Target intelligence / Profile preview

G protein-coupled receptor 32 (GPR32)

Target
GPR32
Molecular classification
G protein-coupled receptor, Class A (Rhodopsin-like receptor), Ophan receptor (historically, as natural ligand(s) were not initially known)
01

Overview

G protein-coupled receptor 32 (GPR32) is a human transmembrane receptor in the rhodopsin-like family of G protein-coupled receptors (GPCRs)[1][3][5]. Initially classified as an *orphan receptor* without a known endogenous ligand, GPR32 was later identified as a receptor for several D-series resolvins (e.g., resolvin D1, D3, and D5)—specialized pro-resolving lipid mediators derived from the omega-3 fatty acid docosahexaenoic acid (DHA)[1][7][9]. Activation of GPR32 by these resolvins mediates potent anti-inflammatory and pro-resolving activities, such as limiting neutrophil migration, enhancing the clearance of cellular debris by macrophages, and promoting the resolution of inflammatory lesions, thereby restoring tissue homeostasis[1][9]. GPR32 is expressed in various immune cells (neutrophils, activated CD8+ T cells, CD4+ T cells, T helper 17 cells, and tissue macrophages), as well as small airway epithelial cells and adipose tissue[1]. GPR32’s closest homologous receptors are the formyl peptide receptors (FPR family), which also mediate responses to lipid pro-resolving mediators[9]. GPR32 is not present in mouse or typical rodent genomes, complicating preclinical research[1]. As of the latest research, it is not yet a primary clinical target, but is of growing interest for the treatment of chronic inflammatory and auto-inflammatory diseases due to its unique role in resolving inflammation[1][9].

Other names
RvD1 receptorProbable G-protein coupled receptor 32
02

Mechanism of action

Activation of GPR32 by resolvins triggers intracellular signaling leading to reduced neutrophil migration, enhanced clearance of apoptotic cells by macrophages, suppression of excessive inflammatory responses, and promotion of resolution phase (restoration of homeostasis)[1][7][9].

03

Biological functions

Signal transductionInhibition and resolution of inflammationModulation of immune cell chemotaxis (especially neutrophils and macrophages)Enhancement of phagocytic and clearance functions in macrophages
04

Disease associations

InflammationPulmonary inflammationOther inflammation-driven disordersPotentially other diseases related to failure of inflammation resolution
05

Safety considerations

No significant safety concerns reported as GPR32 is not yet a clinical drug target.Potential challenges relate to the specificity of modulators and the risk of immunosuppression from excessive anti-inflammatory signaling[1][9].
06

Interacting drugs

Resolvins (endogenously derived agonists): Resolvin D1

4 more in the full profile.

07

Biomarkers

None directly established for GPR32 itself.Expression of GPR32 in immune cells (neutrophils, macrophages, subsets of T cells) may have emerging biomarker relevance in research[1][5].

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