Detail Information of Exogenous Modulation

General Information of Drug Transporter (DT)
DT ID	DTD0519 Transporter Info
Gene Name	CACNA1B
Transporter Name	Voltage-gated calcium channel alpha Cav2.2
Gene ID	774
UniProt ID	Q00975

Exogenous factors (drugs, dietary constituents, etc.) Modulation of This DT (EGM)
Chemical Compound
DT Modulation1	NOG protein co-treated with Valproic Acid co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in increased expression of CACNA1B mRNA		[21]
Regulation Mechanism			Transcription Factor Info
DT Modulation2	Valproic Acid affects the expression of CACNA1B mRNA		[32]
Regulation Mechanism			Transcription Factor Info
DT Modulation1	NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of CACNA1B mRNA		[21]
Regulation Mechanism			Transcription Factor Info
11-nor-delta(9)-tetrahydrocannabinol-9-carboxylic acid	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Cannabinoids results in increased abundance of 11-nor-delta(9)-tetrahydrocannabinol-9-carboxylic acid which affects the methylation of CACNA1B gene		[20]
Regulation Mechanism			Transcription Factor Info
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	2 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of CACNA1B mRNA		[21]
Regulation Mechanism			Transcription Factor Info
DT Modulation2	NOG protein co-treated with Valproic Acid co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in increased expression of CACNA1B mRNA		[21]
Regulation Mechanism			Transcription Factor Info
Barium	16 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	CACNA1B gene polymorphism affects the transport of Barium		[22]
Regulation Mechanism			Transcription Factor Info
DT Modulation2	CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation3	Cadmium Chloride inhibits the reaction CACNA1B protein results in increased transport of Barium		[24]
Regulation Mechanism			Transcription Factor Info
DT Modulation4	GNB1 protein binds to GNG2 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation5	GNB1 protein binds to GNG3 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation6	GNB1 protein binds to GNGT1 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation7	GNB2 protein binds to GNG2 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation8	GNB2 protein binds to GNG3 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation9	GNB2 protein binds to GNGT1 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation10	GNB3 protein binds to GNG2 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation11	GNB3 protein binds to GNG3 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation12	GNB3 protein binds to GNGT1 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation13	GNB4 protein binds to GNG2 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation14	GNB4 protein binds to GNG3 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation15	GNB4 protein binds to GNGT1 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
DT Modulation16	GNB5 protein binds to GNG2 protein inhibits the reaction CACNA1B protein results in increased transport of Barium		[23]
Regulation Mechanism			Transcription Factor Info
Benzo(a)pyrene	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Benzo(a)pyrene results in increased methylation of CACNA1B promoter		[25]
Regulation Mechanism			Transcription Factor Info
bisphenol A	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	bisphenol A results in decreased methylation of CACNA1B gene		[26]
Regulation Mechanism			Transcription Factor Info
Cadmium Chloride	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Cadmium Chloride inhibits the reaction CACNA1B protein results in increased transport of Barium		[24]
Regulation Mechanism			Transcription Factor Info
Cannabinoids	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Cannabinoids results in increased abundance of 11-nor-delta(9)-tetrahydrocannabinol-9-carboxylic acid which affects the methylation of CACNA1B gene		[20]
Regulation Mechanism			Transcription Factor Info
CGP 52608	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	CGP 52608 promotes the reaction RORA protein binds to CACNA1B gene		[27]
Regulation Mechanism			Transcription Factor Info
Cyclosporine	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Cyclosporine results in decreased methylation of CACNA1B promoter		[28]
Regulation Mechanism			Transcription Factor Info
dorsomorphin	2 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of CACNA1B mRNA		[21]
Regulation Mechanism			Transcription Factor Info
DT Modulation2	NOG protein co-treated with Valproic Acid co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in increased expression of CACNA1B mRNA		[21]
Regulation Mechanism			Transcription Factor Info
ethyl-p-hydroxybenzoate	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	ethyl-p-hydroxybenzoate results in decreased expression of CACNA1B mRNA		[29]
Regulation Mechanism			Transcription Factor Info
Methylcholanthrene	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Methylcholanthrene promotes the reaction AHR protein binds to CACNA1B promoter		[30]
Regulation Mechanism			Transcription Factor Info
propionaldehyde	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	propionaldehyde results in decreased expression of CACNA1B mRNA		[31]
Regulation Mechanism			Transcription Factor Info
sodium arsenite	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	sodium arsenite results in increased expression of CACNA1B mRNA		[12]
Regulation Mechanism			Transcription Factor Info
trichostatin A	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	trichostatin A results in increased expression of CACNA1B mRNA		[10]
Regulation Mechanism			Transcription Factor Info
Approved Drug
Clotrimazole	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Clotrimazole inhibits the activity of CACNA1B		[3]
Cell System	SH-SY5Y neuroblastoma cells-CACNA1B
Econazole	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Econazole inhibits the activity of CACNA1B		[3]
Cell System	SH-SY5Y neuroblastoma cells-CACNA1B
Miconazole	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Miconazole inhibits the activity of CACNA1B		[3]
Cell System	SH-SY5Y neuroblastoma cells-CACNA1B
Estradiol	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Estradiol increases the expression of CACNA1B		[4]
Menthol	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Menthol inhibits the expression of CACNA1B		[5]
Valproic Acid	3 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Valproic Acid increases the expression of CACNA1B		[6]
KB-2796	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Lomerizine inhibits the activity of CACNA1B		[7]
Hesperidin	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Hesperidin inhibits the activity of CACNA1B		[8]
Drug in Phase 3 Trial
Triclosan	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Triclosan inhibits the expression of CACNA1B		[13]
Cilnidipine	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Cilnidipine blocks the activity of CACNA1B		[16], [17]
Ralfinamide	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Ralfinamide blocks the activity of CACNA1B		[19]
Drug in Phase 2 Trial
CNV-2197944	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	CNV-2197944 blocks the activity of CACNA1B		[18]
Drug in Phase 1 Trial
Mibefradil	2 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Mibefradil inhibits the activity of CACNA1B		[1], [2]
Cell System	Human embryonic kidney 293 cells (HEK293)-CACNA1B
DT Modulation2	Mibefradil inhibits the activity of CACNA1B		[3]
Cell System	SH-SY5Y neuroblastoma cells-CACNA1B
Trichostatin A	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Trichostatin A increases the expression of CACNA1B		[10]
Sodium arsenite	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Sodium arsenite increases the expression of CACNA1B		[12]
Investigative Drug
Phenylmercuric Acetate	2 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Phenylmercuric Acetate inhibits the expression of CACNA1B		[11]
GNF-PF-3464	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	GNF-PF-3464 inhibits the activity of CACNA1B		[8]
Natural Product
Tobacco Smoke Pollution	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Tobacco Smoke Pollution inhibits the expression of CACNA1B		[15]
Health and Environmental Toxicant
Diethylhexyl Phthalate	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Diethylhexyl Phthalate inhibits the expression of CACNA1B		[14]
Herbicide
Atrazine	1 DT Activity Modulations Related to This Exogenous Factor	Click to Show/Hide the Full List
DT Modulation1	Atrazine increases the expression of CACNA1B		[9]

References
1	Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers. Bioorg Med Chem Lett. 2005 Jan 17;15(2):283-6.
2	Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5244-8.
3	Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca2+ entry in MDA-MB-231 breast cancer cells using a Fluorescence Imaging Plate Reader assay. Bioorg Med Chem. 2017 Jan 1;25(1):440-449.
4	Differential regulation of native estrogen receptor-regulatory elements by estradiol, tamoxifen, and raloxifene. Mol Endocrinol. 2008 Feb;22(2):287-303.
5	Repurposing L-Menthol for Systems Medicine and Cancer Therapeutics? L-Menthol Induces Apoptosis through Caspase 10 and by Suppressing HSP90. OMICS. 2016 Jan;20(1):53-64.
6	Stem Cell Transcriptome Responses and Corresponding Biomarkers That Indicate the Transition from Adaptive Responses to Cytotoxicity. Chem Res Toxicol. 2017 Apr 17;30(4):905-922.
7	Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers. Bioorg Med Chem Lett. 2007 Feb 1;17(3):662-7.
8	In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
9	Endoplasmic reticulum stress impairs insulin signaling through mitochondrial damage in SH-SY5Y cells. Neurosignals. 2012;20(4):265-80.
10	From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
11	A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
12	Cellular and Molecular Effects of Prolonged Low-Level Sodium Arsenite Exposure on Human Hepatic HepaRG Cells. Toxicol Sci. 2018 Apr 1;162(2):676-687.
13	Transcriptome and DNA Methylome Dynamics during Triclosan-Induced Cardiomyocyte Differentiation Toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
14	Di-(2-ethylhexyl)-phthalate induces apoptosis via the PPAR Gamma/PTEN/AKT pathway in differentiated human embryonic stem cells. Food Chem Toxicol. 2019 Sep;131:110552.
15	Integration of transcriptome analysis with pathophysiological endpoints to evaluate cigarette smoke toxicity in an in vitro human airway tissue model. Arch Toxicol. 2021 May;95(5):1739-1761.
16	Pharmacology of N-type Ca2+ channels distributed in cardiovascular system (Review). Int J Mol Med. 1999 May;3(5):455-66.
17	N- and L-type calcium channel antagonist improves glomerular dynamics, reverses severe nephrosclerosis, and inhibits apoptosis and proliferation in an l-NAME/SHR model. J Hypertens. 2002 May;20(5):993-1000.
18	Clinical pipeline report, company report or official report of Convergence Pharmaceuticals Ltd.
19	Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
20	Cannabinoid exposure and altered DNA methylation in rat and human sperm. Epigenetics. 2018;13(12):1208-1221.
21	Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
22	Identification and characterization of novel human Ca(v)2.2 (alpha 1B) calcium channel variants lacking the synaptic protein interaction site. J Neurosci. 2002;22(1):82-92.
23	Selective regulation of N-type Ca channels by different combinations of G-protein beta/gamma subunits and RGS proteins. J Neurosci. 2000;20(19):7143-8.
24	Appearance of voltage-gated calcium channels following overexpression of ATPase II cDNA in neuronal HN2 cells. Brain Res Mol Brain Res. 2003;117(2):109-15.
25	Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017;8(1):1369-1391.
26	DNA methylome-wide alterations associated with estrogen receptor-dependent effects of bisphenols in breast cancer. Clin Epigenetics. 2019;11(1):138.
27	Identification of potential target genes of ROR-alpha in THP1 and HUVEC cell lines. Exp Cell Res. 2017;353(1):6-15.
28	Integrative "-Omics" Analysis in Primary Human Hepatocytes Unravels Persistent Mechanisms of Cyclosporine A-Induced Cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
29	Risk assessment of parabens in a transcriptomics-based in vitro test. Chem Biol Interact. 2023;384:110699.
30	3-methylcholanthrene induces differential recruitment of aryl hydrocarbon receptor to human promoters. Toxicol Sci. 2010;117(1):90-100.
31	Integrated analysis of microRNA and mRNA expression profiles highlights aldehyde-induced inflammatory responses in cells relevant for lung toxicity. Toxicology. 2015 Aug 6;334:111-21.
32	Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20.

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Detail Information of Exogenous Modulation

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