TARGETID

T51748

FORMERID

TTDR01416

UNIPROID

HIF1A_HUMAN

TARGNAME

HIF1-alpha messenger RNA (HIF1A mRNA)

GENENAME

HIF1A

TARGTYPE

Clinical trial target

SYNONYMS

bHLHe78 (mRNA); Transcription factor HIF-1 (mRNA); PASD8 (mRNA); PAS domain-containing protein 8 (mRNA); Member of PAS protein 1 (mRNA); MOP1 (mRNA); Hypoxia-inducible transcription factor (HIF)-1 (mRNA); Hypoxia-inducible factor 1-alpha (mRNA); Hypoxia-inducible factor 1 (mRNA); Hypoxia inducible factor 1 (mRNA); HIF1-alpha (mRNA); HIF1 alpha (mRNA); HIF-1alpha (mRNA); HIF-1-alpha (mRNA); HIF-1 alpha (mRNA); Class E basic helix-loop-helix protein 78 (mRNA); Basic-helix-loop-helix-PAS protein MOP1 (mRNA); ARNT-interacting protein (mRNA); ARNT interacting protein (mRNA)

FUNCTION

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. Plays an essential role in embryonic vascularization, tumor angiogenesis and pathophysiology of ischemic disease. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters. Activation requires recruitment of transcriptional coactivators such as CREBBP and EP300. Activity is enhanced by interaction with both, NCOA1 or NCOA2. Interaction with redox regulatory protein APEX seems to activate CTAD and potentiates activation by NCOA1 and CREBBP. Involved in the axonal distribution and transport of mitochondria in neurons during hypoxia. Functions as a master transcriptional regulator of the adaptive response to hypoxia.

PDBSTRUC

6GMR; 6GFX; 5LAS; 5LA9; 5L9V

BIOCLASS

mRNA target

SEQUENCE

MEGAGGANDKKKISSERRKEKSRDAARSRRSKESEVFYELAHQLPLPHNVSSHLDKASVMRLTISYLRVRKLLDAGDLDIEDDMKAQMNCFYLKALDGFVMVLTDDGDMIYISDNVNKYMGLTQFELTGHSVFDFTHPCDHEEMREMLTHRNGLVKKGKEQNTQRSFFLRMKCTLTSRGRTMNIKSATWKVLHCTGHIHVYDTNSNQPQCGYKKPPMTCLVLICEPIPHPSNIEIPLDSKTFLSRHSLDMKFSYCDERITELMGYEPEELLGRSIYEYYHALDSDHLTKTHHDMFTKGQVTTGQYRMLAKRGGYVWVETQATVIYNTKNSQPQCIVCVNYVVSGIIQHDLIFSLQQTECVLKPVESSDMKMTQLFTKVESEDTSSLFDKLKKEPDALTLLAPAAGDTIISLDFGSNDTETDDQQLEEVPLYNDVMLPSPNEKLQNINLAMSPLPTAETPKPLRSSADPALNQEVALKLEPNPESLELSFTMPQIQDQTPSPSDGSTRQSSPEPNSPSEYCFYVDSDMVNEFKLELVEKLFAEDTEAKNPFSTQDTDLDLEMLAPYIPMDDDFQLRSFDQLSPLESSSASPESASPQSTVTVFQQTQIQEPTANATTTTATTDELKTVTKDRMEDIKILIASPSPTHIHKETTSATSSPYRDTQSRTASPNRAGKGVIEQTEKSHPRSPNVLSVALSQRTTVPEEELNPKILALQNAQRKRKMEHDGSLFQAVGIGTLLQQPDDHAATTSLSWKRVKGCKSSEQNGMEQKTIILIPSDLACRLLGQSMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN

DRUGINFO

PT2385

DRUGINFO

(5-(1-benzyl-1H-indazol-3-yl)furan-2-yl)methanol

DRUGINFO

ISIS 175510

DRUGINFO

ISIS 298697

DRUGINFO

ISIS 298699

DRUGINFO

ISIS 298700

DRUGINFO

ISIS 298701

DRUGINFO

ISIS 298702

DRUGINFO

ISIS 298711