Target Information
Target General Infomation | |||||
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Target ID |
T34234
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Former ID |
TTDS00251
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Target Name |
Vitamin D receptor
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Gene Name |
VDR
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Synonyms |
1,25-dihydroxyvitamin D3 receptor; Nuclear vitamin D receptor; Vitamin D(3) receptor; Vitamin D3 receptor; VDR
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Target Type |
Successful
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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.
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BioChemical Class |
Nuclear hormone receptor
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Target Validation |
T34234
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UniProt ID | |||||
Sequence |
MEAMAASTSLPDPGDFDRNVPRICGVCGDRATGFHFNAMTCEGCKGFFRRSMKRKALFTC
PFNGDCRITKDNRRHCQACRLKRCVDIGMMKEFILTDEEVQRKREMILKRKEEEALKDSL RPKLSEEQQRIIAILLDAHHKTYDPTYSDFCQFRPPVRVNDGGGSHPSRPNSRHTPSFSG DSSSSCSDHCITSSDMMDSSSFSNLDLSEEDSDDPSVTLELSQLSMLPHLADLVSYSIQK VIGFAKMIPGFRDLTSEDQIVLLKSSAIEVIMLRSNESFTMDDMSWTCGNQDYKYRVSDV TKAGHSLELIEPLIKFQVGLKKLNLHEEEHVLLMAICIVSPDRPGVQDAALIEAIQDRLS NTLQTYIRCRHPPPGSHLLYAKMIQKLADLRSLNEEHSKQYRCLSFQPECSMKLTPLVLE VFGNEIS |
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Drugs and Mode of Action | |||||
Drug(s) | Calcidiol | Drug Info | Approved | Vitamin D deficiency | [541966], [551437] |
Calcifediol | Drug Info | Approved | Vitamin D deficiency | [551871] | |
Calcipotriol | Drug Info | Approved | Psoriasis | [536361], [539823] | |
Cholecalciferol | Drug Info | Approved | Vitamin D deficiency | [538574], [539792] | |
Dihydrotachysterol | Drug Info | Approved | Hypocalcemia; Hypoparathyroidism | [551871] | |
Doxercalciferol | Drug Info | Approved | Chronic kidney disease; Kidney transplantation | [537117], [539836] | |
Ergocalciferol | Drug Info | Approved | Hypoparathyroidism | [538195] | |
Paricalcitol | Drug Info | Approved | Hyperparathyroidism | [536361], [539837] | |
S-06911 | Drug Info | Phase 3 | Osteoporosis | [544504] | |
Seocalcitol | Drug Info | Phase 3 | Rickets | [525779], [539822] | |
Inecalcitol oral | Drug Info | Phase 2 | Prostate cancer | [532222], [542712] | |
CTAP-201 | Drug Info | Phase 1 | Hyperparathyroidism | [522488] | |
RO-23-7553 | Drug Info | Phase 1 | Prostate disease | [521467] | |
Atocalcitol | Drug Info | Discontinued in Phase 2 | Psoriasis | [547286] | |
Lexacalcitol | Drug Info | Discontinued in Phase 2 | Cancer | [539820], [545353] | |
RO-26-9228 | Drug Info | Discontinued in Phase 2 | Urinary incontinence | [539830], [547313] | |
Tisocalcitate | Drug Info | Discontinued in Phase 2 | Psoriasis | [547723] | |
BXL-746 | Drug Info | Discontinued in Phase 1 | Inflammatory disease | [548376] | |
CB-1267 | Drug Info | Terminated | Prostate cancer | [546395] | |
CEP-4186 | Drug Info | Terminated | Acute myeloid leukemia | [547043] | |
Ecalcidene | Drug Info | Terminated | Acne vulgaris | [547789] | |
Inhibitor | 19-nor-14-epi-23-yne-1,25 dihydroxyvitamin D3 | Drug Info | [551374] | ||
KSP-BCS-1-alpha-CHF2-1624F2-2 | Drug Info | [528563] | |||
KSP-BCS-1-alpha-CHF2-20-epi-22-oxabishomo-26-OH | Drug Info | [528563] | |||
S-06911 | Drug Info | [526506] | |||
Seocalcitol | Drug Info | [551393] | |||
Tisocalcitate | Drug Info | [544140] | |||
Agonist | 1alpha,25 dihydroxyvitamin D(3) | Drug Info | [535063] | ||
2MD | Drug Info | [534740] | |||
3-keto-lithocholic acid | Drug Info | [526338] | |||
Atocalcitol | Drug Info | [530202] | |||
calcitriol-26,23-lactone | Drug Info | [533561] | |||
CTAP-201 | Drug Info | [544081] | |||
falecalcitriol | Drug Info | [525875] | |||
gemini | Drug Info | [526995] | |||
Inecalcitol oral | Drug Info | [532222] | |||
Lexacalcitol | Drug Info | [534521] | |||
LG190178 | Drug Info | [525489] | |||
Paricalcitol | Drug Info | [537420] | |||
RO-23-7553 | Drug Info | [534747], [551871] | |||
RO-26-9228 | Drug Info | [526506] | |||
Stimulator | BXL-746 | Drug Info | [529746] | ||
Antagonist | Calcidiol | Drug Info | [536026], [536733] | ||
Calcipotriol | Drug Info | [536677] | |||
Dihydrotachysterol | Drug Info | [536026], [537930] | |||
Doxercalciferol | Drug Info | [537117] | |||
Ergocalciferol | Drug Info | [536026], [536733] | |||
TEI-9647 | Drug Info | [528541] | |||
ZK159222 | Drug Info | [525922] | |||
Modulator | Calcifediol | Drug Info | [556264] | ||
CB-1267 | Drug Info | [525534] | |||
CEP-4186 | Drug Info | [534675] | |||
Ecalcidene | Drug Info | [527817] | |||
MC-1301 | Drug Info | ||||
Binder | Cholecalciferol | Drug Info | [536026], [536684], [537184] | ||
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 521467 | ClinicalTrials.gov (NCT00004926) ILX23-7553 in Treating Patients With Solid Tumors That Have Not Responded to Previous Therapy. U.S. National Institutes of Health. | ||||
Ref 522488 | ClinicalTrials.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 525779 | Seocalcitol (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 532222 | Inecalcitol, 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 536361 | Natural 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 538195 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040833. | ||||
Ref 538574 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021762. | ||||
Ref 539792 | (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 539820 | (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 539822 | (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 539823 | (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 539830 | (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 539836 | (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 539837 | (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 541966 | (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 542712 | (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 544504 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 700201063) | ||||
Ref 545353 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002985) | ||||
Ref 546395 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007891) | ||||
Ref 547043 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012493) | ||||
Ref 547286 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014844) | ||||
Ref 547313 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015074) | ||||
Ref 547723 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018814) | ||||
Ref 547789 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019289) | ||||
Ref 525489 | Novel 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 525534 | Novel 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 525875 | Synthesis 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 525922 | Carboxylic ester antagonists of 1alpha,25-dihydroxyvitamin D(3) show cell-specific actions. Chem Biol. 2000 Nov;7(11):885-94. | ||||
Ref 526338 | Vitamin D receptor as an intestinal bile acid sensor. Science. 2002 May 17;296(5571):1313-6. | ||||
Ref 526506 | Evidence 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 526995 | Novel Gemini analogs of 1alpha,25-dihydroxyvitamin D(3) with enhanced transcriptional activity. Biochem Pharmacol. 2004 Apr 1;67(7):1327-36. | ||||
Ref 527817 | Degradation 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 528541 | Further 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 528563 | J 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 529746 | Inter-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 530202 | Elocalcitol, 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 532222 | Inecalcitol, 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 533561 | Biological 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 534521 | The 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 534675 | Novel 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 534740 | New 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 534747 | Three 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 535063 | Kaposi sarcoma is a therapeutic target for vitamin D(3) receptor agonist. Blood. 2000 Nov 1;96(9):3188-94. | ||||
Ref 536026 | Overview of general physiologic features and functions of vitamin D. Am J Clin Nutr. 2004 Dec;80(6 Suppl):1689S-96S. | ||||
Ref 536677 | Cellular and molecular mechanisms involved in the action of vitamin D analogs targeting vitiligo depigmentation. Curr Drug Targets. 2008 Apr;9(4):345-59. | ||||
Ref 536733 | Vitamin D in health and disease. Clin J Am Soc Nephrol. 2008 Sep;3(5):1535-41. Epub 2008 Jun 4. | ||||
Ref 537184 | Genetic 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. | ||||
Ref 537420 | New 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 537930 | In 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 544081 | Vascular 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 544140 | The 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. |
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