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Commentary - (2021) Volume 7, Issue 2

Study of G-Protein Coupled Receptors and its Clinical uses in Asthma

Chandhu Kandregula*

Department of Pharmacology, Manipal University, Manipal, Karnataka, India

*Corresponding Author:
Chandhu Kandregula
Department of Pharmacology
Faculty of Sciences
Manipal University
Manipal, Karnataka, India

Received Date: October 6, 2021; Accepted Date: October 20, 2021; Published Date: October 27, 2021

Citation: Kandregula C (2021) Study of G-Protein Coupled Receptors and its Clinical uses in Asthma. Mol Enzy Drug Targ Vol.7 No.2:2

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Receptors are protein-based chemical structures that receive and transmit signals that can be integrated into biological systems. These signals are usually chemical messengers that attach to a receptor and elicit a cellular/tissue response.

G-Protein Coupled Receptors (GPCRs) are regarded as one of the most widespread families of approved pharmacological targets, having involvement in almost all physiological activities and pathological processes.

GPCRs are integral membrane proteins that cells use to convert extracellular signals into intracellular responses, such as hormone, neurotransmitter, and vision, olfaction, and taste signals. Based on their sequences and structural similarities, these receptors comprise a superfamily of membrane proteins that includes five separate families: rhodopsin (family A), secretin (family B), glutamate (family C), adhesion, and Frizzled/ Taste [1]. They all have seven transmembrane helices coupled to three extracellular loops and three intracellular loops in common. Despite its structural similarities, GPCRs have distinct signal-transduction capabilities that involve both G proteindependent independent signalling pathways, as well as complex regulation mechanisms.

Physiological Roles of GPCRs

GPCRs are involved in a wide variety of physiological processes. Some examples of their physiological roles include:

• The visual sense.

• The gustatory sense (taste).

• The sense of smell.

• Behavioural and mood regulation.

• Regulation of immune system activity and inflammation.

• Autonomic nervous system transmission.

• Cell density sensing.

• Growth and metastasis of some types of tumours.

• Endocrine system.

GPCRs in Treatment of Asthma

GPCRs are the widely spread drug targets in humans. Over 33% of presently used small-molecule medicines are thought to target GPCRs [2]. This is because GPCRs have various drug gable characteristics. To begin, GPCRs are significant participants in the detection of extracellular signalling molecules on cell surfaces. They play a role in almost every aspect of in vivo physiologic processes. By pharmacologically modifying certain GPCRs, almost every physiologic pathway may be reduced or increased. Second, the vast majority of native and endogenous GPCR ligands are small-molecule compounds and peptides, and many GPCR-targeting medications are based on natural molecules. As a result, there are several natural chemical templates for developing novel small-molecule medicines. Finally, the ligand-binding sites of GPCRs are placed in extracellular areas that medicines can easily access.

Many of the current asthma medicines target GPCRs. Several studies over the last several decades have demonstrated variety of roles of GPCRs in asthma, including the β2-adrenergic receptor, muscarinic cholinergic receptors, leukotriene and PG receptors, chemokine receptors, and adenosine receptors. A great number of clinical trials have shed light on the importance of GPCR-targeting medicines in the treatment of asthma. Furthermore, advances in GPCR structural biology over the last decade have helped us to comprehend the chemical effects of numerous GPCR-targeting medicines [3].

Future Perspectives of GPCRs in Asthma

Although current available treatments can manage asthma in the majority of patients, there are still a significant number of asthma patients who need more effective medicines. Our new understanding of asthma's heterogeneity also emphasises the need for novel therapeutics for certain forms of asthma, such as non-atopic, TH2 low or obesity-related asthma endotypes. Despite this demand, therapeutic research for asthma has been moderate during the last two decades. The current standard treatment regimens for asthma, which include the use of ICSs, LABAs, and LAMAs in combination, were established more than 15 years ago. Recently, biologic medicines targeting IL-5 and Ig E were developed as a new class of anti-inflammatory therapies, providing further add-on alternatives for asthma patients with specific phenotypes [4]. Biologics are also being developed to block IL-13, IL-4, and other cytokines.


GPCR-targeting ligands with potential as novel asthma medicines were reviewed in this study, with a focus on those that had entered clinical trials. However, it is important to note that there are a number of additional interesting GPCR modulators in the early stages of research for asthma. Bitter taste receptor agonists like Saccharin, Chloroquine, and Quinine, calcium-sensing receptor antagonists, and specialised proresolving lipid mediators are among them. They might also provide interesting potential for the development of innovative asthma treatments.



  1. Fredriksson R, Lagerström MC, Lundin LG, Schiöth HB (2003) The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol 63:1256-1272.
  2. Santos R, Ursu O, Gaulton A, Bento AP, Donadi RS et al. (2017) A comprehensive map of molecular drug targets. Nat Rev Drug Discov 16:19-34.
  3. Hauser AS, Attwood MM, Rask-Andersen M, Schiöth HB, Gloriam DE (2017) Trends in GPCR drug discovery: new agents, targets and indications. Nat Rev Drug Discov 16:829-842.
  4. Pelaia G, Vatrella A, Maselli R (2012) The potential of biologics for the treatment of asthma. Nat Rev Drug Discov. 11:958-972.