Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTMAHD1)

• DTT Name: Relaxin receptor 1 (RXFP1)
• Synonyms: Relaxin family peptide receptor 1; RXFP1; Leucine-rich repeat-containing G-protein coupled receptor 7
• Gene Name: RXFP1
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: RXFP1_HUMAN
• TTD ID: T73696
• Sequence:
  MTSGSVFFYILIFGKYFSHGGGQDVKCSLGYFPCGNITKCLPQLLHCNGVDDCGNQADED
  NCGDNNGWSLQFDKYFASYYKMTSQYPFEAETPECLVGSVPVQCLCQGLELDCDETNLRA
  VPSVSSNVTAMSLQWNLIRKLPPDCFKNYHDLQKLYLQNNKITSISIYAFRGLNSLTKLY
  LSHNRITFLKPGVFEDLHRLEWLIIEDNHLSRISPPTFYGLNSLILLVLMNNVLTRLPDK
  PLCQHMPRLHWLDLEGNHIHNLRNLTFISCSNLTVLVMRKNKINHLNENTFAPLQKLDEL
  DLGSNKIENLPPLIFKDLKELSQLNLSYNPIQKIQANQFDYLVKLKSLSLEGIEISNIQQ
  RMFRPLMNLSHIYFKKFQYCGYAPHVRSCKPNTDGISSLENLLASIIQRVFVWVVSAVTC
  FGNIFVICMRPYIRSENKLYAMSIISLCCADCLMGIYLFVIGGFDLKFRGEYNKHAQLWM
  ESTHCQLVGSLAILSTEVSVLLLTFLTLEKYICIVYPFRCVRPGKCRTITVLILIWITGF
  IVAFIPLSNKEFFKNYYGTNGVCFPLHSEDTESIGAQIYSVAIFLGINLAAFIIIVFSYG
  SMFYSVHQSAITATEIRNQVKKEMILAKRFFFIVFTDALCWIPIFVVKFLSLLQVEIPGT
  ITSWVVIFILPINSALNPILYTLTTRPFKEMIHRFWYNYRQRKSMDSKGQKTYAPSFIWV
  EMWPLQEMPPELMKPDLFTYPCEMSLISQSTRLNSYS
• Function: Receptor for relaxins. The activity of this receptor is mediated by G proteins leading to stimulation of adenylate cyclase and an increase of cAMP. Binding of the ligand may also activate a tyrosine kinase pathway that inhibits the activity of a phosphodiesterase that degrades cAMP.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Relaxin signaling pathway (hsa04926)
• Reactome Pathway:
  Relaxin receptors (R-HSA-444821)
  ADORA2B mediated anti-inflammatory cytokines production (R-HSA-9660821)
  G alpha (s) signalling events (R-HSA-418555)

Molecular Interaction Atlas (MIA) of This DTT

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RLX030	DMXIRA0	Acute heart failure	BD10-BD13	Approval submitted	[1]
AZD5462	DM2QQZO	Cardiovascular disease	BA00-BE2Z	Phase 1	[2]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ML290	DMPOX4Q	Discovery agent	N.A.	Investigative	[3]

References

• [1] Design of the RELAXin in acute heart failure study. Am Heart J. 2012 Feb;163(2):149-55.e1.
• [2] Clinical pipeline report, company report or official report of AstraZeneca
• [3] Discovery, optimization, and biological activity of the first potent and selective small-molecule agonist series of human relaxin receptor 1 (RXFP1). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010.