G-Protein Coupled Receptors in Cancer and Targeting Strategies

  • Aditya Narvekar
  • Ashu Srivastav
  • Aparna Tripathi
  • Padma V. Devarajan
  • Ratnesh JainEmail author
  • Prajakta DandekarEmail author
Part of the AAPS Advances in the Pharmaceutical Sciences Series book series (AAPS, volume 39)


G-protein-coupled receptors (GPCRs) play a significant role in a myriad of physiological processes. Therefore, deregulation of GPCR function is implicated in various cancers, making them a suitable target for targeted therapy. Many studies have indicated a key role of GPCRs in cancer initiation, progression, tumorigenesis, and metastases. This manuscript will discuss a few examples of GPCRs involved in cancer with respect to their structure activity, mechanism of binding, ligands explored, and antagonists, along with the targeting strategies. Many clinical trials with different GPCR targeting drugs are ongoing and are expected to contribute to existing anticancer therapeutics. The research in the area of targeting GPCR is anticipated to exploit their potential as pharmacologically important targets.


G-protein-coupled receptors (GPCRs) Targeting Protease-activated receptors Lysophosphatidic acid receptor Frizzled receptor 



Activated protein C


Adenomatous polyposis coli


Acetylsalicylic acid


Axis inhibition protein


Coronary artery diseases


Cyclic adenosine monophosphate


Calcium sensing


CREB-binding protein


Casein kinase 1


Cysteine-rich domain








1,2-distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol)


Extracellular loops


Endothelial differentiation gene


Epithelial-mesenchymal transition


Endothelial protein C receptor


Fluorescence resonance energy transfer


Frizzled receptor


FZD7 antibody-nanoshell conjugate


G2 accumulation


Guanosine diphosphate


G-protein-coupled receptors


Glycogen synthase kinas


Guanosine triphosphate


Hepatocellular carcinoma


Inhibitory concentration


Intracellular loops


Inositol triphosphate


Lymphoid enhancer factor/T-cell factor


Lysophosphatidic acid


Lipoprotein receptor-related proteins


Leucine-rich repeat-containing receptors


Mitogen-activated protein kinase


Myocardial infarction


Matrix metalloproteases


Mammalian target of rapamycin complex 2

NDP gene

Norrie disease protein gene


Nuclear factor kappa light chain enhancer of activated B cells


Near-infrared radiation


N-terminal sequence


Vantictumab, a monoclonal antibody


A novel recombinant fusion protein


Protease activable prodrugs


Protease-activated receptor


Planar cell polarity


Polyethylene glycol


Phosphatidylinositol 3-kinase-protein kinase B




Protein kinase


Protein kinase C


Phospholipase C


Phospholipase C-β




Ras-related C3 botulinum toxin substrate


Rapidly accelerated fibrosarcoma-MAPK ERK kinase-mitogen-activated protein kinase


RAS homologous protein family

Ryk and Ror2

Tyrosine kinase receptor


Secreted frizzled-related protein


Soluble frizzled receptor 7 antagonist decoy receptor


Clostridium difficile toxin B


Tethered ligand sequence




Thyroid-stimulating hormone


Up-conversion nanoparticles


Vascular endothelial growth factor;


Wingless type protein


Xenopus wingless type protein


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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Aditya Narvekar
    • 1
  • Ashu Srivastav
    • 3
  • Aparna Tripathi
    • 1
  • Padma V. Devarajan
    • 2
  • Ratnesh Jain
    • 3
    Email author
  • Prajakta Dandekar
    • 2
    Email author
  1. 1.Department of Pharmaceutical Sciences & TechnologyInstitute of Chemical Technology, MatungaMumbaiIndia
  2. 2.Department of Pharmaceutical SciencesInsitute of Chemical Technology, Deemed University, Elite Status and Centre of Excellence, Government of MaharashtraMumbaiIndia
  3. 3.Department of Chemical EngineeringInstitute of Chemical Technology, MatungaMumbaiIndia

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