Proteins > Endothelial PAS domain-containing protein 1
Page last updated: 2024-08-07 17:23:40
Endothelial PAS domain-containing protein 1
An endothelial PAS domain-containing protein 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99814]
Synonyms
EPAS-1;
Basic-helix-loop-helix-PAS protein MOP2;
Class E basic helix-loop-helix protein 73;
bHLHe73;
HIF-1-alpha-like factor;
HLF;
Hypoxia-inducible factor 2-alpha;
HIF-2-alpha;
HIF2-alpha;
Member of PAS protein 2;
Research
Bioassay Publications (20)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 11 (55.00) | 29.6817 |
| 2010's | 9 (45.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (28)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| emetine | Homo sapiens (human) | MIC | 0.3000 | 1 | 1 |
Development of 1-aryl-3-furanyl/thienyl-imidazopyridine templates for inhibitors against hypoxia inducible factor (HIF)-1 transcriptional activity.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 26, Issue:24, 2016
Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 23, Issue:8, 2015
Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 18, Issue:12, 2008
(Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.Journal of natural products, , Sep-28, Volume: 75, Issue:9, 2012
Structures and mechanisms of antitumor agents: xestoquinones uncouple cellular respiration and disrupt HIF signaling in human breast tumor cells.Journal of natural products, , Sep-28, Volume: 75, Issue:9, 2012
Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species.Journal of natural products, , Volume: 72, Issue:1, 2009
Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.Journal of natural products, , Volume: 70, Issue:7, 2007
Structure-activity relationship of 2,2-dimethyl-2H-chromene based arylsulfonamide analogs of 3,4-dimethoxy-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]-N-phenylbenzenesulfonamide, a novel small molecule hypoxia inducible factor-1 (HIF-1) pathway inhibitor andBioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
Enables
This protein enables 8 target(s):
| Target | Category | Definition |
|---|
| 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 coactivator binding | molecular function | Binding to a transcription coactivator, a protein involved in positive regulation of transcription via protein-protein interactions with transcription factors and other proteins that positively regulate transcription. Transcription coactivators do not bind DNA directly, but rather mediate protein-protein interactions between activating transcription factors and the basal transcription machinery. [GOC:krc] |
| DNA-binding transcription activator activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that activates or increases transcription of specific gene sets transcribed by RNA polymerase II. [GOC:aruk, GOC:txnOH-2018, PMID:20737563, PMID:27145859] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
| RNA polymerase II-specific DNA-binding transcription factor binding | molecular function | Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw] |
| 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] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| 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] |
| nuclear speck | cellular component | A discrete extra-nucleolar subnuclear domain, 20-50 in number, in which splicing factors are seen to be localized by immunofluorescence microscopy. [http://www.cellnucleus.com/] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
| 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] |
Involved In
This protein is involved in 21 target(s):
| Target | Category | Definition |
|---|
| angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
| embryonic placenta development | biological process | The embryonically driven process whose specific outcome is the progression of the placenta over time, from its formation to the mature structure. The placenta is an organ of metabolic interchange between fetus and mother, partly of embryonic origin and partly of maternal origin. [GOC:add, ISBN:068340007X] |
| blood vessel remodeling | biological process | The reorganization or renovation of existing blood vessels. [GOC:hjd] |
| regulation of heart rate | biological process | Any process that modulates the frequency or rate of heart contraction. [GOC:dph, GOC:tb, PMID:10358008] |
| epithelial cell maturation | biological process | The developmental process, independent of morphogenetic (shape) change, that is required for an epithelial cell to attain its fully functional state. An epithelial cell is a cell usually found in a two-dimensional sheet with a free surface. [GOC:dph] |
| response to oxidative stress | 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 oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, e.g. superoxide anions, hydrogen peroxide (H2O2), and hydroxyl radicals. [GOC:jl, PMID:12115731] |
| mitochondrion organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a mitochondrion; includes mitochondrial morphogenesis and distribution, and replication of the mitochondrial genome as well as synthesis of new mitochondrial components. [GOC:dph, GOC:jl, GOC:mah, GOC:sgd_curators, PMID:9786946] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| visual perception | biological process | The series of events required for an organism to receive a visual stimulus, convert it to a molecular signal, and recognize and characterize the signal. Visual stimuli are detected in the form of photons and are processed to form an image. [GOC:ai] |
| erythrocyte differentiation | biological process | The process in which a myeloid precursor cell acquires specializes features of an erythrocyte. [GOC:mah] |
| lung development | biological process | The process whose specific outcome is the progression of the lung over time, from its formation to the mature structure. In all air-breathing vertebrates the lungs are developed from the ventral wall of the oesophagus as a pouch which divides into two sacs. In amphibians and many reptiles the lungs retain very nearly this primitive sac-like character, but in the higher forms the connection with the esophagus becomes elongated into the windpipe and the inner walls of the sacs become more and more divided, until, in the mammals, the air spaces become minutely divided into tubes ending in small air cells, in the walls of which the blood circulates in a fine network of capillaries. In mammals the lungs are more or less divided into lobes, and each lung occupies a separate cavity in the thorax. [GOC:jid, UBERON:0002048] |
| norepinephrine metabolic process | biological process | The chemical reactions and pathways involving norepinephrine, a hormone secreted by the adrenal medulla, and a neurotransmitter in the sympathetic peripheral nervous system and in some tracts in the central nervous system. It is also the demethylated biosynthetic precursor of epinephrine. [GOC:jl, ISBN:0198506732] |
| 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] |
| surfactant homeostasis | biological process | Any process involved in the maintenance of a steady-state level of a surface-active agent that maintains the surface tension of a liquid. [PMID:23708874, PMID:9751757] |
| 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] |
| myoblast fate commitment | biological process | The process in which the developmental fate of a cell becomes restricted such that it will develop into a myoblast. A myoblast is a mononucleate cell type that, by fusion with other myoblasts, gives rise to the myotubes that eventually develop into skeletal muscle fibers. [CL:0000056, GOC:dph, GOC:mtg_muscle] |
| multicellular organismal-level iron ion homeostasis | biological process | A chemical homeostatic process involved in the maintenance of a steady state level of iron within extracellular body fluids, such as blood, xylem or phloem, of a multicellular organism. This is distinct from maintenance of cellular homeostasis, which occurs within a cell. [PMID:31431773] |
| cellular response to hypoxia | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
| positive regulation of cold-induced thermogenesis | biological process | Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809] |
| regulation of protein neddylation | biological process | Any process that modulates the frequency, rate or extent of protein neddylation. [GOC:obol] |
| regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |