Target Information
| Target General Information | Top | |||||
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| Target ID |
T41003
(Former ID: TTDR01423)
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| Target Name |
HIF2-alpha messenger RNA (EPAS1 mRNA)
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| Synonyms |
PASD2 mRNA; PAS domain-containing protein 2 mRNA; Member of PAS protein 2 mRNA; MOP2 mRNA; Hypoxia-inducible factor 2-alpha mRNA; HLF mRNA; HIF2A mRNA; HIF2-alpha mRNA; HIF-2-alpha mRNA; HIF-1-alpha-like factor mRNA; Endothelial PAS domain-containing protein 1 mRNA; EPAS-1 mRNA; Class E basic helix-loop-helix protein 73 mRNA; Basic-helix-loop-helix-PAS protein MOP2 mRNA; BHLHE73 mRNA
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| Gene Name |
EPAS1
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Adrenomedullary hyperfunction [ICD-11: 5A75] | |||||
| 2 | Brain cancer [ICD-11: 2A00] | |||||
| 3 | Renal cell carcinoma [ICD-11: 2C90] | |||||
| Function |
Transcription factor involved in the induction of oxygen regulated genes. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Regulates the vascular endothelial growth factor (VEGF) expression and seems to be implicated in the development of blood vessels and the tubular system of lung. May also play a role in the formation of the endothelium that gives rise to the blood brain barrier. Potent activator of the Tie-2 tyrosine kinase expression. Activation requires recruitment of transcriptional coactivators such as CREBBP and probably EP300. Interaction with redox regulatory protein APEX seems to activate CTAD (By similarity).
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| BioChemical Class |
mRNA target
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| UniProt ID | ||||||
| Sequence |
MTADKEKKRSSSERRKEKSRDAARCRRSKETEVFYELAHELPLPHSVSSHLDKASIMRLA
ISFLRTHKLLSSVCSENESEAEADQQMDNLYLKALEGFIAVVTQDGDMIFLSENISKFMG LTQVELTGHSIFDFTHPCDHEEIRENLSLKNGSGFGKKSKDMSTERDFFMRMKCTVTNRG RTVNLKSATWKVLHCTGQVKVYNNCPPHNSLCGYKEPLLSCLIIMCEPIQHPSHMDIPLD SKTFLSRHSMDMKFTYCDDRITELIGYHPEELLGRSAYEFYHALDSENMTKSHQNLCTKG QVVSGQYRMLAKHGGYVWLETQGTVIYNPRNLQPQCIMCVNYVLSEIEKNDVVFSMDQTE SLFKPHLMAMNSIFDSSGKGAVSEKSNFLFTKLKEEPEELAQLAPTPGDAIISLDFGNQN FEESSAYGKAILPPSQPWATELRSHSTQSEAGSLPAFTVPQAAAPGSTTPSATSSSSSCS TPNSPEDYYTSLDNDLKIEVIEKLFAMDTEAKDQCSTQTDFNELDLETLAPYIPMDGEDF QLSPICPEERLLAENPQSTPQHCFSAMTNIFQPLAPVAPHSPFLLDKFQQQLESKKTEPE HRPMSSIFFDAGSKASLPPCCGQASTPLSSMGGRSNTQWPPDPPLHFGPTKWAVGDQRTE FLGAAPLGPPVSPPHVSTFKTRSAKGFGARGPDVLSPAMVALSNKLKLKRQLEYEEQAFQ DLSGGDPPGGSTSHLMWKRMKNLRGGSCPLMPDKPLSANVPNDKFTQNPMRGLGHPLRHL PLPQPPSAISPGENSKSRFPPQCYATQYQDYSLSSAHKVSGMASRLLGPSFESYLLPELT RYDCEVNVPVLGSSTLLQGGDLLRALDQAT Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | PT2385 | Drug Info | Phase 2 | Recurrent glioblastoma | [1], [2] | |
| 2 | ARO-HIF2 | Drug Info | Phase 1 | Renal cell carcinoma | [3] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | PT2385 | Drug Info | [1] | |||
| 2 | ARO-HIF2 | Drug Info | [4] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Pathways in cancer | |||||
| 2 | Renal cell carcinoma | |||||
| NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
| 1 | TCR Signaling Pathway | |||||
| 2 | TGF_beta_Receptor Signaling Pathway | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | HIF-2-alpha transcription factor network | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Regulation of gene expression by Hypoxia-inducible Factor | |||||
| 2 | Oxygen-dependent proline hydroxylation of Hypoxia-inducible Factor Alpha | |||||
| 3 | Transcriptional regulation of pluripotent stem cells | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | Transcriptional regulation of pluripotent stem cells | |||||
| 2 | Regulation of Hypoxia-inducible Factor (HIF) by Oxygen | |||||
| 3 | Adipogenesis | |||||
| References | Top | |||||
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| 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 | ClinicalTrials.gov (NCT04169711) Study of ARO-HIF2 in Patients With Advanced Clear Cell Renal Cell Carcinoma. U.S. National Institutes of Health. | |||||
| REF 4 | National Cancer Institute Drug Dictionary (drug name ARO-HIF2). | |||||
| REF 5 | US patent application no. 7,217,572, Modulation of HIF1.alpha. and HIF2.alpha. expression. | |||||
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