Target Information
| Target General Information | Top | |||||
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| Target ID |
T98091
(Former ID: TTDI03248)
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| Target Name |
Inflammation-related GPCR EX33 (GPR84)
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| Synonyms |
Inflammation-related G-protein coupled receptor EX33; G-protein coupled receptor 84; EX33
Click to Show/Hide
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| Gene Name |
GPR84
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Idiopathic interstitial pneumonitis [ICD-11: CB03] | |||||
| 2 | Type 2 diabetes mellitus [ICD-11: 5A11] | |||||
| 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.
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| UniProt ID | ||||||
| Sequence |
MWNSSDANFSCYHESVLGYRYVAVSWGVVVAVTGTVGNVLTLLALAIQPKLRTRFNLLIA
NLTLADLLYCTLLQPFSVDTYLHLHWRTGATFCRVFGLLLFASNSVSILTLCLIALGRYL LIAHPKLFPQVFSAKGIVLALVSTWVVGVASFAPLWPIYILVPVVCTCSFDRIRGRPYTT ILMGIYFVLGLSSVGIFYCLIHRQVKRAAQALDQYKLRQASIHSNHVARTDEAMPGRFQE LDSRLASGGPSEGISSEPVSAATTQTLEGDSSEVGDQINSKRAKQMAEKSPPEASAKAQP IKGARRAPDSSSEFGKVTRMCFAVFLCFALSYIPFLLLNILDARVQAPRVVHMLAANLTW LNGCINPVLYAAMNRQFRQAYGSILKRGPRSFHRLH Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T89IFP | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | PBI-4050 | Drug Info | Phase 2 | Idiopathic pulmonary fibrosis | [2] | |
| 2 | SHR0534 | Drug Info | Phase 1 | Type 2 diabetes | [3] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Antagonist | [+] 1 Antagonist drugs | + | ||||
| 1 | PBI-4050 | Drug Info | [4] | |||
| Agonist | [+] 7 Agonist drugs | + | ||||
| 1 | SHR0534 | Drug Info | [5] | |||
| 2 | 2-hydroxy capric acid | Drug Info | [6] | |||
| 3 | 2-hydroxylauric acid | Drug Info | [6] | |||
| 4 | 3-hydroxy capric acid | Drug Info | [6] | |||
| 5 | 3-hydroxylauric acid | Drug Info | [6] | |||
| 6 | 6-n-octylaminouracil | Drug Info | [6] | |||
| 7 | undecanoic acid | Drug Info | [1] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | Medium-chain fatty acids as ligands for orphan G protein-coupled receptor GPR84. J Biol Chem. 2006 Nov 10;281(45):34457-64. | |||||
| REF 2 | Clinical pipeline report, company report or official report of Liminal BioSciences. | |||||
| REF 3 | ClinicalTrials.gov (NCT03006159) A Phase 1, Randomized, Placebo-controlled, Multiple Dose Escalation Study to Investigate Safety, Pharmacokinetics, and Pharmacodynamics of SHR0534 in Chinese Type 2 Diabetic Patients. U.S. National Institutes of Health. | |||||
| REF 4 | Phase 2 clinical trial of PBI-4050 in patients with idiopathic pulmonary fibrosis. Eur Respir J. 2019 Mar 18;53(3):1800663. | |||||
| REF 5 | Targeting metabolic dysregulation for fibrosis therapy. Nat Rev Drug Discov. 2020 Jan;19(1):57-75. | |||||
| REF 6 | Medium-chain fatty acid-sensing receptor, GPR84, is a proinflammatory receptor. J Biol Chem. 2013 Apr 12;288(15):10684-91. | |||||
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