Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T51748
(Former ID: TTDR01416)
|
|||||
Target Name |
HIF1-alpha messenger RNA (HIF1A mRNA)
|
|||||
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)
Click to Show/Hide
|
|||||
Gene Name |
HIF1A
|
|||||
Target Type |
Clinical trial target
|
[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Adrenomedullary hyperfunction [ICD-11: 5A75] | |||||
2 | Brain cancer [ICD-11: 2A00] | |||||
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.
Click to Show/Hide
|
|||||
BioChemical Class |
mRNA target
|
|||||
UniProt ID | ||||||
Sequence |
MEGAGGANDKKKISSERRKEKSRDAARSRRSKESEVFYELAHQLPLPHNVSSHLDKASVM
RLTISYLRVRKLLDAGDLDIEDDMKAQMNCFYLKALDGFVMVLTDDGDMIYISDNVNKYM GLTQFELTGHSVFDFTHPCDHEEMREMLTHRNGLVKKGKEQNTQRSFFLRMKCTLTSRGR TMNIKSATWKVLHCTGHIHVYDTNSNQPQCGYKKPPMTCLVLICEPIPHPSNIEIPLDSK TFLSRHSLDMKFSYCDERITELMGYEPEELLGRSIYEYYHALDSDHLTKTHHDMFTKGQV TTGQYRMLAKRGGYVWVETQATVIYNTKNSQPQCIVCVNYVVSGIIQHDLIFSLQQTECV LKPVESSDMKMTQLFTKVESEDTSSLFDKLKKEPDALTLLAPAAGDTIISLDFGSNDTET DDQQLEEVPLYNDVMLPSPNEKLQNINLAMSPLPTAETPKPLRSSADPALNQEVALKLEP NPESLELSFTMPQIQDQTPSPSDGSTRQSSPEPNSPSEYCFYVDSDMVNEFKLELVEKLF AEDTEAKNPFSTQDTDLDLEMLAPYIPMDDDFQLRSFDQLSPLESSSASPESASPQSTVT VFQQTQIQEPTANATTTTATTDELKTVTKDRMEDIKILIASPSPTHIHKETTSATSSPYR DTQSRTASPNRAGKGVIEQTEKSHPRSPNVLSVALSQRTTVPEEELNPKILALQNAQRKR KMEHDGSLFQAVGIGTLLQQPDDHAATTSLSWKRVKGCKSSEQNGMEQKTIILIPSDLAC RLLGQSMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN Click to Show/Hide
|
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
1 | PT2385 | Drug Info | Phase 2 | Recurrent glioblastoma | [1], [2] | |
Mode of Action | [+] 1 Modes of Action | + | ||||
Inhibitor | [+] 2 Inhibitor drugs | + | ||||
1 | PT2385 | Drug Info | [1] | |||
2 | (5-(1-benzyl-1H-indazol-3-yl)furan-2-yl)methanol | Drug Info | [3] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
Co-Targets | Top | |||||
---|---|---|---|---|---|---|
Co-Targets |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 2 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 3 | Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6305-10. | |||||
REF 4 | US patent application no. 7,217,572, Modulation of HIF1.alpha. and HIF2.alpha. expression. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.