Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT4O5P0)

• DTT Name: Helodermin-preferring VIP receptor (VIPR2)
• Synonyms: Vasoactive intestinal polypeptide receptor 2; VPAC2; VIPR2; VIP-R-2; Pituitary adenylate cyclase-activating polypeptide typeIII receptor; PACAP-R3; PACAP-R-3; PACAP type III receptor
• Gene Name: VIPR2
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR secretin
• UniProt ID: VIPR2_HUMAN
• TTD ID: T06182
• Sequence:
  MRTLLPPALLTCWLLAPVNSIHPECRFHLEIQEEETKCAELLRSQTEKHKACSGVWDNIT
  CWRPANVGETVTVPCPKVFSNFYSKAGNISKNCTSDGWSETFPDFVDACGYSDPEDESKI
  TFYILVKAIYTLGYSVSLMSLATGSIILCLFRKLHCTRNYIHLNLFLSFILRAISVLVKD
  DVLYSSSGTLHCPDQPSSWVGCKLSLVFLQYCIMANFFWLLVEGLYLHTLLVAMLPPRRC
  FLAYLLIGWGLPTVCIGAWTAARLYLEDTGCWDTNDHSVPWWVIRIPILISIIVNFVLFI
  SIIRILLQKLTSPDVGGNDQSQYKRLAKSTLLLIPLFGVHYMVFAVFPISISSKYQILFE
  LCLGSFQGLVVAVLYCFLNSEVQCELKRKWRSRCPTPSASRDYRVCGSSFSRNGSEGALQ
  FHRGSRAQSFLQTETSVI
• Function: This is a receptor for VIP as well as PACAP-38 and -27,the activity of this receptor is mediated by G proteins which activate adenylyl cyclase. Can be coupled to phospholipase C.
• KEGG Pathway:
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway: 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
PB1046	DM8MJ3F	Heart failure	BD10-BD13	Phase 2	[1]
RG-7103	DM2IDQ9	Chronic obstructive pulmonary disease	CA22	Phase 1	[2]

3 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
helodermin	DMIUABO	Discovery agent	N.A.	Investigative	[3]
PACAP-27	DMB26IK	Discovery agent	N.A.	Investigative	[4]
PB-1120	DMX7WU9	Discovery agent	N.A.	Investigative	[5]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Chronic obstructive pulmonary disease	CA23	Lung tissue	1.54E-01	-0.08	-0.4
Chronic obstructive pulmonary disease	CA23	Small airway epithelium	6.31E-01	6.73E-03	0.03

References

• [1] Clinical pipeline report, company report or official report of PhaseBio Pharmaceuticals.
• [2] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027925)
• [3] Analogues of VIP, helodermin, and PACAP discriminate between rat and human VIP1 and VIP2 receptors. Ann N Y Acad Sci. 1998 Dec 11;865:247-52.
• [4] A systematic comparison of intracellular cyclic AMP and calcium signalling highlights complexities in human VPAC/PAC receptor pharmacology. Neuropharmacology. 2006 Nov;51(6):1086-98.
• [5] Company report (PhaseBio)