Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTIY658)

• DTT Name: Corticotropin-releasing factor receptor 2 (CRHR2)
• Synonyms: Corticotropin-releasinghormone receptor 2; CRHR2; CRH2 receptor; CRH-R 2; CRF2; CRF-R 2
• Gene Name: CRHR2
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR secretin
• UniProt ID: CRFR2_HUMAN
• TTD ID: T11011
• Sequence:
  MDAALLHSLLEANCSLALAEELLLDGWGPPLDPEGPYSYCNTTLDQIGTCWPRSAAGALV
  ERPCPEYFNGVKYNTTRNAYRECLENGTWASKINYSQCEPILDDKQRKYDLHYRIALVVN
  YLGHCVSVAALVAAFLLFLALRSIRCLRNVIHWNLITTFILRNVMWFLLQLVDHEVHESN
  EVWCRCITTIFNYFVVTNFFWMFVEGCYLHTAIVMTYSTERLRKCLFLFIGWCIPFPIIV
  AWAIGKLYYENEQCWFGKEPGDLVDYIYQGPIILVLLINFVFLFNIVRILMTKLRASTTS
  ETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDDLSQIMFIYFNSFLQSFQGFFVSVFYC
  FFNGEVRSAVRKRWHRWQDHHSLRVPMARAMSIPTSPTRISFHSIKQTAAV
• Function: This is a receptor for corticotropin releasing factor. Shows high-affinity crf binding. Also binds to urocortin i, ii and iii. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
• KEGG Pathway: Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  G alpha (s) signalling events (R-HSA-418555)
  Class B/2 (Secretin family receptors) (R-HSA-373080)

Molecular Interaction Atlas (MIA) of This DTT

3 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RT-400	DM8DVC9	Acute decompensated heart failure	BD1Z	Phase 2	[2]
Urocortin 2	DM0YO4Q	Congestive heart failure	BD10	Phase 2	[1]
NBI-34041	DM5BQK3	Eating disorder	6B82	Phase 1	[3]

2 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PF-572778	DMZ8HW7	Generalized anxiety disorder	6B00	Terminated	[4]
SC-241	DM7I6VO	Anxiety disorder	6B00-6B0Z	Terminated	[5]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
astressin	DMSFLTK	Discovery agent	N.A.	Investigative	[6]

References

• [1] Evolution of complementary peptide systems: teneurin C-terminal-associated peptides and corticotropin-releasing factor superfamilies. Ann N Y Acad Sci. 2009 Apr;1163:215-20.
• [2] Advances in therapeutic peptides targeting G protein-coupled receptors. Nat Rev Drug Discov. 2020 Jun;19(6):389-413.
• [3] Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36.
• [4] WO patent application no. 2013,1603,15, Genetic predictors of response to treatment with crhr1 antagonists.
• [5] US patent application no. 2015,0094,310, Crhr1 antagonists for use in the treatment of patients having crh overactivity.
• [6] Comparison of an agonist, urocortin, and an antagonist, astressin, as radioligands for characterization of corticotropin-releasing factor receptors. J Pharmacol Exp Ther. 1999 Feb;288(2):729-34.