Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT2O4W9)

• DTT Name: Luteinizing hormone receptor (LHCGR)
• Synonyms: Luteinizing hormone-releasing hormone receptor; LSH-R; LHRH receptor; LHCGR; LH/CG-R
• Gene Name: LHCGR
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: LSHR_HUMAN
• TTD ID: T79473
• Sequence:
  MKQRFSALQLLKLLLLLQPPLPRALREALCPEPCNCVPDGALRCPGPTAGLTRLSLAYLP
  VKVIPSQAFRGLNEVIKIEISQIDSLERIEANAFDNLLNLSEILIQNTKNLRYIEPGAFI
  NLPRLKYLSICNTGIRKFPDVTKVFSSESNFILEICDNLHITTIPGNAFQGMNNESVTLK
  LYGNGFEEVQSHAFNGTTLTSLELKENVHLEKMHNGAFRGATGPKTLDISSTKLQALPSY
  GLESIQRLIATSSYSLKKLPSRETFVNLLEATLTYPSHCCAFRNLPTKEQNFSHSISENF
  SKQCESTVRKVNNKTLYSSMLAESELSGWDYEYGFCLPKTPRCAPEPDAFNPCEDIMGYD
  FLRVLIWLINILAIMGNMTVLFVLLTSRYKLTVPRFLMCNLSFADFCMGLYLLLIASVDS
  QTKGQYYNHAIDWQTGSGCSTAGFFTVFASELSVYTLTVITLERWHTITYAIHLDQKLRL
  RHAILIMLGGWLFSSLIAMLPLVGVSNYMKVSICFPMDVETTLSQVYILTILILNVVAFF
  IICACYIKIYFAVRNPELMATNKDTKIAKKMAILIFTDFTCMAPISFFAISAAFKVPLIT
  VTNSKVLLVLFYPINSCANPFLYAIFTKTFQRDFFLLLSKFGCCKRRAELYRRKDFSAYT
  SNCKNGFTGSNKPSQSTLKLSTLHCQGTALLDKTRYTEC
• Function: Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Ovarian steroidogenesis (hsa04913)
  Prolactin signaling pathway (hsa04917)
• Reactome Pathway:
  G alpha (s) signalling events (R-HSA-418555)
  Hormone ligand-binding receptors (R-HSA-375281)

Molecular Interaction Atlas (MIA) of This DTT

3 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Choriogonadotropin alfa	DMFMZ3G	Female infertility	GA31.Z	Approved	[2]
Chorionic Gonadotropin	DMFT73E	Fertility disorders	5A61	Approved	[2]
Lutropin alfa	DM7K5GD	Female infertility	GA31.Z	Approved	[1]

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ML-04	DMQSO4L	Myelodysplastic syndrome	2A37	Phase 2	[3]
Org-43902	DME0WX2	Infertility	GB04	Phase 1	[4]

2 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LDI-200	DMKMTR7	leukaemia	2A60-2B33	Discontinued in Phase 3	[5]
Human chorionic gonadotropin	DMA7EFM	Heart disease	BA41-BA42	Terminated	[5]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
EP-200	DMAURX5	Solid tumour/cancer	2A00-2F9Z	Investigative	[5]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Acute myelocytic leukaemia	2C82	Bone marrow	3.55E-01	5.41E-04	4.54E-03
Myelodysplastic syndrome	2C82	Bone marrow	6.04E-01	0.06	0.34
Breast cancer	2C82	Breast tissue	1.48E-21	-0.27	-0.25

References

• [1] Lutropin alfa. Drugs. 2008;68(11):1529-40.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [3] Evaluation of radiolabeled ML04, a putative irreversible inhibitor of epidermal growth factor receptor, as a bioprobe for PET imaging of EGFR-overexpressing tumors. Nucl Med Biol. 2007 Jan;34(1):55-70.
• [4] First evidence of ovulation induced by oral LH agonists in healthy female volunteers of reproductive age. J Clin Endocrinol Metab. 2013 Apr;98(4):1558-66.
• [5] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 254).