General Information of Drug Therapeutic Target (DTT) (ID: TTWPA54)

DTT Name HIF2-alpha messenger RNA (EPAS1 mRNA)
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
Gene Name EPAS1
DTT Type
Clinical trial target
[1]
BioChemical Class
mRNA target
UniProt ID
EPAS1_HUMAN
TTD ID
T41003
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTADKEKKRSSSERRKEKSRDAARCRRSKETEVFYELAHELPLPHSVSSHLDKASIMRLA
ISFLRTHKLLSSVCSENESEAEADQQMDNLYLKALEGFIAVVTQDGDMIFLSENISKFMG
LTQVELTGHSIFDFTHPCDHEEIRENLSLKNGSGFGKKSKDMSTERDFFMRMKCTVTNRG
RTVNLKSATWKVLHCTGQVKVYNNCPPHNSLCGYKEPLLSCLIIMCEPIQHPSHMDIPLD
SKTFLSRHSMDMKFTYCDDRITELIGYHPEELLGRSAYEFYHALDSENMTKSHQNLCTKG
QVVSGQYRMLAKHGGYVWLETQGTVIYNPRNLQPQCIMCVNYVLSEIEKNDVVFSMDQTE
SLFKPHLMAMNSIFDSSGKGAVSEKSNFLFTKLKEEPEELAQLAPTPGDAIISLDFGNQN
FEESSAYGKAILPPSQPWATELRSHSTQSEAGSLPAFTVPQAAAPGSTTPSATSSSSSCS
TPNSPEDYYTSLDNDLKIEVIEKLFAMDTEAKDQCSTQTDFNELDLETLAPYIPMDGEDF
QLSPICPEERLLAENPQSTPQHCFSAMTNIFQPLAPVAPHSPFLLDKFQQQLESKKTEPE
HRPMSSIFFDAGSKASLPPCCGQASTPLSSMGGRSNTQWPPDPPLHFGPTKWAVGDQRTE
FLGAAPLGPPVSPPHVSTFKTRSAKGFGARGPDVLSPAMVALSNKLKLKRQLEYEEQAFQ
DLSGGDPPGGSTSHLMWKRMKNLRGGSCPLMPDKPLSANVPNDKFTQNPMRGLGHPLRHL
PLPQPPSAISPGENSKSRFPPQCYATQYQDYSLSSAHKVSGMASRLLGPSFESYLLPELT
RYDCEVNVPVLGSSTLLQGGDLLRALDQAT
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).
KEGG Pathway
Pathways in cancer (hsa05200 )
Renal cell carcinoma (hsa05211 )
Reactome Pathway
Oxygen-dependent proline hydroxylation of Hypoxia-inducible Factor Alpha (R-HSA-1234176 )
Transcriptional regulation of pluripotent stem cells (R-HSA-452723 )
Regulation of gene expression by Hypoxia-inducible Factor (R-HSA-1234158 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
2 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PT2385 DMCSN69 Recurrent glioblastoma 2A00.00 Phase 2 [1]
ARO-HIF2 DMV5PEK Renal cell carcinoma 2C90 Phase 1 [2]
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5 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ISIS 222001 DMD7HA3 Discovery agent N.A. Investigative [3]
ISIS 222035 DMQY2EA Discovery agent N.A. Investigative [3]
ISIS 222039 DMVL1SN Discovery agent N.A. Investigative [3]
ISIS 222041 DMS03TR Discovery agent N.A. Investigative [3]
ISIS 222043 DM26M7E Discovery agent N.A. Investigative [3]
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References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 National Cancer Institute Drug Dictionary (drug name ARO-HIF2).
3 US patent application no. 7,217,572, Modulation of HIF1.alpha. and HIF2.alpha. expression.