General Information of the Protein
Protein ID |
PT02791
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Protein Name |
Hypoxia-inducible factor 1-alpha
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Secondarily Protein Name |
ARNT-interacting protein
Basic-helix-loop-helix-PAS protein MOP1
Class E basic helix-loop-helix protein 78
Member of PAS protein 1
PAS domain-containing protein 8
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Gene Name |
HIF1A
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Secondarily Gene Name |
BHLHE78
MOP1
PASD8
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Sequence |
MEGAGGANDKKKISSERRKEKSRDAARSRRSKESEVFYELAHQLPLPHNVSSHLDKASVMRLTISYLRVRKLLDAGDLDIEDDMKAQMNCFYLKALDGFVMVLTDDGDMIYISDNVNKYMGLTQFELTGHSVFDFTHPCDHEEMREMLTHRNGLVKKGKEQNTQRSFFLRMKCTLTSRGRTMNIKSATWKVLHCTGHIHVYDTNSNQPQCGYKKPPMTCLVLICEPIPHPSNIEIPLDSKTFLSRHSLDMKFSYCDERITELMGYEPEELLGRSIYEYYHALDSDHLTKTHHDMFTKGQVTTGQYRMLAKRGGYVWVETQATVIYNTKNSQPQCIVCVNYVVSGIIQHDLIFSLQQTECVLKPVESSDMKMTQLFTKVESEDTSSLFDKLKKEPDALTLLAPAAGDTIISLDFGSNDTETDDQQLEEVPLYNDVMLPSPNEKLQNINLAMSPLPTAETPKPLRSSADPALNQEVALKLEPNPESLELSFTMPQIQDQTPSPSDGSTRQSSPEPNSPSEYCFYVDSDMVNEFKLELVEKLFAEDTEAKNPFSTQDTDLDLEMLAPYIPMDDDFQLRSFDQLSPLESSSASPESASPQSTVTVFQQTQIQEPTANATTTTATTDELKTVTKDRMEDIKILIASPSPTHIHKETTSATSSPYRDTQSRTASPNRAGKGVIEQTEKSHPRSPNVLSVALSQRTTVPEEELNPKILALQNAQRKRKMEHDGSLFQAVGIGTLLQQPDDHAATTSLSWKRVKGCKSSEQNGMEQKTIILIPSDLACRLLGQSMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN
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Organism |
Homo sapiens, Human
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Protein Classification |
Transcription factor
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Function |
Functions as a master transcriptional regulator of the adaptive response to hypoxia (PubMed:11292861, PubMed:11566883, PubMed:15465032, PubMed:16973622, PubMed:17610843, PubMed:18658046, PubMed:20624928, PubMed:22009797, PubMed:9887100, PubMed:30125331). Under hypoxic conditions, activates the transcription of over 40 genes, including erythropoietin, glucose transporters, glycolytic enzymes, vascular endothelial growth factor, HILPDA, and other genes whose protein products increase oxygen delivery or facilitate metabolic adaptation to hypoxia (PubMed:11292861, PubMed:11566883, PubMed:15465032, PubMed:16973622, PubMed:17610843, PubMed:20624928, PubMed:22009797, PubMed:9887100, PubMed:30125331). Plays an essential role in embryonic vascularization, tumor angiogenesis and pathophysiology of ischemic disease (PubMed:22009797). Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Activation requires recruitment of transcriptional coactivators such as CREBBP and EP300 (PubMed:9887100, PubMed:16543236). Activity is enhanced by interaction with NCOA1 and/or NCOA2 (PubMed:10594042). Interaction with redox regulatory protein APEX1 seems to activate CTAD and potentiates activation by NCOA1 and CREBBP (PubMed:10202154, PubMed:10594042). Involved in the axonal distribution and transport of mitochondria in neurons during hypoxia (PubMed:19528298).
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Uniprot ID |
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Subcellular Location |
Cytoplasm
Nucleus
Nucleus speckle
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Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity |
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Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000275 , AGS
Cell Line ID: CL000067 , HCT 116
Cell Line ID: CL000025 , HEK-293T
Cell Line ID: CL000006 , HEK293
Cell Line ID: CL000017 , HeLa
Cell Line ID: CL000273 , Hep 3B2.1-7
Cell Line ID: CL000083 , MCF-7
Cell Line ID: CL000655 , ME-180
Cell Line ID: CL000274 , SK-HEP-1
Cell Line ID: CL000118 , U-251MG
Cell Line ID: CL000043 , U2OS
Biochemical Assays
Clinical Information about the Protein
Target 1 ( HIF1-alpha messenger RNA (HIF1A mRNA) )
Target Type | Clinical trial Target | ||||
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Disease | 1 Target-related Disease | 1 | |||
1 | Recurrent glioblastoma [ICD-11: 2A00.00] | ||||
Clinical Trial Drug(s) | 1 Clinical Trial Drug | 1 | |||
1 | PT2385 | Phase 2 |
Target 2 ( Hypoxia-inducible factor 1 alpha (HIF-1A) )
Target Type | Clinical trial Target | ||||
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Disease | 3 Target-related Diseases | 3 | |||
1 | Lymphoma [ICD-11: 2A80-2A86] | ||||
2 | Pulmonary arterial hypertension [ICD-11: BB01.0] | ||||
3 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | ||||
Approved Drug(s) | 1 Approved Drug | 1 | |||
1 | HIF-1alpha | Phase 4 | |||
Clinical Trial Drug(s) | 2 Clinical Trial Drugs | 2 | |||
1 | 2-Methoxyestradiol | Phase 2 | |||
2 | PX-478 | Phase 1 |