G protein-coupled receptors (GPCRs)

Introduction

G protein-coupled receptors (GPCRs) are a large family of cell-surface receptors with a conserved seven-transmembrane structure. They convert extracellular signals, including hormones, neurotransmitters, chemokines, lipids, metabolites, and sensory stimuli, into intracellular responses through G protein- and β-arrestin-mediated signaling. As key regulators of cell communication, GPCRs are involved in immune regulation, tumor biology, metabolism, neuroscience, cardiovascular function, and inflammation, making them one of the most important target families in modern drug discovery.

DIMA BIOTECH provides an overview of GPCR targets organized by research focus, including immune cell trafficking, cancer and tumor immunology, metabolic and endocrine diseases, and vascular or fibrosis-related research. This resource also connects researchers to related target pages, blogs, videos, and GPCR products.

the structure of GPCRs

The structure of GPCRs

Popular Targets Products Digital Resource

Popular Targets by Research Focus

To help researchers navigate this diverse target family more efficiently, the following section organizes selected GPCR targets by major research focus rather than structural class. Each category highlights representative targets with strong relevance to current drug discovery, antibody development, and cell-based assay applications.

Immune cell trafficking controls leukocyte migration, tissue infiltration, and responses to inflammatory or tumor-associated signals. GPCRs, especially chemokine receptors such as CCR/CXCR family members and complement receptors such as C5AR1 and C5AR2, are key regulators of this process. These targets are widely used in immunology, oncology, inflammation, and antibody discovery research.

C-X-C chemokine receptor type 4 (CXCR4)

  • Aliases: CD184, Fusin, LESTR
  • Indication: Hematologic malignancies; tumor metastasis
Explore the blog of CXCR4

Atypical chemokine receptor 3 (ACKR3)

  • Aliases: CXCR7, RDC1
  • Indication: cancer progression; angiogenesis
Explore the blog of CXCR7

C-C chemokine receptor type 8 (CCR8)

  • Aliases: CD198, CMKBR8
  • Indication: Treg-targeted solid tumor immunotherapy
Explore the blog of CCR8

C-C motif chemokine receptor 1 (CCR1)

  • Aliases: CD191, CMKBR1
  • Indication: Autoimmune and Inflammatory Diseases
Explore the blog of CCR1

C-C chemokine receptor type 2 (CCR2)

  • Aliases: CD192, MCP-1R, CKR2
  • Indication: Inflammatory disease; fibrosis

C-X-C chemokine receptor type 3 (CXCR3)

  • Aliases: CD183, GPR9
  • Indication: Autoimmune disease; T cell-mediated inflammation

Complement C5a receptor 1 (C5AR1)

  • Aliases: C5aR, CD88
  • Indication: Complement-mediated inflammation

Complement C5a receptor 2 (C5AR2)

  • Aliases: C5L2, GPR77
  • Indication: Sepsis; inflammatory disease

Metabolic GPCRs regulate glucose homeostasis, insulin secretion, appetite, energy balance, lipid metabolism, and hormone signaling. These targets are highly relevant to diabetes, obesity, metabolic syndrome, and next-generation weight-loss drug discovery.

G protein-coupled receptor 75 (GPR75)

  • Indication: Obesity
Explore the Blog of GPR75

Glucagon receptor (GCGR)

  • Aliases: GCG receptor
  • Indication: Obesity; metabolic disease
Explore the Blog of GCGR

Neuropeptide Y receptor Y2 (NPY2R)

  • Aliases: NPY Y2 receptor, Y2 receptor
  • Indication: Obesity; appetite regulation
Explore the Blog of NPY2R

G protein-coupled receptor 84 (GPR84)

  • Aliases: EX33
  • Indication: Metabolic inflammation; fibrosis
Explore the Blog of GPR84

Melanocortin 4 receptor (MC4R)

  • Aliases: MC4 receptor
  • Indication: Obesity; appetite regulation
Explore the Blog of MC4R

Glucose-dependent insulinotropic receptor (GPR119)

  • Aliases: G-protein coupled receptor 119
  • Indication: Type 2 diabetes

Many GPCRs are involved in tumor progression, immune suppression, Wnt/Hedgehog signaling, and antibody-based therapeutic development. Targets such as GPRC5D and FZD10 are relevant to antibody drugs, T cell engagers, CAR-T strategies, and solid or hematologic tumor research.

Frizzled class receptor 10 (FZD10)

  • Aliases: Frizzled-10, Fz-10, CD350
  • Indication: Solid tumors

Prostaglandin E receptor 4 (PTGER4)

  • Aliases: EP4, PGE2 receptor EP4
  • Indication: Cancer inflammation; immuno-oncology

Leucine-rich repeat-containing G protein-coupled receptor 5 (LGR5)

  • Aliases: GPR49, HG38
  • Indication: Colorectal cancer; cancer stem cells

These GPCRs regulate vascular tone, endothelial function, tissue remodeling, fibrosis, and inflammatory repair responses. They are important in cardiovascular disease, pulmonary hypertension, respiratory disease, chronic inflammation, and fibrosis-related drug discovery.

Adrenoceptor beta 2 (ADRB2)

  • Aliases: β2AR, Beta-2 adrenergic receptor, B2AR
  • Indication: Asthma; COPD

Lysophosphatidic acid receptor 1 (LPAR1)

  • Aliases: LPA1, EDG2, VZG1
  • Indication: Idiopathic pulmonary fibrosis

Sphingosine-1-phosphate receptor 1 (S1PR1)

  • Aliases: S1P1, EDG1, CD363
  • Indication: Multiple sclerosis; autoimmune disease

Products

DIMA BIOTECH provides integrated GPCR research solutions to support target validation, antibody discovery, functional screening, and drug development. With expertise in membrane protein preparation, cell-based validation, and antibody reagent development, DIMA BIOTECH helps researchers access reliable tools for challenging GPCR targets.

*Search by gene name, alias, UniProt ID, or product SKU. Can’t find what you need? Contact us for custom development.

Nanodisc Proteins

Human BRIL-MC2R-Strep full length protein-synthetic nanodisc

SKU:  FLP120182A     Target:  MC2R     Tag:  C-Flag&Strep Tag

Expression Host:  HEK293

Price: 10 μg $810.00 ; 50 μg $3960.00 ; 100 μg $7200.00

Human BRIL-TAAR1-Strep full length protein-synthetic nanodisc

SKU:  FLP120481A     Target:  TAAR1     Tag:  C-Flag&Strep Tag

Expression Host:  HEK293

Price: 10 μg $810.00 ; 50 μg $3960.00 ; 100 μg $7200.00

Human BRIL-GPR75 full length protein-synthetic nanodisc

SKU:  FLP100031C     Target:  GPR75     Tag:  C-Flag Tag

Expression Host:  HEK293

Price: 10 μg $900.00 ; 50 μg $4400.00 ; 100 μg $8000.00

Human GPRC5C-Strep full length protein-synthetic nanodisc

SKU:  FLP120289     Target:  GPRC5C     Tag:  C-Flag&Strep Tag

Expression Host:  HEK293

Price: 10 μg $810.00 ; 50 μg $3960.00 ; 100 μg $7200.00

Human beta2AR-GPR75-BRIL full length protein-synthetic nanodisc

SKU:  FLP100031A     Target:  GPR75     Tag:  C-Flag Tag

Expression Host:  HEK293

Price: 10 μg $900.00 ; 50 μg $4400.00 ; 100 μg $8000.00

Human MBP-GPR75 full length protein-synthetic nanodisc

SKU:  FLP110031     Target:  GPR75     Tag:  N-MBP Tag, C-Flag Tag

Expression Host:  HEK293

Price: 10 μg $900.00 ; 50 μg $4400.00 ; 100 μg $8000.00

Human S1PR3-Strep full length protein-synthetic nanodisc

SKU:  FLP120462     Target:  S1PR3     Tag:  C-Flag&Strep Tag

Expression Host:  HEK293

Price: 10 μg $810.00 ; 50 μg $3960.00 ; 100 μg $7200.00

Human S1PR2-Strep full length protein-synthetic nanodisc

SKU:  FLP120461     Target:  S1PR2     Tag:  C-Flag&Strep Tag

Expression Host:  HEK293

Price: 10 μg $810.00 ; 50 μg $3960.00 ; 100 μg $7200.00

Explore All of Nanodisc Proteins!

FACS-Validated Antibodies

Anti-CLDN18.2 antibody(353A3), IgG1 Chimeric mAb

SKU:  DMC101768     Target:  CLDN18.2

Application:  Flow Cyt

Price: 10μg $99.00 ; 100μg $446.00 ; 500μg $1340.00

Anti-LGR5(petosemtamab biosimilar) mAb

SKU:  BME100297     Target:  LGR5

Application:  Flow Cyt

Price: 50 μg $82.00 ; 100 μg $162.00

Biotinylated Anti-LGR4 antibody(1D9), Rabbit mAb

SKU:  DME101188B     Target:  LGR4

Application:  ELISA

Price: 10μg $139.00 ; 100 μg $670.00 ; 500 μg $1999.00

Anti-CXCR6 antibody(2B3), IgG1 Chimeric mAb

SKU:  DMC101533     Target:  CXCR6

Application:  ELISA

Price: 10μg $99.00 ; 100 μg $446.00 ; 500 μg $1340.00

Anti-CXCR3 (53Hu37 biosimilar)mAb

SKU:  BME100283     Target:  CXCR3

Application:  ELISA, Flow Cyt

Price: 50 μg $82.00 ; 100 μg $162.00

30%

Anti-MC4R antibody(2H10), Rabbit mAb

SKU:  DME101294     Target:  MC4R

Application:  Flow Cyt

Price: 10μg $99.00 ; 100 μg $446.00 ; 500 μg $1340.00

30%

Anti-GPR20 antibody(1E10), Rabbit mAb

SKU:  DME101292     Target:  GPR20

Application:  Flow Cyt

Price: 10μg $99.00 ; 100 μg $446.00 ; 500 μg $1340.00

30%

Anti-GLP1R antibody(1A4), Rabbit mAb

SKU:  DME101291     Target:  GLP1R

Application:  Flow Cyt

Price: 10μg $99.00 ; 100 μg $446.00 ; 500 μg $1340.00

Explore All of FACS mAbs

Digital Resource

Videos

High Quality GPCR mAb Discovery Using Full Length Nanodisc GPCR Proteins & Single B Cell technology

CC Chemokine Receptors CCR1–CCR10 Drug Development and Nanodisc Protein Solutions

CXCR4 in Disease and Therapy Full Length Protein and Antibody Solutions

GLP1R, a popular target for blood sugar control and weight loss

Explore All Vedios