Page last updated: 2024-08-07 15:55:06
Vitamin D3 receptor
A vitamin D3 receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11473]
Synonyms
VDR;
1,25-dihydroxyvitamin D3 receptor;
Nuclear receptor subfamily 1 group I member 1
Research
Bioassay Publications (52)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (1.92) | 18.2507 |
| 2000's | 11 (21.15) | 29.6817 |
| 2010's | 34 (65.38) | 24.3611 |
| 2020's | 6 (11.54) | 2.80 |
Compounds (29)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Identification of the Histidine Residue in Vitamin D Receptor That Covalently Binds to Electrophilic Ligands.Journal of medicinal chemistry, , Jul-26, Volume: 61, Issue:14, 2018
25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin DJournal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Structural development of non-secosteroidal vitamin D receptor (VDR) ligands without any asymmetric carbon.Bioorganic & medicinal chemistry, , 12-15, Volume: 26, Issue:23-24, 2018
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.Journal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs).European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Vitamin D Analogues with a p-Hydroxyphenyl Group at the C25 Position: Crystal Structure of Vitamin D Receptor Ligand-Binding Domain Complexed with the Ligand Explains the Mechanism Underlying Full Antagonistic Action.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Structural development of stapled short helical peptides as vitamin D receptor (VDR)-coactivator interaction inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Fine tuning of agonistic/antagonistic activity for vitamin D receptor by 22-alkyl chain length of ligands: 22S-Hexyl compound unexpectedly restored agonistic activity.Bioorganic & medicinal chemistry, , Nov-15, Volume: 23, Issue:22, 2015
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1α-Hydroxyl Derivatives.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
A mixed population of antagonist and agonist binding conformers in a single crystal explains partial agonism against vitamin D receptor: active vitamin D analogues with 22R-alkyl group.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
Synthesis of VS-105: A novel and potent vitamin D receptor agonist with reduced hypercalcemic effects.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 23, Issue:21, 2013
Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Synthesis of 2α-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.ACS medicinal chemistry letters, , Jul-11, Volume: 4, Issue:7, 2013
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Structural basis for the accommodation of bis- and tris-aromatic derivatives in vitamin D nuclear receptor.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.Bioorganic & medicinal chemistry, , Jun-01, Volume: 18, Issue:11, 2010
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
(2S,2'R)-analogue of LG190178 is a major active isomer.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 18, Issue:1, 2008
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.Journal of medicinal chemistry, , Mar-08, Volume: 50, Issue:5, 2007
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3).Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
New dermatological agents for the treatment of psoriasis.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Vitamin D3 analogues that contain modified A- and seco-B-rings as hedgehog pathway inhibitors.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 24, Issue:22, 2014
Structure-activity relationships for vitamin D3-based aromatic a-ring analogues as hedgehog pathway inhibitors.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Identification of vitamin d3-based hedgehog pathway inhibitors that incorporate an aromatic a-ring isostere.ACS medicinal chemistry letters, , Jul-11, Volume: 4, Issue:7, 2013
Probing the structural requirements for vitamin D3 inhibition of the hedgehog signaling pathway.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1α-Hydroxyl Derivatives.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 15, Issue:19, 2005
Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.Chemistry & biology, , Volume: 6, Issue:5, 1999
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 15, Issue:19, 2005
Enables
This protein enables 10 target(s):
| Target | Category | Definition |
|---|
| DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
| DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
| nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
| bile acid nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a bile acid that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:bf, PMID:12016314] |
| nuclear retinoid X receptor binding | molecular function | Binding to a nuclear retinoid X receptor. [GOC:ai] |
| calcitriol binding | molecular function | Binding to calcitriol. Calcitriol (1,25-dihydroxycholecalciferol) is the hormonally active form of vitamin D3. [GOC:TermGenie, PMID:21872797, Wikipedia:Calcitriol_receptor] |
| lithocholic acid binding | molecular function | Binding to lithocholic acid. [GOC:bf, GOC:TermGenie, PMID:20371703] |
| RNA polymerase II cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| RNA polymerase II transcription regulator complex | cellular component | A transcription factor complex that acts at a regulatory region of a gene transcribed by RNA polymerase II. [GOC:tb] |
| chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 27 target(s):
| Target | Category | Definition |
|---|
| negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
| cell morphogenesis | biological process | The developmental process in which the size or shape of a cell is generated and organized. [GOC:clt, GOC:dph, GOC:go_curators, GOC:tb] |
| skeletal system development | biological process | The process whose specific outcome is the progression of the skeleton over time, from its formation to the mature structure. The skeleton is the bony framework of the body in vertebrates (endoskeleton) or the hard outer envelope of insects (exoskeleton or dermoskeleton). [GOC:dph, GOC:jid, GOC:tb] |
| calcium ion transport | biological process | The directed movement of calcium (Ca) ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| intracellular calcium ion homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah] |
| lactation | biological process | The regulated release of milk from the mammary glands and the period of time that a mother lactates to feed her young. [ISBN:0198506732] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| negative regulation of keratinocyte proliferation | biological process | Any process that decreases the rate, frequency or extent of keratinocyte proliferation. Keratinocyte proliferation is the multiplication or reproduction of keratinocytes, resulting in the expansion of a cell population. [GOC:dph, GOC:tb] |
| positive regulation of vitamin D 24-hydroxylase activity | biological process | Any process that increases the rate, frequency or extent of vitamin D 24-hydroxylase activity. Vitamin D 24-hydroxylase activity catalyzes the hydroxylation of C-24 of any form of vitamin D. [GOC:BHF, GOC:dph, GOC:tb] |
| positive regulation of bone mineralization | biological process | Any process that activates or increases the frequency, rate or extent of bone mineralization. [GOC:go_curators] |
| phosphate ion transmembrane transport | biological process | The process in which a phosphate is transported across a membrane. [GOC:vw] |
| bile acid signaling pathway | biological process | The series of molecular signals initiated by bile acid binding to its receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:signaling, PMID:12016314] |
| mRNA transcription by RNA polymerase II | biological process | The cellular synthesis of messenger RNA (mRNA) from a DNA template by RNA polymerase II, originating at an RNA polymerase II promoter. [GOC:jl, ISBN:0321000382] |
| positive regulation of keratinocyte differentiation | biological process | Any process that activates or increases the frequency, rate or extent of keratinocyte differentiation. [GOC:go_curators] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| decidualization | biological process | The cellular and vascular changes occurring in the endometrium of the pregnant uterus just after the onset of blastocyst implantation. This process involves the proliferation and differentiation of the fibroblast-like endometrial stromal cells into large, polyploid decidual cells that eventually form the maternal component of the placenta. [ISBN:0721662544, PMID:11133685] |
| intestinal absorption | biological process | A process in which nutrients are taken up from the contents of the intestine. [GOC:ai, GOC:dph] |
| apoptotic process involved in mammary gland involution | biological process | Any apoptotic process that triggers the activity of proteolytic caspases whose actions dismantle the mammary epithelial cells resulting in their programmed cell death. [GOC:dph, GOC:mtg_apoptosis] |
| positive regulation of apoptotic process involved in mammary gland involution | biological process | Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process of mammary epithelial cells during mammary gland involution. [GOC:dph, GOC:mtg_apoptosis, PMID:15282149] |
| regulation of calcidiol 1-monooxygenase activity | biological process | Any process that modulates the rate, frequency or extent of calcidiol 1-monooxygenase activity. Calcidiol 1-monooxygenase activity is catalysis of the reaction: calcidiol + NADPH + H+ + O2 = calcitriol + NADP+ + H2O. [GOC:BHF, GOC:dph, GOC:tb] |
| mammary gland branching involved in pregnancy | biological process | The process in which the branching structure of the mammary gland duct is generated and organized as a part of pregnancy. [GOC:dph, PMID:19261859] |
| vitamin D receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a vitamin D receptor binding to one of its physiological ligands. [GOC:BHF, GOC:mah, PMID:12637589] |
| positive regulation of vitamin D receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of vitamin D receptor signaling pathway activity. [GOC:BHF, GOC:mah] |
| response to bile acid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a bile acid stimulus. [GO_REF:0000071, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:21757002] |
| multicellular organism development | biological process | The biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb] |
| cell differentiation | biological process | The cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732] |