Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTG0MQD)

• DTT Name: Inflammation-related GPCR EX33 (GPR84)
• Synonyms: Inflammation-related G-protein coupled receptor EX33; G-protein coupled receptor 84; EX33
• Gene Name: GPR84
• DTT Type: Clinical trial target; [1]
• UniProt ID: GPR84_HUMAN
• TTD ID: T98091
• Sequence:
  MWNSSDANFSCYHESVLGYRYVAVSWGVVVAVTGTVGNVLTLLALAIQPKLRTRFNLLIA
  NLTLADLLYCTLLQPFSVDTYLHLHWRTGATFCRVFGLLLFASNSVSILTLCLIALGRYL
  LIAHPKLFPQVFSAKGIVLALVSTWVVGVASFAPLWPIYILVPVVCTCSFDRIRGRPYTT
  ILMGIYFVLGLSSVGIFYCLIHRQVKRAAQALDQYKLRQASIHSNHVARTDEAMPGRFQE
  LDSRLASGGPSEGISSEPVSAATTQTLEGDSSEVGDQINSKRAKQMAEKSPPEASAKAQP
  IKGARRAPDSSSEFGKVTRMCFAVFLCFALSYIPFLLLNILDARVQAPRVVHMLAANLTW
  LNGCINPVLYAAMNRQFRQAYGSILKRGPRSFHRLH
• Function: Receptor for medium-chain free fatty acid (FFA) with carbon chain lengths of C9 to C14. Capric acid (C10:0), undecanoic acid (C11:0) and lauric acid (C12:0) are the most potent agonists. Not activated by short-chain and long-chain saturated and unsaturated FFAs. Activation by medium-chain free fatty acid is coupled to a pertussis toxin sensitive G(i/o) protein pathway. May have important roles in processes from fatty acid metabolism to regulation of the immune system.
• Reactome Pathway:
  Neutrophil degranulation (R-HSA-6798695)
  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
PBI-4050	DMPXK27	Idiopathic pulmonary fibrosis	CB03.4	Phase 2	[2]
SHR0534	DMGFTAI	Type 2 diabetes	5A11	Phase 1	[3]

6 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-hydroxy capric acid	DMJAN52	Discovery agent	N.A.	Investigative	[4]
2-hydroxylauric acid	DMCNW3M	Discovery agent	N.A.	Investigative	[4]
3-hydroxy capric acid	DMC70P1	Discovery agent	N.A.	Investigative	[4]
3-hydroxylauric acid	DMNMB6V	Discovery agent	N.A.	Investigative	[4]
6-n-octylaminouracil	DMXJFCQ	Discovery agent	N.A.	Investigative	[4]
undecanoic acid	DMFOIPL	Discovery agent	N.A.	Investigative	[1]

References

• [1] Medium-chain fatty acids as ligands for orphan G protein-coupled receptor GPR84. J Biol Chem. 2006 Nov 10;281(45):34457-64.
• [2] Phase 2 clinical trial of PBI-4050 in patients with idiopathic pulmonary fibrosis. Eur Respir J. 2019 Mar 18;53(3):1800663.
• [3] Targeting metabolic dysregulation for fibrosis therapy. Nat Rev Drug Discov. 2020 Jan;19(1):57-75.
• [4] Medium-chain fatty acid-sensing receptor, GPR84, is a proinflammatory receptor. J Biol Chem. 2013 Apr 12;288(15):10684-91.