Target Information

Target General Infomation
Target ID
T34234
Former ID
TTDS00251
Target Name
Vitamin D receptor
Gene Name
VDR
Synonyms
1,25-dihydroxyvitamin D3 receptor; Nuclear vitamin D receptor; Vitamin D(3) receptor; Vitamin D3 receptor; VDR
Target Type
Successful
Disease Acute myeloid leukemia [ICD9: 205; ICD10: C92.0]
Acne vulgaris [ICD9: 706.1; ICD10: L70.0]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Chronic kidney disease; Kidney transplantation [ICD9: 403, 580-589, 585.1-585.5, 585.9, 996; ICD10: N00-N29, N18, T86]
Hypoparathyroidism [ICD9: 252.1; ICD10: E20, E89.2, P71.4]
Hypocalcemia; Hypoparathyroidism [ICD9: 252.0, 275.41; ICD10: E21, E83.51]
Hyperparathyroidism [ICD9: 252.02, 588.81; ICD10: E21.1]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890]
Psoriasis [ICD9: 696; ICD10: L40]
Prostate disease [ICD10: N42.9]
Prostate cancer [ICD9: 185; ICD10: C61]
Rickets [ICD10: E55]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Vitamin D deficiency [ICD9: 268; ICD10: E55]
Unspecified [ICD code not available]
Function
Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Recruited to promoters via its interaction with BAZ1B/WSTF which mediates the interaction with acetylated histones, an essential step for VDR-promoter association. Plays a central role in calcium homeostasis.
BioChemical Class
Nuclear hormone receptor
Target Validation
T34234
UniProt ID
P11473
Sequence
MEAMAASTSLPDPGDFDRNVPRICGVCGDRATGFHFNAMTCEGCKGFFRRSMKRKALFTC
PFNGDCRITKDNRRHCQACRLKRCVDIGMMKEFILTDEEVQRKREMILKRKEEEALKDSL
RPKLSEEQQRIIAILLDAHHKTYDPTYSDFCQFRPPVRVNDGGGSHPSRPNSRHTPSFSG
DSSSSCSDHCITSSDMMDSSSFSNLDLSEEDSDDPSVTLELSQLSMLPHLADLVSYSIQK
VIGFAKMIPGFRDLTSEDQIVLLKSSAIEVIMLRSNESFTMDDMSWTCGNQDYKYRVSDV
TKAGHSLELIEPLIKFQVGLKKLNLHEEEHVLLMAICIVSPDRPGVQDAALIEAIQDRLS
NTLQTYIRCRHPPPGSHLLYAKMIQKLADLRSLNEEHSKQYRCLSFQPECSMKLTPLVLE
VFGNEIS
Drugs and Mode of Action
Drug(s) Calcidiol Drug Info Approved Vitamin D deficiency [1], [2]
Calcifediol Drug Info Approved Vitamin D deficiency [3]
Calcipotriol Drug Info Approved Psoriasis [4], [5]
Cholecalciferol Drug Info Approved Vitamin D deficiency [6], [7]
Dihydrotachysterol Drug Info Approved Hypocalcemia; Hypoparathyroidism [3]
Doxercalciferol Drug Info Approved Chronic kidney disease; Kidney transplantation [8], [9]
Ergocalciferol Drug Info Approved Hypoparathyroidism [10]
Paricalcitol Drug Info Approved Hyperparathyroidism [4], [11]
S-06911 Drug Info Phase 3 Osteoporosis [12]
Seocalcitol Drug Info Phase 3 Rickets [13], [14]
Inecalcitol oral Drug Info Phase 2 Prostate cancer [15], [16]
CTAP-201 Drug Info Phase 1 Hyperparathyroidism [17]
RO-23-7553 Drug Info Phase 1 Prostate disease [18]
Atocalcitol Drug Info Discontinued in Phase 2 Psoriasis [19]
Lexacalcitol Drug Info Discontinued in Phase 2 Cancer [20], [21]
RO-26-9228 Drug Info Discontinued in Phase 2 Urinary incontinence [22], [23]
Tisocalcitate Drug Info Discontinued in Phase 2 Psoriasis [24]
BXL-746 Drug Info Discontinued in Phase 1 Inflammatory disease [25]
CB-1267 Drug Info Terminated Prostate cancer [26]
CEP-4186 Drug Info Terminated Acute myeloid leukemia [27]
Ecalcidene Drug Info Terminated Acne vulgaris [28]
Inhibitor 19-nor-14-epi-23-yne-1,25 dihydroxyvitamin D3 Drug Info [29]
KSP-BCS-1-alpha-CHF2-1624F2-2 Drug Info [30]
KSP-BCS-1-alpha-CHF2-20-epi-22-oxabishomo-26-OH Drug Info [30]
S-06911 Drug Info [31]
Seocalcitol Drug Info [32]
Tisocalcitate Drug Info [33]
Agonist 1alpha,25 dihydroxyvitamin D(3) Drug Info [34]
2MD Drug Info [35]
3-keto-lithocholic acid Drug Info [36]
Atocalcitol Drug Info [37]
calcitriol-26,23-lactone Drug Info [38]
CTAP-201 Drug Info [39]
falecalcitriol Drug Info [40]
gemini Drug Info [41]
Inecalcitol oral Drug Info [15]
Lexacalcitol Drug Info [42]
LG190178 Drug Info [43]
Paricalcitol Drug Info [44]
RO-23-7553 Drug Info [45], [3]
RO-26-9228 Drug Info [31]
Stimulator BXL-746 Drug Info [46]
Antagonist Calcidiol Drug Info [47], [48]
Calcipotriol Drug Info [49]
Dihydrotachysterol Drug Info [47], [50]
Doxercalciferol Drug Info [8]
Ergocalciferol Drug Info [47], [48]
TEI-9647 Drug Info [51]
ZK159222 Drug Info [52]
Modulator Calcifediol Drug Info [53]
CB-1267 Drug Info [54]
CEP-4186 Drug Info [55]
Ecalcidene Drug Info [56]
MC-1301 Drug Info
Binder Cholecalciferol Drug Info [47], [57], [58]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Endocrine and other factor-regulated calcium reabsorption
Mineral absorption
Tuberculosis
NetPath Pathway IL4 Signaling Pathway
PANTHER Pathway Vitamin D metabolism and pathway
Pathway Interaction Database Regulation of nuclear SMAD2/3 signaling
Direct p53 effectors
RXR and RAR heterodimerization with other nuclear receptor
Retinoic acid receptors-mediated signaling
Validated transcriptional targets of deltaNp63 isoforms
Validated transcriptional targets of TAp63 isoforms
Reactome Nuclear Receptor transcription pathway
WikiPathways Ovarian Infertility Genes
Nuclear Receptors in Lipid Metabolism and Toxicity
Nuclear Receptors Meta-Pathway
Vitamin D Receptor Pathway
Drug Induction of Bile Acid Pathway
Nuclear Receptors
Vitamin D Metabolism
References
REF 1(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: 6921).
REF 2Drug Information of Carbetocin from nextbio research in illumina. 2015.
REF 3Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 4Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
REF 5(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: 2778).
REF 6FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021762.
REF 7(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: 2747).
REF 8Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.
REF 9(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: 2790).
REF 10FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040833.
REF 11(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: 2791).
REF 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 700201063)
REF 13Seocalcitol (EB 1089): a vitamin D analogue of anti-cancer potential. Background, design, synthesis, pre-clinical and clinical evaluation. Curr Pharm Des. 2000 May;6(7):803-28.
REF 14(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: 2777).
REF 15Inecalcitol, an analog of 1,25D3, displays enhanced antitumor activity through the induction of apoptosis in a squamous cell carcinoma model system. Cell Cycle. 2013 Mar 1;12(5):743-52.
REF 16(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: 7747).
REF 17ClinicalTrials.gov (NCT00792857) Comparison of I.V. CTAP201 and Doxercalciferol (Hectorol) in Subjects With Chronic Kidney Disease (CKD) and Secondary Hyperparathyroidism (SHPT). U.S. National Institutes of Health.
REF 18ClinicalTrials.gov (NCT00004926) ILX23-7553 in Treating Patients With Solid Tumors That Have Not Responded to Previous Therapy. U.S. National Institutes of Health.
REF 19Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014844)
REF 20(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: 2775).
REF 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002985)
REF 22(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: 2785).
REF 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015074)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018814)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025073)
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007891)
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012493)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019289)
REF 29The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 30J Med Chem. 2006 Dec 14;49(25):7513-7.Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
REF 31Evidence for tissue- and cell-type selective activation of the vitamin D receptor by Ro-26-9228, a noncalcemic analog of vitamin D3. J Cell Biochem. 2003 Feb 1;88(2):267-73.
REF 32How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 33The Rationale Behind Topical Vitamin D Analogs in the Treatment of Psoriasis: Where Does Topical Calcitriol Fit In?. J Clin Aesthet Dermatol. 2010 August; 3(8): 46-53.
REF 34Kaposi sarcoma is a therapeutic target for vitamin D(3) receptor agonist. Blood. 2000 Nov 1;96(9):3188-94.
REF 35New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues. J Med Chem. 1998 Nov 5;41(23):4662-74.
REF 36Vitamin D receptor as an intestinal bile acid sensor. Science. 2002 May 17;296(5571):1313-6.
REF 37Elocalcitol, a vitamin D3 analog for the potential treatment of benign prostatic hyperplasia, overactive bladder and male infertility. IDrugs. 2009 Jun;12(6):381-93.
REF 38Biological activity of 24,24-difluoro-1 alpha, 25-dihydroxyvitamin D3 and 1 alpha, 25-dihydroxyvitamin D3-26,23-lactone in inducing differentiation of human myeloid leukemia cells. Arch Biochem Biophys. 1983 Jan;220(1):90-4.
REF 39Vascular calcification and secondary hyperparathyroidism of severe chronic kidney disease and its relation to serum phosphate and calcium levels. Br J Pharmacol. 2009 April; 156(8): 1267-1278.
REF 40Synthesis and biological evaluations of A-ring isomers of 26,26,26,27,27,27-hexafluoro-1,25-dihydroxyvitamin D3. Bioorg Med Chem. 2000 Aug;8(8):2157-66.
REF 41Novel Gemini analogs of 1alpha,25-dihydroxyvitamin D(3) with enhanced transcriptional activity. Biochem Pharmacol. 2004 Apr 1;67(7):1327-36.
REF 42The vitamin D analog, KH1060, is rapidly degraded both in vivo and in vitro via several pathways: principal metabolites generated retain significant biological activity. Endocrinology. 1997 Dec;138(12):5485-96.
REF 43Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3. Chem Biol. 1999 May;6(5):265-75.
REF 44New Acquisitions in Therapy of Secondary Hyperparathyroidism in Chronic Kidney Disease and Peritoneal Dialysis Patients: Role of Vitamin D Receptor Activators. Contrib Nephrol. 2009;163:219-226. Epub 2009 Jun 3.
REF 45Three synthetic vitamin D analogues induce prostate-specific acid phosphatase and prostate-specific antigen while inhibiting the growth of human prostate cancer cells in a vitamin D receptor-dependent fashion. Clin Cancer Res. 1997 Aug;3(8):1331-8.
REF 46Inter-species differences in sensitivity to the calcemic activity of the novel 1,25-dihydroxyvitamin D3 analog BXL746. Regul Toxicol Pharmacol. 2008 Dec;52(3):332-41.
REF 47Overview of general physiologic features and functions of vitamin D. Am J Clin Nutr. 2004 Dec;80(6 Suppl):1689S-96S.
REF 48Vitamin D in health and disease. Clin J Am Soc Nephrol. 2008 Sep;3(5):1535-41. Epub 2008 Jun 4.
REF 49Cellular and molecular mechanisms involved in the action of vitamin D analogs targeting vitiligo depigmentation. Curr Drug Targets. 2008 Apr;9(4):345-59.
REF 50In vivo metabolism of the vitamin D analog, dihydrotachysterol. Evidence for formation of 1 alpha,25- and 1 beta,25-dihydroxy-dihydrotachysterol metabolites and studies of their biological activity. J Biol Chem. 1993 Jan 5;268(1):282-92.
REF 51Further synthetic and biological studies on vitamin D hormone antagonists based on C24-alkylation and C2alpha-functionalization of 25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones. J Med Chem. 2006 Nov 30;49(24):7063-75.
REF 52Carboxylic ester antagonists of 1alpha,25-dihydroxyvitamin D(3) show cell-specific actions. Chem Biol. 2000 Nov;7(11):885-94.
REF 53Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 54Novel 20-epi-vitamin D3 analog combined with 9-cis-retinoic acid markedly inhibits colony growth of prostate cancer cells. Prostate. 1999 Aug 1;40(3):141-9.
REF 55Novel vitamin D3 analog (CB1093) when combined with paclitaxel and cisplatin inhibit growth of MCF-7 human breast cancer cells in vivo. Int J Oncol. 1998 Sep;13(3):421-8.
REF 56Degradation chemistry of a Vitamin D analogue (ecalcidene) investigated by HPLC-MS, HPLC-NMR and chemical derivatization. J Pharm Biomed Anal. 2006 Mar 3;40(4):850-63. Epub 2005 Oct 20.
REF 57Vitamin D2 or vitamin D3?. Rev Med Interne. 2008 Oct;29(10):815-20. Epub 2008 Apr 11.
REF 58Genetic polymorphisms in vitamin D receptor, vitamin D-binding protein, Toll-like receptor 2, nitric oxide synthase 2, and interferon-gamma genes and its association with susceptibility to tuberculosis. Braz J Med Biol Res. 2009 Apr;42(4):312-22.

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