DOP070 The FFA2 antagonist GLPG0974: opportunity to treat neutrophil-driven inflammation

Vanhoutte, Frédéric; Namour, F.; Dupont, Sonia; Haazen, Wouter; Petkova, M; Aa, Annegret Van der; Klooster, Gerben van ’t; Beetens, Johan

doi:10.1016/s1873-9946(14)60095-7

Cited by 2 publications

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“…We have shown that the GPR84 agonist ZQ16 induces a rise in [Ca 2+ ]i, is a weak secretagogue (triggered a low level of degranulation), a modest chemoattractant and a weak activator of NADPH oxidase‐derived ROS in naïve neutrophils (Sundqvist et al, 2018). All these neutrophil functions were abolished by the GPR84 selective antagonist GLPG1205 (Labéguère et al, 2020; Vanhoutte et al, 2015), confirming the involvement of GPR84 in neutrophil activation. Furthermore, when we examined the GPR84‐mediated ROS production induced by ZQ16 in more detail, we found that the level of ROS could be significantly enhanced by pre‐treatment of the cells with either the priming agent TNF‐α or the actin cytoskeleton disrupting agent latrunculin A (Sundqvist et al, 2018).…”

Section: Expression and Function Of Gpr84 In Neutrophilsmentioning

confidence: 79%

Function and regulation of GPR84 in human neutrophils

Forsman

Dahlgren

Mårtensson

et al. 2023

British J Pharmacology

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Human neutrophils are components of the innate immune system and are the most abundant white blood cells in the circulation. They are professional phagocytes and express several G protein‐coupled receptors (GPCRs), which are essential for proper neutrophil functions. So far, the two formyl peptide receptors, FPR1 and FPR2, have been the most extensively studied group of neutrophil GPCRs, but recently, a new group, the free fatty acid (FFA) receptors, has attracted growing attention. Neutrophils express two FFA receptors, GPR84 and FFA2, which sense medium‐ and short‐chain fatty acids respectively, and display similar activation profiles. The exact pathophysiological role of GPR84 is not yet fully understood, but it is generally regarded as a pro‐inflammatory receptor that mediates neutrophil activation. In this review, we summarize current knowledge of how GPR84 affects human neutrophil functions and discuss the regulatory mechanisms that control these responses, focusing on the similarities and differences in comparison to the two FPRs and FFA2.

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Section: Expression and Function Of Gpr84 In Neutrophilsmentioning

confidence: 79%

Function and regulation of GPR84 in human neutrophils

Forsman

Dahlgren

Mårtensson

et al. 2023

British J Pharmacology

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Update on Janus Kinase Antagonists in Inflammatory Bowel Disease

Boland

Sandborn

Chang

2014

Gastroenterology Clinics of North America

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Janus kinase (JAK) inhibitors have emerged as a novel orally administered small molecule therapy for the treatment of ulcerative colitis and possibly Crohn’s disease. These molecules are designed to selectively target the activity of specific JAKs and offer a targeted mechanism of action without risk of immunogenicity. Based on data from clinical trials in rheumatoid arthritis and phase 2 studies in inflammatory bowel disease, tofacitinib and other JAK inhibitors are likely to become a new form of medical therapy for the treatment of inflammatory bowel disease.

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DOP070 The FFA2 antagonist GLPG0974: opportunity to treat neutrophil-driven inflammation

Cited by 2 publications

References 0 publications

Function and regulation of GPR84 in human neutrophils

Function and regulation of GPR84 in human neutrophils

Update on Janus Kinase Antagonists in Inflammatory Bowel Disease

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