Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTQDMX5)

• DTT Name: Prostaglandin D2 receptor 2 (PTGDR2)
• Synonyms: PTGDR2; Chemoattractant receptor-homologous molecule expressed on Th2 cells; CD294
• Gene Name: PTGDR2
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: PD2R2_HUMAN
• TTD ID: T61722
• Sequence:
  MSANATLKPLCPILEQMSRLQSHSNTSIRYIDHAAVLLHGLASLLGLVENGVILFVVGCR
  MRQTVVTTWVLHLALSDLLASASLPFFTYFLAVGHSWELGTTFCKLHSSIFFLNMFASGF
  LLSAISLDRCLQVVRPVWAQNHRTVAAAHKVCLVLWALAVLNTVPYFVFRDTISRLDGRI
  MCYYNVLLLNPGPDRDATCNSRQVALAVSKFLLAFLVPLAIIASSHAAVSLRLQHRGRRR
  PGRFVRLVAAVVAAFALCWGPYHVFSLLEARAHANPGLRPLVWRGLPFVTSLAFFNSVAN
  PVLYVLTCPDMLRKLRRSLRTVLESVLVDDSELGGAGSSRRRRTSSTARSASPLALCSRP
  EEPRGPARLLGWLLGSCAASPQTGPLNRALSSTSS
• Function: Receptor for prostaglandin D2 (PGD2). Coupled to the G(i)-protein. Receptor activation may result in pertussis toxin- sensitive decreases in cAMP levels and Ca(2+) mobilization. PI3K signaling is also implicated in mediating PTGDR2 effects. PGD2 induced receptor internalization. CRTH2 internalization can be regulated by diverse kinases such as, PKC, PKA, ADRBK1/GRK2, GPRK5/GRK5 and GRK6. Receptoractivation is responsible, at least in part, in immune regulation and allergic/inflammation responses.
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Prostanoid ligand receptors (R-HSA-391908)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[1]

16 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fevipiprant	DM4NX0C	Asthma	CA23	Phase 3	[2]
Setipiprant	DMZ61IA	Asthma	CA23	Phase 3	[3]
Ramatroban	DMB8UQ3	Perennial allergic rhinitis	CA08.03	Phase 2/3	[4]
ADC-3680	DM8GHIX	Allergic rhinitis	CA08.0	Phase 2	[5]
AMG 853	DM973N4	Asthma	CA23	Phase 2	[6]
AP-761	DMISQOZ	Asthma	CA23	Phase 2	[7]
ARRY-502	DM17469	Allergic asthma	CA23.0	Phase 2	[8]
AZD1981	DMMCL9F	Chronic obstructive pulmonary disease	CA22	Phase 2	[9]
BBI-5000	DMR59I4	Alopecia	ED70	Phase 2	[10]
GB001	DM58TGA	Asthma	CA23	Phase 2	[11]
OC-000459	DM1JBD8	Allergy	4A80-4A85	Phase 2	[12]
QAV-680	DMIZYV1	Allergic rhinitis	CA08.0	Phase 2	[13]
AM-211	DMVXRYC	Asthma	CA23	Phase 1	[14]
AM-461	DM7Z8NP	Respiratory disease	CB40	Phase 1	[15]
MK-7246	DMLQOF1	Respiratory disease	CB40	Phase 1	[16]
PGF2alpha	DM4XAU7	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[17]

3 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AZD5985	DMCAKMV	Chronic obstructive pulmonary disease	CA22	Discontinued in Phase 1	[9]
AZD8075	DMKF9U3	Chronic obstructive pulmonary disease	CA22	Discontinued in Phase 1	[9]
RG-7185	DM12VHC	Asthma	CA23	Discontinued in Phase 1	[18]

38 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
13,14-dihydro-15-keto-PGD2	DMZVWCG	Discovery agent	N.A.	Investigative	[4]
13,14-dihydro-15-keto-PGF2alpha	DMNT1XI	Discovery agent	N.A.	Investigative	[19]
15(R)-15-methyl-PGD2	DMY9ZT8	Discovery agent	N.A.	Investigative	[4]
15(S)-15-methyl-PGD2	DMG273T	Discovery agent	N.A.	Investigative	[19]
15-deoxy-Delta12,14-PGD2	DMJ27QT	Discovery agent	N.A.	Investigative	[17]
15-deoxy-Delta12,14-PGJ2	DMNDECA	Discovery agent	N.A.	Investigative	[17]
2-(2,4-diphenylthiazol-5-yl)acetic acid	DMG49N2	Discovery agent	N.A.	Investigative	[20]
2-(2-acetyl-4-bromophenoxy)acetic acid	DMITKZY	Discovery agent	N.A.	Investigative	[21]
2-(2-allyl-4-chlorophenoxy)acetic acid	DMXDGEF	Discovery agent	N.A.	Investigative	[22]
2-(2-benzhydryl-4-phenylthiazol-5-yl)acetic acid	DMN6IV2	Discovery agent	N.A.	Investigative	[23]
2-(2-benzoyl-4-bromophenoxy)acetic acid	DMLOD2Y	Discovery agent	N.A.	Investigative	[21]
2-(2-cyclohexyl-4-fluorophenoxy)acetic acid	DMUN2CS	Discovery agent	N.A.	Investigative	[22]
2-(2-cyclohexyl-4-methoxyphenoxy)acetic acid	DMSI07M	Discovery agent	N.A.	Investigative	[22]
2-(2-cyclohexyl-4-methylphenoxy)acetic acid	DMVCY42	Discovery agent	N.A.	Investigative	[22]
2-(2-cyclohexylphenoxy)acetic acid	DM81WJK	Discovery agent	N.A.	Investigative	[22]
2-(2-formylphenoxy)acetic acid	DMMEBH3	Discovery agent	N.A.	Investigative	[21]
2-(4-bromo-2-(hydroxymethyl)phenoxy)acetic acid	DM7QK5C	Discovery agent	N.A.	Investigative	[21]
2-(4-bromo-2-cyclohexylphenoxy)acetic acid	DM6I1NQ	Discovery agent	N.A.	Investigative	[22]
2-(4-bromo-2-formylphenoxy)acetic acid	DMQVUZP	Discovery agent	N.A.	Investigative	[21]
2-(4-bromo-2-tert-butylphenoxy)acetic acid	DMXAQZ0	Discovery agent	N.A.	Investigative	[21]
2-(4-chloro-2-cycloheptylphenoxy)acetic acid	DM15YM7	Discovery agent	N.A.	Investigative	[24]
2-(4-chloro-2-cyclohexylphenoxy)acetic acid	DMGYZ8D	Discovery agent	N.A.	Investigative	[22]
2-(4-chloro-2-cyclopentylphenoxy)acetic acid	DMA6KQU	Discovery agent	N.A.	Investigative	[22]
2-(4-cyano-2-cyclohexylphenoxy)acetic acid	DM4XFJI	Discovery agent	N.A.	Investigative	[22]
3-(4-chloro-2-cyclohexylphenoxy)propanoic acid	DMQ2D09	Discovery agent	N.A.	Investigative	[22]
4-(4-chloro-2-cyclohexylphenoxy)butanoic acid	DM14I6C	Discovery agent	N.A.	Investigative	[22]
ADC-9971	DMY6PMJ	Allergic rhinitis	CA08.0	Investigative	[25]
AM-156	DMGCOQF	Allergic rhinitis	CA08.0	Investigative	[25]
CAY 10471	DM4O69H	Allergy	4A80-4A85	Investigative	[26]
Delta12-PGJ2	DMB6ADI	Discovery agent	N.A.	Investigative	[19]
IW-1221	DMBTWF0	Asthma	CA23	Investigative	[25]
L-888,291	DMMAIQ2	Discovery agent	N.A.	Investigative	[27]
L-888607	DMJCTWO	Discovery agent	N.A.	Investigative	[28]
Methyl 2-(4-chloro-2-cyclohexylphenoxy)acetate	DMA82IQ	Discovery agent	N.A.	Investigative	[22]
PGD2	DMYDW6J	Discovery agent	N.A.	Investigative	[4]
PGD3	DMWNCLJ	Discovery agent	N.A.	Investigative	[17]
PGJ2	DMR2LTC	Discovery agent	N.A.	Investigative	[19]
U46619	DM13FX4	Discovery agent	N.A.	Investigative	[19]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Asthma	CA23	Nasal and bronchial airway	6.11E-02	-0.15	-0.25
Chronic obstructive pulmonary disease	CA23	Lung tissue	8.36E-01	9.06E-03	0.05
Chronic obstructive pulmonary disease	CA23	Small airway epithelium	1.13E-03	0.14	0.78

References

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