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Overview of Orphan G Protein-coupled Receptors (oGPCRs)
oGPCRs are receptors that don't have any endogenous ligands. There are now about 140 GPCRs that have not been linked to endogenous ligands. They were discovered by molecular biological investigations and became the foundations of reverse pharmacology, in which receptors are sought to be matched to potential transmitters, resulting in the deorphanization of dozens of oGPCRs.
Fig.1 A schematic illustration of the oGPCRs in the CNS. (Alavi, 2018)
Functions of oGPCRs
Studies have shown that oGPCRs may perform multiple functions in the central nervous system. Furthermore, oGPCRs may have considerable effects on regulating behavioral disorders such as depression and anxiety. Notably, oGPCRs play important roles in the pathophysiology of different disorders, such as epilepsy, schizophrenia, Parkinson's disease, and Alzheimer's disease. Moreover, recent studies have identified oGPCRs as new candidate targets for addressing the deficiencies in pain treatment.
oGPCRs and Their Mechanisms
oGPCRs hold great promise as they can provide novel therapeutic targets with specificity and provide new strategies for drug design. Here, we exemplify common orphan receptors and their associated mechanisms.
Receptor
|
Gene
|
Mechanism
|
Agonists
|
Antagonists
|
GPR3 receptor
|
GPR3
|
-
GPR3 is coupled to Gs protein and can increase the intracellular cAMP.
-
GPR3 signals via ERK1/2 and Akt.
|
-
S1P
-
AF64394
-
Cannabidiol
-
Diphenyleneiodonium chloride
-
Dihydrosphingosine 1-phosphate
|
|
GPR6 receptor
|
GPR6
|
-
GPR6 is capable of stimulating the Gs-cAMP signaling pathway.
-
GPR6 signals via ERK1/2 and sphingosine kinase phosphorylation.
|
-
Cannabidiol
-
IAG
-
CVN424
-
SR141716A
-
SR144528
|
-
Cannabidiol
-
SR144528
-
AM630
|
GPR12 receptor
|
GPR12
|
-
GPR12 can constitutively activate the Gs-cAMP/PKA signaling pathway.
-
GPR12 signals via ERK1/2.
|
|
|
GPR17 receptor
|
GPR17
|
-
GPR17 is phosphorylated by GRKs with consequent recruitment of β-Arrestin.
|
-
PF9 tetrasodium salt
-
MDL29951
-
Asinex 1
-
AC1MLNKK
-
T0510.3657
|
-
Montelukast
-
Cangrelor
-
Pranlukast
-
HAMI3379
|
GPR39 receptor
|
GPR39
|
|
-
Cpd1324
-
TC-G 1008
-
TM N1324
-
LY2784544
-
GSK2636771
|
|
GPR43 receptor
|
GPR43
|
-
GPR43 is coupled to Gq/11 protein.
-
GPR43 regulates the RhoA signaling pathway to activate YAP/TAZ.
|
-
Acetate
-
4-CMTB
-
Propionate
-
Butyrate
|
|
GPR81 receptor
|
GPR81
|
-
GPR81 couples to the Gi signaling pathway.
-
Activated GPR81 could decrease intracellular cAMP levels and PKA activity.
|
|
|
GPR183 receptor
|
GPR183
|
-
GPR183 directly triggers the Gαi protein signaling pathway.
-
GPR183 is coupled to Gi/o proteins, resulting in adenylyl cyclase inhibition and activation of p38 MAPK and ERK signaling pathways.
|
-
7α,25-Dihydroxycholesterol
|
|
Assay List of Orphan Receptors
Creative Biolabs can provide a range of assays of orphan receptors. You can choose the assay in the list or contact us for more information:
GPR183 GPR35 GPR17 GPR84 GPR39 Other Orphan Receptors
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
cAMP Assay
|
S01YF-0722-KX179
|
Magic™ Human GPR183 In Vitro cAMP Assay, SK-N-MC-CRE
|
SK-N-MC-CRE
|
cAMP Assay
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
cAMP Assay
|
S01YF-1122-KX462
|
Magic™ Mouse GPR35 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
Calcium Flux Assay
|
S01YF-1122-KX458
|
Magic™ Human GPR35 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
S01YF-1122-KX461
|
Magic™ Mouse GPR35 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
S01YF-1122-KX463
|
Magic™ Rat GPR35 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
[35S]GTPγS Binding Assay
|
S01YF-1122-KX460
|
Magic™ Human GPR35 In Vitro [35S]GTPγS binding Assay
|
CHO-K1
|
[35S]GTPγS binding Assay
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
cAMP Assay
|
S01YF-1122-KX766
|
Magic™ Human GPR17 (Long Isoform) In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX770
|
Magic™ Human GPR17 (Short Isoform) In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX774
|
Magic™ Mouse GPR17 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX778
|
Magic™ Rat GPR17 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
Calcium Flux Assay
|
S01YF-0722-KX174
|
Magic™ Human GPR17 (long form) In Vitro Calcium Assay, HEK293
|
HEK293
|
Calcium Flux Assay
|
|
S01YF-0722-KX175
|
Magic™ Human GPR17 (short form) In Vitro Calcium Assay, HEK293
|
HEK293
|
Calcium Flux Assay
|
|
S01YF-1122-KX765
|
Magic™ Human GPR17 (Long Isoform) In Vitro Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-1122-KX769
|
Magic™ Human GPR17 (Short Isoform) In Vitro Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-1122-KX773
|
Magic™ Mouse GPR17 In Vitro Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-1122-KX777
|
Magic™ Rat GPR17 In Vitro Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
IP1 Assay
|
S01YF-1122-KX767
|
Magic™ Human GPR17 (Long Isoform) In Vitro IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-1122-KX771
|
Magic™ Human GPR17 (Short Isoform) In Vitro IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-1122-KX775
|
Magic™ Mouse GPR17 In Vitro IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-1122-KX779
|
Magic™ Rat GPR17 In Vitro IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
[35S]GTPγS Binding Assay
|
S01YF-1122-KX768
|
Magic™ Human GPR17 (Long Isoform) In Vitro [35S]GTPγS binding Assay
|
CHO-K1
|
[35S]GTPγS binding Assay
|
|
S01YF-1122-KX772
|
Magic™ Human GPR17 (Short Isoform) In Vitro [35S]GTPγS binding Assay
|
CHO-K1
|
[35S]GTPγS binding Assay
|
|
S01YF-1122-KX776
|
Magic™ Mouse GPR17 In Vitro [35S]GTPγS binding Assay
|
CHO-K1
|
[35S]GTPγS binding Assay
|
|
S01YF-1122-KX780
|
Magic™ Rat GPR17 In Vitro [35S]GTPγS binding Assay
|
CHO-K1
|
[35S]GTPγS binding Assay
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
cAMP Assay
|
S01YF-1122-KX469
|
Magic™ Mouse GPR84 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX471
|
Magic™ Rat GPR84 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
Calcium Flux Assay
|
S01YF-1122-KX464
|
Magic™ Human GPR84 In Vitro Calcium Flux Assay
|
CHO-K1-Gqi5
|
Calcium Flux Assay
|
|
S01YF-1122-KX468
|
Magic™ Mouse GPR84 In Vitro Calcium Flux Assay
|
CHO-K1-Gqi5
|
Calcium Flux Assay
|
|
S01YF-1122-KX470
|
Magic™ Rat GPR84 In Vitro Calcium Flux Assay
|
CHO-K1-Gqi5
|
Calcium Flux Assay
|
|
[35S]GTPγS Binding Assay
|
S01YF-1122-KX466
|
Magic™ Human GPR84 In Vitro [35S]GTPγS binding Assay
|
CHO-K1
|
[35S]GTPγS binding Assay
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
cAMP Assay
|
S01YF-1122-KX782
|
Magic™ Human GPR39 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX784
|
Magic™ Mouse GPR39 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX785
|
Magic™ Rat GPR39 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
Calcium Flux Assay
|
S01YF-1122-KX781
|
Magic™ Human GPR39 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
S01YF-1122-KX783
|
Magic™ Mouse GPR39 In Vitro Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
S01YF-0722-KX173
|
Magic™ Human GPR12 In Vitro cAMP Assay, HEK293
|
HEK293
|
cAMP Assay
|
|
S01YF-1122-KX761
|
Magic™ Human GPR139 In Vitro Calcium Flux Assay
|
HEK293
|
Calcium Flux Assay
|
|
S01YF-1122-KX762
|
Magic™ Human GPR142 In Vitro IP1 Assay
|
HEK293
|
IP1 Assay
|
|
S01YF-1122-KX763
|
Magic™ Mouse GPR142 In Vitro IP1 Assay
|
HEK293
|
IP1 Assay
|
|
S01YF-1122-KX764
|
Magic™ Rat GPR142 In Vitro IP1 Assay
|
HEK293
|
IP1 Assay
|
|
S01YF-0722-KX171
|
Magic™ Human GPR3 In Vitro cAMP Assay, HEK293
|
HEK293
|
cAMP Assay
|
|
S01YF-1122-KX564
|
Magic™ Human GPR34 In Vitro Calcium Flux Assay
|
CHO-K1-Gqi5
|
Calcium Flux Assay
|
|
S01YF-1122-KX565
|
Magic™ Human GPR34 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX566
|
Magic™ Human GPR34 In Vitro [35S]GTPγS binding Assay
|
CHO-K1
|
[35S]GTPγS binding Assay
|
|
S01YF-1122-KX799
|
Magic™ Human GPR4 In Vitro cAMP Assay
|
1321N1
|
cAMP Assay
|
|
S01YF-1122-KX800
|
Magic™ Mouse GPR4 In Vitro cAMP Assay
|
1321N1
|
cAMP Assay
|
|
S01YF-1122-KX801
|
Magic™ Rat GPR4 In Vitro cAMP Assay
|
1321N1
|
cAMP Assay
|
|
S01YF-1122-KX786
|
Magic™ Human GPR52 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX787
|
Magic™ Mouse GPR52 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX788
|
Magic™ Rat GPR52 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-1122-KX567
|
Magic™ Human GPR55 In Vitro Calcium Flux Assay
|
CHO-K1-Gq13
|
Calcium Flux Assay
|
|
S01YF-1122-KX568
|
Magic™ Human GPR55 In Vitro Internalization Assay
|
CHO-K1
|
Internalization Assay
|
|
S01YF-0722-KX172
|
Magic™ Human GPR6 In Vitro cAMP Assay, HEK293-TREx
|
HEK293-TREx
|
cAMP Assay
|
|
S01YF-1122-KX802
|
Magic™ Human GPR65 In Vitro cAMP Assay
|
1321N1
|
cAMP Assay
|
|
S01YF-1122-KX803
|
Magic™ Human GPR65 In Vitro IP1 Assay
|
1321N1
|
IP1 Assay
|
|
S01YF-1122-KX804
|
Magic™ Mouse GPR65 In Vitro cAMP Assay
|
1321N1
|
cAMP Assay
|
|
S01YF-1122-KX805
|
Magic™ Rat GPR65 In Vitro cAMP Assay
|
1321N1
|
cAMP Assay
|
|
S01YF-1122-KX789
|
Magic™ Human GPR83 In Vitro Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-1122-KX790
|
Magic™ Human GPR83 In Vitro IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-1122-KX791
|
Magic™ Mouse GPR83 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
S01YF-1122-KX792
|
Magic™ Mouse GPR83 In Vitro IP1 Assay
|
CHO-K1-Gα16
|
IP1 Assay
|
|
S01YF-1122-KX793
|
Magic™ Human GPR88 In Vitro Calcium Flux Assay
|
CHO-K1-Gqi5
|
Calcium Flux Assay
|
|
S01YF-1122-KX794
|
Magic™ Human GPR88 In Vitro cAMP Assay
|
HEK293
|
cAMP Assay
|
|
S01YF-1122-KX795
|
Magic™ Mouse GPR88 In Vitro cAMP Assay
|
HEK293
|
cAMP Assay
|
|
S01YF-1122-KX796
|
Magic™ Rat GPR88 In Vitro cAMP Assay
|
HEK293
|
cAMP Assay
|
|
S01YF-1122-KX585
|
Magic™ Human MAS1 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
Published Data
Paper Title
|
The Roles of Orphan G Protein-Coupled Receptors in Autoimmune Diseases
|
Journal
|
Clinical Reviews in Allergy & Immunology
|
Published
|
2021
|
Abstract
|
GPCRs constitute the largest family of plasma membrane receptors and play crucial roles in the transduction of a variety of extracellular signals. oGPCRs are GPCRs for which natural ligands have not yet been discovered. They not only mediate various physiological functions, such as metabolism, sensory, reproduction, and development but are also closely related to many major diseases, such as central nervous system (CNS) diseases, metabolic diseases, and cancer. Studies have shown that oGPCRs play an increasingly important role in the occurrence and progression of autoimmune diseases. Therefore, oGPCRs are emerging as attractive therapeutic targets. This article summarized the latest research progress of oGPCRs in three common autoimmune diseases, multiple sclerosis (MS), rheumatoid arthritis (RA), and systemic lupus erythematosus (SLE), which provided the basis for proposing new therapeutic strategies.
|
Result
|
Studies have shown GPR56 as a potential novel marker associated with enhanced cellular activation in RA patients. In MS, oGPCRs regulate peripheral and CNS myelination by modulating myelination mechanisms. oGPCRs mediate inflammatory responses by modulating immune cell responses and the release of pro-inflammatory cytokines. Furthermore, in SLE, oGPCRs regulate disease progression by modulating immune cell involvement in IFN-I production. The same class of oGPCRs may be involved in the regulation of multiple autoimmune diseases and are involved in disease progression. In conclusion, oGPCRs occupy a crucial position in the occurrence, development, and treatment of autoimmune diseases.
Fig.2 The role of β-arrestins in the desensitization, endocytosis, and signal transduction of GPCRs. (Zhao, 2021)
|
References
-
Alavi, M. S.; et al. Orphan G protein-coupled receptors: The role in CNS disorders. Biomedicine & Pharmacotherapy. 2018; 98: 222-232.
-
Zhao, M.; et al. The Roles of Orphan G Protein-Coupled Receptors in Autoimmune Diseases. Clinical Reviews in Allergy & Immunology. 2018; 98: 222-232.
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