Bioactive Lipid G Protein-Coupled Receptors

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Bioactive Lipid G Protein-Coupled Receptors Background

About Bioactive Lipid G Protein-Coupled Receptors

Bioactive Lipid G Protein-Coupled Receptors are a class of coupled receptors on cell membranes that are widely involved in the regulation of cellular physiological activities. These coupled receptors transduce signals primarily by coupling to membrane G proteins, thereby affecting biological processes such as respiration, growth, fermentation, and ferment within the cell. For example, these receptors can interact with lysosomal phospholipase A2, lipocalins, phenolics, and other coupled molecules. These interactions lead to conformational changes in the subunits within G proteins, which activate or inhibit intracellular signaling to begin replenishment and affect cellular function.

Bioactive inhibitors G-coupled receptors are widely expressed in a variety of tissues and play critical roles in numerous physiological processes such as inflammation, immune response, regulation of vascular tone, cell growth, and neurotransmission. They are medically significant because they are important in association with a wide range of diseases and physiological conditions. As a result, these receptors are considered potential drug targets, and researchers are conducting in-depth studies of their functions and regulatory mechanisms to develop new drug therapeutic options.

Mechanism of Action of Bioactive Lipid G Protein-Coupled Receptors

Bioactive lipid GPCRs transduce signals across the cell membrane through their interaction with intracellular G proteins. Upon ligand binding, these receptors undergo conformational changes, leading to the activation of specific G proteins. Activated G proteins modulate intracellular signaling pathways, such as cyclic adenosine monophosphate (cAMP) signaling, phosphoinositide signaling, and mitogen-activated protein kinase (MAPK) signaling, ultimately leading to cellular responses.

GPCRs are known to be activated by a diverse plethora of ligands and stimuli. Fig.1 GPCRs are known to be activated by a diverse plethora of ligands and stimuli. (Heng B C, et al., 2013)

G-protein-coupled receptors (GPCRs) are conventionally considered to function at the plasma membrane, where they detect extracellular ligands and activate heterotrimeric G proteins that transmit intracellular signals. Consequently, drug discovery efforts have focused on the identification of agonists and antagonists of cell surface GPCRs. However, β-arrestin (ARR)-dependent desensitization and endocytosis rapidly terminate G protein signaling at the plasma membrane. Emerging evidence indicates that GPCRs can continue to signal from endosomes by G-protein- and βARR-dependent processes. By regulating the duration and location of intracellular signaling events, GPCRs in endosomes control critically important processes, including gene transcription and ion channel activity. Thus, GPCRs in endosomes, in addition to at the cell surface, have emerged as important therapeutic targets.

Therapeutic Targeting of Endosomal G-Protein-Coupled Receptors.Fig.2 Therapeutic Targeting of Endosomal G-Protein-Coupled Receptors. (Thomsen A R B, et al., 2018)

Functions of Bioactive Lipid G Protein-Coupled Receptors

Bioactive lipid GPCRs exhibit diverse functions in various physiological and pathological processes, including:

  • Inflammation and Immune Responses

Certain bioactive lipid GPCRs, such as LPA receptors and prostaglandin receptors, play critical roles in modulating inflammation and immune responses, including leukocyte activation, chemotaxis, and cytokine production.

  • Vascular Regulation

Receptors for bioactive lipids like prostaglandins and S1P regulate vascular tone, blood vessel permeability, and angiogenesis, impacting cardiovascular physiology and pathology.

  • Neurotransmission and Neuromodulation

Bioactive lipid GPCRs, including endocannabinoid receptors, participate in neurotransmission and neuromodulation processes, influencing neuronal excitability, synaptic plasticity, and pain perception.

  • Cancer and Metastasis

Dysregulation of bioactive lipid GPCRs is associated with various types of cancer, highlighting their roles in tumor growth, angiogenesis, and metastasis.

Available Resources for Bioactive Lipid G Protein-Coupled Receptors

Bioactive lipid GPCRs play critical roles in cellular signaling and regulate various physiological processes. Creative BioMart offers a comprehensive range of resources and services for bioactive lipid GPCR research, enabling scientists to study their mechanisms of action, functions, and involvement in disease processes. The following bioactive lipid G protein-coupled receptors are displayed, click to view all related molecules/targets and research reagents. Please feel free to contact us with any questions or requests.


  1. Heng B C, Aubel D, Fussenegger M. An overview of the diverse roles of G-protein coupled receptors (GPCRs) in the pathophysiology of various human diseases[J]. Biotechnology advances, 2013, 31(8): 1676-1694.
  2. Thomsen A R B, Jensen D D, Hicks G A, et al. Therapeutic targeting of endosomal G-protein-coupled receptors[J]. Trends in pharmacological sciences, 2018, 39(10): 879-891.


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