Recombinant Human Probable G-protein coupled receptor 52 (GPR52)

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Cat. No.
BT2063513
Source
in vitro E.coli expression system
Synonyms
GPR52; G-protein coupled receptor 52
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Description

Cryo-EM Structures

  • Ligand-free state: ECL2 occupies the orthosteric pocket, enabling self-activation .

  • Gs-coupled state: Achieves full activation without external ligands, with a resolution of 3.32 Å .

  • Allosteric ligand-bound state: Reveals a side pocket for potential drug targeting .

Signaling Mechanisms

  • Constitutive Activity: Unliganded GPR52 exhibits 83–87% maximal Gs activity but only 5–26% β-arrestin recruitment, indicating intrinsic signaling bias .

  • Pathway Modulation:

    • Gs/cAMP: Regulates dopamine receptor signaling and huntingtin (HTT) stabilization via Rab39B .

    • Disease Link: Knockout reduces mutant HTT levels in Huntington’s disease models .

Neurological Disorders

  • Schizophrenia: Agonists (e.g., FTBMT, HTL’149) suppress psychosis-related behaviors in rodents .

  • Huntington’s Disease: GPR52 knockout decreases mutant HTT accumulation and rescues behavioral deficits .

Cancer Biology

  • Triple-Negative Breast Cancer (TNBC): GPR52 loss promotes EMT and invasiveness via upregulated CREB1 pathways .

Immune Regulation

  • T Cells: Modulates cAMP levels but shows no impact on autoimmune encephalomyelitis (EAE) severity in knockout models .

Agonists and Drug Development

CompoundEC₅₀ (cAMP)BioavailabilityTherapeutic Potential
FTBMT30 nMHighSchizophrenia (Phase I trials)
EX5467ComparableModerateCognitive symptom rescue

Challenges

  • Orphan Status: Lack of confirmed endogenous ligands complicates mechanistic studies .

  • PTM Sensitivity: N-glycosylation at N20 is essential for receptor trafficking and activity .

Future Directions

  • Ligand Discovery: High-throughput screening to identify endogenous or synthetic modulators .

  • Structural Optimization: Targeting allosteric pockets for biased signaling drugs .

Product Specs

Form
Lyophilized powder
Note: We prioritize shipping the format currently in stock. However, if you have specific format requirements, please indicate them when placing your order. We will fulfill your request if possible.
Lead Time
Delivery time may vary based on the purchase method and location. Please consult your local distributor for specific delivery details.
Note: All our proteins are shipped with standard blue ice packs. If you require dry ice shipping, please inform us in advance. Additional fees will apply.
Notes
Repeated freezing and thawing is discouraged. Store working aliquots at 4°C for up to one week.
Reconstitution
We recommend centrifuging the vial briefly prior to opening to ensure the contents settle at the bottom. Reconstitute the protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL. We recommend adding 5-50% glycerol (final concentration) and aliquoting for long-term storage at -20°C/-80°C. Our default glycerol concentration is 50%. Customers can use this as a reference.
Shelf Life
Shelf life is influenced by factors such as storage conditions, buffer components, temperature, and the protein's intrinsic stability.
Generally, liquid forms have a shelf life of 6 months at -20°C/-80°C. Lyophilized forms have a shelf life of 12 months at -20°C/-80°C.
Storage Condition
Store at -20°C/-80°C upon receipt. Aliquoting is necessary for multiple uses. Avoid repeated freeze-thaw cycles.
Tag Info
Tag type will be determined during the manufacturing process.
The tag type is determined during production. If you have a specific tag type requirement, please inform us, and we will prioritize developing the specified tag.
Synonyms
GPR52; G-protein coupled receptor 52
Buffer Before Lyophilization
Tris/PBS-based buffer, 6% Trehalose.
Datasheet
Please contact us to get it.
Expression Region
1-361
Protein Length
full length protein
Species
Homo sapiens (Human)
Target Names
GPR52
Target Protein Sequence
MNESRWTEWRILNMSSGIVNVSERHSCPLGFGHYSVVDVCIFETVVIVLLTFLIIAGNLT VIFVFHCAPLLHHYTTSYFIQTMAYADLFVGVSCLVPTLSLLHYSTGVHESLTCQVFGYI ISVLKSVSMACLACISVDRYLAITKPLSYNQLVTPCRLRICIILIWIYSCLIFLPSFFGW GKPGYHGDIFEWCATSWLTSAYFTGFIVCLLYAPAAFVVCFTYFHIFKICRQHTKEINDR RARFPSHEVDSSRETGHSPDRRYAMVLFRITSVFYMLWLPYIIYFLLESSRVLDNPTLSF LTTWLAISNSFCNCVIYSLSNSVFRLGLRRLSETMCTSCMCVKDQEAQEPKPRKRANSCS I
Uniprot No.
Q9Y2T5

Target Background

Function
G protein-coupled receptor 52 (GPR52) is activated by the antipsychotic reserpine, leading to an increase in intracellular cAMP and its internalization. GPR52 may play a role in locomotor activity by modulating dopamine, NMDA, and ADORA2A-induced locomotor activity. These behavioral changes are associated with modulation of the dopamine receptor signaling pathway in the striatum. GPR52 modulates huntingtin (HTT) levels through cAMP-dependent but PKA-independent mechanisms by activating RAB39B, which translocates HTT to the endoplasmic reticulum, preventing proteasome degradation.
Gene References Into Functions
  1. Data indicate that G protein-coupled receptor 52 (GPR52) regulates huntingtin protein (HTT) levels in striatal cells both in vitro and in vivo. PMID: 25738228
Database Links

HGNC: 4508

OMIM: 604106

KEGG: hsa:9293

STRING: 9606.ENSP00000356658

UniGene: Hs.673850

Protein Families
G-protein coupled receptor 1 family
Subcellular Location
Cell membrane; Multi-pass membrane protein.
Tissue Specificity
Expressed in brain, especially in striatum.

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