General Information of Drug Therapeutic Target (DTT) (ID: TTDSB34)

DTT Name G-protein coupled estrogen receptor 1 (GPER1)
Synonyms
Membrane estrogen receptor; Lymphocyte-derived G-protein coupled receptor; LYGPR; IL8-related receptor DRY12; GPER1; GPER; GPCR-BR; G-protein coupled receptor 30; Flow-induced endothelial G-protein coupled receptor 1; FEG-1; Chemoattractant receptor-like 2
Gene Name GPER1
DTT Type
Successful target
[1]
BioChemical Class
GPCR rhodopsin
UniProt ID
GPER1_HUMAN
TTD ID
T65236
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDVTSQARGVGLEMYPGTAQPAAPNTTSPELNLSHPLLGTALANGTGELSEHQQYVIGLF
LSCLYTIFLFPIGFVGNILILVVNISFREKMTIPDLYFINLAVADLILVADSLIEVFNLH
ERYYDIAVLCTFMSLFLQVNMYSSVFFLTWMSFDRYIALARAMRCSLFRTKHHARLSCGL
IWMASVSATLVPFTAVHLQHTDEACFCFADVREVQWLEVTLGFIVPFAIIGLCYSLIVRV
LVRAHRHRGLRPRRQKALRMILAVVLVFFVCWLPENVFISVHLLQRTQPGAAPCKQSFRH
AHPLTGHIVNLAAFSNSCLNPLIYSFLGETFRDKLRLYIEQKTNLPALNRFCHAALKAVI
PDSTEQSDVRFSSAV
Function Receptor for estrogen. .
KEGG Pathway
Endocrine resistance (hsa01522 )
Estrogen signaling pathway (hsa04915 )
GnRH secretion (hsa04929 )
Reactome Pathway
G alpha (i) signalling events (R-HSA-418594 )
Peptide ligand-binding receptors (R-HSA-375276 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Segesterone acetate; ethinyl estradiol DMFEGB0 Contraception QA21 Approved [1]
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1 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
G1 DMTV42K Lymphoma 2A80-2A86 Phase 1/2 [2]
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2 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
G15 DMMEC9D Discovery agent N.A. Investigative [3]
G36 DMDJCIP Discovery agent N.A. Investigative [4]
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References

1 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
2 Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat Chem Biol. 2006 Apr;2(4):207-12.
3 In vivo effects of a GPR30 antagonist. Nat Chem Biol. 2009 Jun;5(6):421-7.
4 Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J Steroid Biochem Mol Biol. 2011 Nov;127(3-5):358-66.