Retinoic acid receptor RXR-alpha

A retinoic acid receptor RXR-alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P19793]

Synonyms

Nuclear receptor subfamily 2 group B member 1;
Retinoid X receptor alpha

Research

Bioassay Publications (75)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	16 (21.33)	18.2507
2000's	16 (21.33)	29.6817
2010's	33 (44.00)	24.3611
2020's	10 (13.33)	2.80

Compounds (48)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
lg 100268	Homo sapiens (human)	IC50	0.0080	1	1
lg 100268	Homo sapiens (human)	Ki	0.0113	3	3
bexarotene	Homo sapiens (human)	IC50	0.6320	1	1
bexarotene	Homo sapiens (human)	Ki	0.1647	7	7
hx 600	Homo sapiens (human)	Ki	1.9000	1	1
tretinoin	Homo sapiens (human)	IC50	1.0000	1	1
tretinoin	Homo sapiens (human)	Ki	0.2268	3	3
docosahexaenoate	Homo sapiens (human)	Ki	6.2920	1	1
eicosapentaenoic acid	Homo sapiens (human)	Ki	7.6320	1	1
t0901317	Homo sapiens (human)	Ki	0.1268	4	4
alitretinoin	Homo sapiens (human)	IC50	0.0305	2	2
alitretinoin	Homo sapiens (human)	Ki	0.2179	5	5
sulindac	Homo sapiens (human)	IC50	82.9000	1	1
lg 100567	Homo sapiens (human)	Ki	0.1138	1	2
fenretinide	Homo sapiens (human)	Ki	2.2000	1	1
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid	Homo sapiens (human)	IC50	1.0000	1	1
pregna-4,17-diene-3,16-dione	Homo sapiens (human)	IC50	33.0000	1	1
lg100754	Homo sapiens (human)	Ki	0.0080	1	1
lg 1506	Homo sapiens (human)	IC50	0.0080	1	1
lg 1506	Homo sapiens (human)	Ki	0.0063	4	4
nrx 194204	Homo sapiens (human)	IC50	0.0060	1	1
bms453	Homo sapiens (human)	Ki	0.0139	3	3
hx 630	Homo sapiens (human)	Ki	0.9000	1	1
way 252623	Homo sapiens (human)	IC50	10.0000	1	1
[5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid	Homo sapiens (human)	IC50	2.4000	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
domperidone	Homo sapiens (human)	Kd	8.8000	1	1
lg 100268	Homo sapiens (human)	EC50	0.0220	5	5
lg 100268	Homo sapiens (human)	Kd	0.0030	1	1
oxaprozin	Homo sapiens (human)	EC50	16.1000	1	1
pirinixic acid	Homo sapiens (human)	EC50	9.1000	1	1
pirinixic acid	Homo sapiens (human)	Kd	1.2800	1	1
3,3',5-triiodothyroacetic acid	Homo sapiens (human)	EC50	12.0000	1	1
3,3',5-triiodothyroacetic acid	Homo sapiens (human)	Kd	1.3200	1	1
thyroxine	Homo sapiens (human)	EC50	15.4000	1	1
thyroxine	Homo sapiens (human)	Kd	0.9300	1	1
Berberine chloride (TN)	Homo sapiens (human)	Kd	24.8000	1	1
pioglitazone hydrochloride	Homo sapiens (human)	EC50	0.4900	1	1
tetraiodothyroacetic acid	Homo sapiens (human)	EC50	2.9600	2	2
tetraiodothyroacetic acid	Homo sapiens (human)	Kd	1.5000	1	1
honokiol	Homo sapiens (human)	EC50	11.8000	1	1
bexarotene	Homo sapiens (human)	EC50	0.0390	21	21
bexarotene	Homo sapiens (human)	Kd	0.2691	9	15
dehydroabietic acid	Homo sapiens (human)	EC50	42.0000	1	1
sr 11237	Homo sapiens (human)	EC50	0.0340	1	1
isopimaric acid	Homo sapiens (human)	EC50	26.0000	1	1
tretinoin	Homo sapiens (human)	EC50	0.6141	7	8
tretinoin	Homo sapiens (human)	Kd	0.0681	6	8
gw 3965	Homo sapiens (human)	EC50	0.0003	2	2
t0901317	Homo sapiens (human)	EC50	0.0001	2	2
alitretinoin	Homo sapiens (human)	EC50	0.0772	14	14
alitretinoin	Homo sapiens (human)	Kd	0.3115	12	12
sr 11217	Homo sapiens (human)	EC50	0.0860	1	1
calcitriol	Homo sapiens (human)	EC50	0.0016	1	1
clothiapine	Homo sapiens (human)	Kd	15.0100	1	1
nk 104	Homo sapiens (human)	Kd	13.3000	1	1
lg 100567	Homo sapiens (human)	EC50	0.1340	1	1
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid	Homo sapiens (human)	EC50	5.0000	2	2
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid	Homo sapiens (human)	Kd	11.0400	1	1
agn 191659	Homo sapiens (human)	EC50	0.0110	1	1
agn 191701	Homo sapiens (human)	EC50	0.2010	1	1
pregna-4,17-diene-3,16-dione	Homo sapiens (human)	EC50	100.0000	1	1
valerenic acid	Homo sapiens (human)	EC50	27.0000	1	1
lg100754	Homo sapiens (human)	EC50	0.0020	1	1
lg 1506	Homo sapiens (human)	EC50	0.0057	3	3
nrx 194204	Homo sapiens (human)	EC50	0.0002	1	1
nrx 194204	Homo sapiens (human)	Kd	0.0004	2	2
agn 194204	Homo sapiens (human)	Kd	0.0015	1	1
uab 30	Homo sapiens (human)	EC50	0.8350	2	2
uab 30	Homo sapiens (human)	Kd	0.6610	5	5
sr 11302	Homo sapiens (human)	EC50	1.0000	1	1
bms 687453	Homo sapiens (human)	EC50	25.0000	1	1
way 252623	Homo sapiens (human)	EC50	0.0003	2	2
[5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid	Homo sapiens (human)	Kd	2.3800	1	1
1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1h-benzotriazole-5-carboxylic acid	Homo sapiens (human)	EC50	0.1430	3	3

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
lg 100268	Homo sapiens (human)	Efficacy	0.0435	2	2
honokiol	Homo sapiens (human)	ED50	11.8000	1	1
bexarotene	Homo sapiens (human)	Activity	3.7400	1	1
6-(1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-naphthyl)-2-naphthalenecarboxylic acid	Homo sapiens (human)	AC50	1.0000	1	1
docosahexaenoate	Homo sapiens (human)	ED50	50.0000	1	1
alitretinoin	Homo sapiens (human)	AC50	0.0070	1	1
alitretinoin	Homo sapiens (human)	Activity	3.4500	1	1
sr 11217	Homo sapiens (human)	AC50	0.1600	1	1
bigelovin	Homo sapiens (human)	ED50	4.9000	1	1
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid	Homo sapiens (human)	AC50	1.0000	1	1
nrx 194204	Homo sapiens (human)	Efficacy	0.0440	2	2

Enables

This protein enables 21 target(s):

Target	Category	Definition
transcription cis-regulatory region binding	molecular function	Binding to a specific sequence of DNA that is part of a regulatory region that controls transcription of that section of the DNA. The transcribed region might be described as a gene, cistron, or operon. [GOC:txnOH]
RNA polymerase II transcription regulatory region sequence-specific DNA binding	molecular function	Binding to a specific sequence of DNA that is part of a regulatory region that controls the transcription of a gene or cistron by RNA polymerase II. [GOC:txnOH]
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]
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]
transcription coregulator binding	molecular function	Binding to a transcription coregulator, a protein involved in regulation of transcription via protein-protein interactions with transcription factors and other transcription regulatory proteins. Cofactors do not bind DNA directly, but rather mediate protein-protein interactions between regulatory transcription factors and the basal transcription machinery. [GOC:krc]
retinoic acid binding	molecular function	Binding to retinoic acid, 3,7-dimethyl-9-(2,6,-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraenoic acid. [GOC:hjd]
double-stranded DNA binding	molecular function	Binding to double-stranded DNA. [GOC:elh, GOC:vw]
DNA-binding transcription factor activity	molecular function	A transcription regulator activity that modulates transcription of gene sets via selective and non-covalent binding to a specific double-stranded genomic DNA sequence (sometimes referred to as a motif) within a cis-regulatory region. Regulatory regions include promoters (proximal and distal) and enhancers. Genes are transcriptional units, and include bacterial operons. [GOC:txnOH-2018]
nuclear steroid receptor activity	molecular function	Combining with a steroid hormone and transmitting the signal within the cell to initiate a change in cell activity or function. [GOC:signaling, PMID:14708019]
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]
enzyme binding	molecular function	Binding to an enzyme, a protein with catalytic activity. [GOC:jl]
peptide binding	molecular function	Binding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl]
identical protein binding	molecular function	Binding to an identical protein or proteins. [GOC:jl]
nuclear vitamin D receptor binding	molecular function	Binding to a nuclear vitamin D receptor, a nuclear receptor that mediates the action of vitamin D by binding DNA and controlling the transcription of hormone-sensitive genes. [GOC:jl, PMID:12637589]
sequence-specific DNA binding	molecular function	Binding to DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA e.g. promotor binding or rDNA binding. [GOC:jl]
retinoic acid-responsive element binding	molecular function	Binding to a retinoic acid-responsive element, a variable direct repeat of the sequence PuGGTCA spaced by five nucleotides (DR5) found in the promoters of retinoic acid-responsive genes, to which retinoic acid receptors bind. [GOC:jl, GOC:vw, GOC:yaf, PMID:11327309, PMID:19917671]
DNA binding domain binding	molecular function	Binding to a protein's DNA binding domain (DBD). [PMID:9682036]
LBD domain binding	molecular function	Binding to a protein's ligand binding domain (LBD) domain, found in nuclear receptors. In general, the LBDs consist of three layers comprised of twelve alpha-helices and several beta-strands that are organized around a lipophilic ligand-binding pocket. [PMID:9682036]
sequence-specific double-stranded DNA binding	molecular function	Binding to double-stranded DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA, e.g. promotor binding or rDNA binding. [GOC:dos, GOC:sl]

Located In

This protein is located in 4 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]
mitochondrion	cellular component	A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732]
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]

Part Of

This protein is part of 4 target(s):

Target	Category	Definition
transcription regulator complex	cellular component	A protein complex that is capable of associating with DNA by direct binding, or via other DNA-binding proteins or complexes, and regulating transcription. [GOC:jl]
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 15 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]
positive regulation of thyroid hormone mediated signaling pathway	biological process	Any process that increases the frequency, rate or extent of thyroid hormone mediated signaling pathway. [GOC:hjd]
hormone-mediated signaling pathway	biological process	The series of molecular signals mediated by the detection of a hormone. [GOC:sm]
positive regulation of bone mineralization	biological process	Any process that activates or increases the frequency, rate or extent of bone mineralization. [GOC:go_curators]
positive regulation of transporter activity	biological process	Any process that activates or increases the activity of a transporter. [GOC:mah]
response to retinoic 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 retinoic acid stimulus. [GOC:sl]
peroxisome proliferator activated receptor signaling pathway	biological process	The series of molecular signals initiated by binding of a ligand to any of the peroxisome proliferator activated receptors (alpha, beta or gamma) in the nuclear membrane, and ending with the initiation or termination of the transcription of target genes. [GOC:BHF, PMID:18221086]
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]
steroid hormone mediated signaling pathway	biological process	The series of molecular signals mediated by a steroid hormone binding to a receptor. [PMID:12606724]
positive regulation of DNA-templated transcription	biological process	Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH]
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]
retinoic acid receptor signaling pathway	biological process	The series of molecular signals generated as a consequence of a retinoic acid receptor binding to one of its physiological ligands. [GOC:dgh]
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]
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]
anatomical structure development	biological process	The biological process whose specific outcome is the progression of an anatomical structure from an initial condition to its mature state. This process begins with the formation of the structure and ends with the mature structure, whatever form that may be including its natural destruction. An anatomical structure is any biological entity that occupies space and is distinguished from its surroundings. Anatomical structures can be macroscopic such as a carpel, or microscopic such as an acrosome. [GO_REF:0000021]