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GPCRs are Important Drug Targets

G protein-coupled receptors (GPCRs) are the largest family of human cell-surface receptors. These seven-transmembrane (7TM) proteins are activated by a diverse range of extracellular ligands, including neurotransmitters, odorants, hormones, ions, and photons. Ligand binding causes a conformational change in the GPCR and the subsequent activation of the bound G protein. The activated G proteins stimulate multiple downstream signaling pathways, resulting in the regulation of a variety of physiological processes. GPCR or G protein mutations and abnormal GPCR signaling has been shown to underlie many diseases such as cardiac and inflammatory disorders, metabolic diseases, and cancer. As such, GPCRs have been a common target for therapeutic development. Roughly 35% of drugs approved by the FDA are directed against GPCRs. However, only a small proportion of the 800 GPCRs identified are currently targeted by therapeutics, leaving over 55% of the non-olfactory GPCRs to still be explored as potential drug targets.

GPCR Antibodies for GPCR Drug Development

Expanding the range of therapeutics directed against GPCRs requires highly specific tools for drug discovery, particularly GPCR antibodies. Antibodies are invaluable tools for drug development as they are used for:

  • Identification and validation of the biological target
  • Assay development
  • Patient selection
  • Evaluation of cell models
  • Verification of consistent analyte expression by engineered cell lines

Since there is great interest in GPCRs as targets for new therapeutics, there is considerable demand for GPCR antibodies. However, antibodies directed against GPCRs are difficult to generate as the receptors are embedded in the plasma membrane, which limits usable immunogenic epitopes and makes the receptors difficult to isolate. As such, many commercially available GPCR antibodies lack the specificity that is needed for the drug development process.

Bio-Techne brand R&D Systems, has been the leader in designing and manufacturing GPCR antibodies for over 20 years. Our antibodies out-perform our competitors because:

  • We use whole cell transfectants as immunogens. This allows us to produce antibodies against the full, native GPCR.
  • We screen our GPCR antibodies using native GPCR-expressing cells to ensure that our antibodies detect the native protein.
  • Our antibody validation protocol is unmatched in the industry. In addition to continually testing lot-to-lot consistency and antibody performance, we confirm antibody specificity using true and irrelevant transfected cells and perform live cell staining to verify detection for low expressing GPCRS.
  • About 95% of our 1900+ GPCR antibodies are validated for flow cytometry, allowing you to easily detect receptor expression in your cell models or engineered cell lines.

To learn more about our approach to manufacturing GPCR antibodies visit the R&D Systems Antibodies for G Protein-Coupled Receptors page .

R&D Systems CCR7 antibody binds to endogenously expressed CCR7.

Case Studies Using Bio-Techne GPCR Antibodies

CCR5 Epitope Mapping

Authors of a 1999 Journal of Biological Chemistry paper sought to map the epitopes of the chemokine receptor CCR5, a coreceptor for HIV-1, to determine the domains that are involved in binding to the viral envelope glycoprotein. R&D Systems worked with the investigators to generate a panel of CCR5 monoclonal antibodies that can distinguish the different epitopes.

PAR2 Epitope Responsible for Blocking Antibody Binding

Authors of a 2017 Nature paper wanted to determine the crystal structure of Protease-Activated Receptor 2 (PAR2) in complex with antagonists to determine allosteric sites that could be used for drug design. R&D Systems worked with the authors to purify the Fab from our Human PAR2 Monoclonal Antibody, which blocks PAR2 activation, so to determine the epitope that is responsible for the antibody’s blocking activity.

Small Molecules And Peptides for Developing GPCR Therapeutics

Bio-Techne, through its Tocris brand, offers DREADD ligands to investigate GPCR signaling.

DREADD Ligands by Tocris

DREADDs are genetically modified GPCRs that only respond to biologically inert compounds, i.e., DREADD ligands. Bio-Techne offers DREADD ligands for investigating GPCR signaling and manipulation of neuronal activity.

Chemokines bind to G protein-coupled receptors and regulate cell migration under homeostatic and inflammatory conditions.

Chemokines and Chemokine Receptors

Chemokines and their G protein-coupled receptors are considered to be highly promising drug targets for the treatment of chronic inflammatory and autoimmune diseases. Explore our wide range of R&D Systems™ bioactive chemokines for investigating chemokine-receptor interactions, signaling pathways, and functions.

GPCR-Related Resources

R&D Systems offers antibodies for over 70% of the GPCR families. Explore our interactive graphic to view our coverage

Interactive GPCR Family Tree

Explore this interactive GPCR family tree on the R&D Systems site. The clickable family names link to antibodies and other research tools that we offer for the receptors in that family.