercanidipine | Drug Info | Approved | Hypertension | [6] | |
| 4 | Nitrendipine | Drug Info | Approved | Hypertension | [7], [8] | |
| 5 | Pregabalin | Drug Info | Approved | Chronic obstructive pulmonary disease | [9], [10] | |
| 6 | Mirogabalin | Drug Info | Registered | Peripheral neuropathy | [11] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | Imagabalin | Drug Info | Phase 3 | Generalized anxiety disorder | [12] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | NP-118809 | Drug Info | Discontinued in Phase 2 | Pain | [13] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Blocker | [+] 4 Blocker drugs | + | ||||
| 1 | Amlodipine | Drug Info | [1], [14] | |||
| 2 | Diltiazem | Drug Info | [15] | |||
| 3 | Lercanidipine | Drug Info | [16] | |||
| 4 | Nitrendipine | Drug Info | [17] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Pregabalin | Drug Info | [10] | |||
| 2 | Mirogabalin | Drug Info | [10], [18] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | Imagabalin | Drug Info | [10], [12] | |||
| Inhibitor | [+] 55 Inhibitor drugs | + | ||||
| 1 | NP-118809 | Drug Info | [19] | |||
| 2 | (R)-3-(aminomethyl)-4-(furan-2-yl)butanoic acid | Drug Info | [20] | |||
| 3 | (S)-2-amino-2-cyclohexylacetic acid | Drug Info | [21] | |||
| 4 | (S)-2-amino-2-o-tolylacetic acid | Drug Info | [21] | |||
| 5 | (S)-2-amino-2-p-tolylacetic acid | Drug Info | [21] | |||
| 6 | (S)-2-amino-2-phenylpropanoic acid | Drug Info | [21] | |||
| 7 | (S)-2-amino-3-(benzylthio)propanoic acid | Drug Info | [21] | |||
| 8 | (S)-2-amino-3-cyclohexylpropanoic acid | Drug Info | [21] | |||
| 9 | (S)-2-amino-4-(benzylthio)butanoic acid | Drug Info | [21] | |||
| 10 | (S)-3-(aminomethyl)-4-(furan-2-yl)butanoic acid | Drug Info | [20] | |||
| 11 | (S)-phenylglycine | Drug Info | [21] | |||
| 12 | 1-benzhydryl-4-(3,3-diphenylpropyl)piperazine | Drug Info | [19] | |||
| 13 | 1-benzhydryl-4-(4,4-diphenylbutyl)piperazine | Drug Info | [19] | |||
| 14 | 2-(1-(aminomethyl)-3-butylcyclopentyl)acetic acid | Drug Info | [22] | |||
| 15 | 2-(1-(aminomethyl)-3-ethylcyclopentyl)acetic acid | Drug Info | [22] | |||
| 16 | 2-amino-2-(2,3-difluorophenyl)acetic acid | Drug Info | [21] | |||
| 17 | 2-amino-2-(2,4-difluorophenyl)acetic acid | Drug Info | [21] | |||
| 18 | 2-amino-2-(2-fluorophenyl)acetic acid | Drug Info | [21] | |||
| 19 | 2-amino-2-(3-bromophenyl)acetic acid | Drug Info | [21] | |||
| 20 | 2-amino-2-(3-chloro-4-fluorophenyl)acetic acid | Drug Info | [21] | |||
| 21 | 2-amino-2-(3-chlorophenyl)acetic acid | Drug Info | [21] | |||
| 22 | 2-amino-2-(thiophen-2-yl)acetic acid | Drug Info | [21] | |||
| 23 | 2-amino-4-(2-methyl-benzylsulfanyl)-butyric acid | Drug Info | [21] | |||
| 24 | 3-(aminomethyl)-4-(furan-2-yl)butanoic acid | Drug Info | [20] | |||
| 25 | 3-(aminomethyl)-4-(furan-3-yl)butanoic acid | Drug Info | [20] | |||
| 26 | 3-(aminomethyl)-4-(thiophen-2-yl)butanoic acid | Drug Info | [20] | |||
| 27 | 3-(aminomethyl)-4-(thiophen-3-yl)butanoic acid | Drug Info | [20] | |||
| 28 | 3-Aminomethyl-5-methyl-hexanoic acid | Drug Info | [23] | |||
| 29 | 4-(2,3-dichlorobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 30 | 4-(2,5-dichlorobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 31 | 4-(2-bromobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 32 | 4-(2-cyanobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 33 | 4-(2-methoxybenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 34 | 4-(2-nitrobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 35 | 4-(3,4-dichlorobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 36 | 4-(3,4-dimethylbenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 37 | 4-(3,5-dichlorobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 38 | 4-(3,5-dimethylbenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 39 | 4-(3-bromobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 40 | 4-(3-chlorobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 41 | 4-(3-cyanobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 42 | 4-(3-fluorobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 43 | 4-(3-methoxybenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 44 | 4-(3-nitrobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 45 | 4-(4-bromobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 46 | 4-(4-chlorobenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 47 | 4-(4-tert-butylbenzylthio)-2-aminobutanoic acid | Drug Info | [21] | |||
| 48 | ETHIONINE | Drug Info | [21] | |||
| 49 | Gababutin | Drug Info | [22] | |||
| 50 | N'-Acridin-9-yl-N,N-diethyl-butane-1,4-diamine | Drug Info | [24] | |||
| 51 | N,4-dibenzhydrylpiperazine-1-carboxamide | Drug Info | [19] | |||
| 52 | PD-144550 | Drug Info | [23] | |||
| 53 | Rac-2-amino-4-phenylbutanoic acid | Drug Info | [21] | |||
| 54 | Rac-2-amino-5-cyclohexylpentanoic acid | Drug Info | [21] | |||
| 55 | Trans-dimethyl gababutin | Drug Info | [25] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | Human N-type voltage-gated calcium channel Cav2.2 in the presence of ziconotide at 3.0 Angstrom resolution | PDB:7MIX | ||||
| Method | Electron microscopy | Resolution | 3.00 Å | Mutation | No | [26] |
| PDB Sequence |
FPSAVTIKSW
36 VDKMQEDLVT46 LAKTASGVNQ56 LVDIYEKYQD66 LYTVEPNNAR76 QLVEIAARDI 86 EKLLSNRSKA96 LVRLALEAEK106 VQAAHQWRED116 FASNEVVYYN126 AKDDEPGSQR 144 IKPVFIEDAN154 FGRQISYQHA164 AVHIPTDIYE174 GSTIVLNELN184 WTSALDEVFK 194 KNREEDPSLL204 WQVFGSATGL214 ARYYPASPWV224 KIDLYDVRRR241 PWYIQGAASP 251 KDMLILVDVS261 GSVSGLTLKL271 IRTSVSEMLE281 TLSDDDFVNV291 ASFNSNAQDV 301 SCFQHLVQAN311 VRNKKVLKDA321 VNNITAKGIT331 DYKKGFSFAF341 EQLLNYNVSR 351 ANCNKIIMLF361 TDGGEERAQE371 IFNKYNKDKK381 VRVFTFSVGQ391 HNYDRGPIQW 401 MACENKGYYY411 EIPSIGAIRI421 NTQEYLDVLG431 RPMVLAGDKA441 KQVQWTNVYL 451 DALELGLVIT461 GTLPVFNITG471 QFENKTNLKN481 QLILGVMGVD491 VSLEDIKRLT 501 PRFTLCPNGY511 YFAIDPNGYV521 LLHPNLQPKP531 IGVGIPTINS553 QEPVTLDFLD 563 AELENDIKVE573 IRNKMIDGES583 GEKTFRTLVK593 SQDERYIDKG603 NRTYTWTPVN 613 GTDYSLALVL623 PTYSFYYIKA633 KLEETITQAR643 YSETLKPDNF653 EESGYTFIAP 663 RDYCNDLKIS673 DNNTEFLLNF683 NEFIDRKTPN693 NPSCNADLIN703 RVLLDAGFTN 713 ELVQNYWSKQ723 KNIKGVKARF733 VVTDGGITRV743 YPKEAGENWQ753 ENPETYEDSF 763 YKRSLDNDNY773 VFTAPYFNKS783 GPGAYESGIM793 VSKAVEIYIQ803 GKLLKPAVVG 813 IKIDVNSWIE823 NFTKRNSDVM848 DCVILDDGGF858 LLMANHDDYT868 NQIGRFFGEI 878 DPSLMRHLVN888 ISVYAFNKSY898 DYQSVCEPGA908 ASKQSCITEQ978 TQYFFDNDSK 988 SFSGVLDCGN998 CSRIFHGEKL1008 MNTNLIFIMV1018 ESKGTCPCDT1028 RLLIQAEQTS 1038 DGPNPCDMVK1048 QPRYRKGPDV1058 CFDNNVLEDY1068 TDCGGVSG
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| MAPK signaling pathway | hsa04010 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Cardiac muscle contraction | hsa04260 | Affiliated Target |
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| Class: Organismal Systems => Circulatory system | Pathway Hierarchy | ||
| Adrenergic signaling in cardiomyocytes | hsa04261 | Affiliated Target |
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| Class: Organismal Systems => Circulatory system | Pathway Hierarchy | ||
| Oxytocin signaling pathway | hsa04921 | Affiliated Target |
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| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Degree | 13 | Degree centrality | 1.40E-03 | Betweenness centrality | 1.23E-04 |
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| Closeness centrality | 1.69E-01 | Radiality | 1.27E+01 | Clustering coefficient | 3.21E-01 |
| Neighborhood connectivity | 7.31E+00 | Topological coefficient | 2.21E-01 | Eccentricity | 14 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 7 KEGG Pathways | + | ||||
| 1 | MAPK signaling pathway | |||||
| 2 | Cardiac muscle contraction | |||||
| 3 | Adrenergic signaling in cardiomyocytes | |||||
| 4 | Oxytocin signaling pathway | |||||
| 5 | Hypertrophic cardiomyopathy (HCM) | |||||
| 6 | Arrhythmogenic right ventricular cardiomyopathy (ARVC) | |||||
| 7 | Dilated cardiomyopathy | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Muscarinic acetylcholine receptor 2 and 4 signaling pathway | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | Arrhythmogenic Right Ventricular Cardiomyopathy | |||||
| 2 | miR-targeted genes in muscle cell - TarBase | |||||
| 3 | miR-targeted genes in lymphocytes - TarBase | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | A 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 2 | URL: 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 3 | Antihypertensive 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 4 | URL: 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 5 | Partial 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 6 | Fixed-dose combination lercanidipine/enalapril. Drugs. 2007;67(1):95-106; discussion 107-8. | |||||
| REF 7 | URL: 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 8 | Drug information of Nitrendipine, 2008. eduDrugs. | |||||
| REF 9 | URL: 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 10 | Pregabalin reduces the release of synaptic vesicles from cultured hippocampal neurons. Mol Pharmacol. 2006 Aug;70(2):467-76. | |||||
| REF 11 | Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. | |||||
| REF 12 | Methodology 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 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016715) | |||||
| REF 14 | Benidipine, an anti-hypertensive drug, inhibits reactive oxygen species production in polymorphonuclear leukocytes and oxidative stress in salt-loa... Eur J Pharmacol. 2008 Feb 2;580(1-2):201-13. | |||||
| REF 15 | Egr-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. | |||||
| REF 16 | Treatment 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 17 | Sulfobutyl ether-alkyl ether mixed cyclodextrin derivatives with enhanced inclusion ability. J Pharm Sci. 2009 Dec;98(12):4769-80. | |||||
| REF 18 | Efficacy 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 19 | Scaffold-based design and synthesis of potent N-type calcium channel blockers. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. | |||||
| REF 20 | Heteroaromatic side-chain analogs of pregabalin. Bioorg Med Chem Lett. 2006 May 1;16(9):2329-32. | |||||
| REF 21 | Structure-activity relationships of alpha-amino acid ligands for the alpha2delta subunit of voltage-gated calcium channels. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1138-41. | |||||
| REF 22 | Synthesis and in vivo evaluation of 3-substituted gababutins. Bioorg Med Chem Lett. 2010 Jan 1;20(1):362-5. | |||||
| REF 23 | Enantioselective synthesis of PD144723: a potent stereospecific anticonvulsant, Bioorg. Med. Chem. Lett. 4(6):823-826 (1994). | |||||
| REF 24 | N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1913-6. | |||||
| REF 25 | Synthesis and in vivo evaluation of bicyclic gababutins. Bioorg Med Chem Lett. 2010 Jan 15;20(2):461-4. | |||||
| REF 26 | Structure of human Ca(v)2.2 channel blocked by the painkiller ziconotide. Nature. 2021 Aug;596(7870):143-147. | |||||
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