Details of the Drug Therapeutic Target (DTT)

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]
Related Disease	Contraceptive management [ICD-11: QA21]
BioChemical Class	GPCR rhodopsin
UniProt ID	GPER1_HUMAN
TTD ID	T65236
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
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.