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Monoclonal antibody targeting GPCR

G protein-coupled receptors (GPCRs) are membrane proteins that have only a relatively small mass exposed outside the membrane that can be recognized by antibody. The expression of GPCRs in cells is quite limited and the generation of mAbs targeting GPCRs, which can interfere directly with signaling, is considered difficult.

NBHL has been studying methods to fit the development of functional mAbs targeting GPCRs with available technologies. Antigen format is a critical consideration when developing functional mAbs targeting GPCRs. In our proprietary technology, we have tried to present antigen GPCR in a conformationally stable form with a high level of expression in vivo with the specific GPCR expression vector system.

A high-throughput flow cytometry system is used to screen for mAbs of interest. NBHL also uses state-of-the-art assay platforms that monitor various GPCR signaling pathways to identify mAbs with the desired agonist or antagonist function.

Properties of NBHL mAbs

  1. Antibodies that recognize native GPCRs
  2. High selectivity
  3. High affinity
  4. Direct modulation of GPCR signaling, without antibody-dependent cellular cytotoxicity (ADCC) or complement-dependent cytotoxicity (CDC)

Potential applications for NBHL mAbs

  1. Therapeutic antibodies
  2. Diagnostic tools
  3. Research tools for GPCR-targeted drug discovery
    1. Expression analysis of target GPCRs on a cell surface
    2. Co-crystallization of GPCR with antibody for in silico drug design
    3. Positive references for target GPCR functional assays
    4. Surrogate ligands for orphan GPCRs
    5. Proof of concept in animal models
mAb library targeting GPCR under development with NBHL technology platform
Ligand Class Activity Indication
Prostaglandin A Full antagonist Autoimmune disease
Chemokine A Full antagonist Fibrosis
Lipid mediator A Full antagonist Pain, Fibrosis
Fatty acid A Agonist Diabetes
Amine A Modulator Metabolic diseases
Peptide B Modulator Diabetes
Chemokine A Full antagonist Infectious diseases
Wnt FZD Full antagonist Cancer
Orphan C Agonist Respirtory diseases
Peptide A Full antagonist Ophthalmology