Ligand-specific conformational change of the G-protein–coupled receptor ALX/FPR2 determines proresolving functional responses

No abstract is available for this paper.

• Publication year

  2013

• Venue

  Proceedings of the National Academy of Sciences of the United States of America

• Publication date

  2013-10-09

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1073/pnas.1308253110PMID 24108355PMCID PMC3831442
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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• International Union of Basic and Clinical Pharmacology. LXXIII. Nomenclature for the Formyl Peptide Receptor (FPR) Family

  2009influential reference
• Resolving inflammation: dual anti-inflammatory and pro-resolution lipid mediators

  2008cited by this paper
• Gene expression in human peripheral blood mononuclear cells upon acute ischemic stroke

  2008cited by this paper
• Design and synthesis of benzo-lipoxin A4 analogs with enhanced stability and potent anti-inflammatory properties.

  2008cited by this paper
• Neutrophil secretion products pave the way for inflammatory monocytes.

  2008cited by this paper
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  2007cited by this paper
• JNK pathway: diseases and therapeutic potential

  2007cited by this paper
• Aspirin-Triggered Lipoxins Override the Apoptosis-Delaying Action of Serum Amyloid A in Human Neutrophils: A Novel Mechanism for Resolution of Inflammation1

  2007influential reference
• FPRL‐1 induces modifications of migration‐associated proteins in human neutrophils

  2006cited by this paper
• Cyclin-dependent kinase inhibitors enhance the resolution of inflammation by promoting inflammatory cell apoptosis

  2006cited by this paper
• The Lipoxin Receptor ALX: Potent Ligand-Specific and Stereoselective Actions in Vivo

  2006cited by this paper
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  2006cited by this paper
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  2004cited by this paper
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  2003cited by this paper
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  2003cited by this paper
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• Exaggerated Human Monocyte IL-10 Concomitant to Minimal TNF-α Induction by Heat-Shock Protein 27 (Hsp27) Suggests Hsp27 Is Primarily an Antiinflammatory Stimulus1

  2000cited by this paper
• Detection of beta 2-adrenergic receptor dimerization in living cells using bioluminescence resonance energy transfer (BRET).

  2000cited by this paper
• Oxidoreductases in Lipoxin A4 Metabolic Inactivation

  2000cited by this paper
• The chemokine monocyte chemoattractant protein-1 induces functional responses through dimerization of its receptor CCR2.

  1999cited by this paper
• Regulation of monocyte IL-10 synthesis by endogenous IL-1 and TNF-alpha: role of the p38 and p42/44 mitogen-activated protein kinases.

  1998influential reference
• Interleukin-1-induced intracellular signaling pathways converge in the activation of mitogen-activated protein kinase and mitogen-activated protein kinase-activated protein kinase 2 and the subsequent phosphorylation of the 27-kilodalton heat shock protein in monocytic cells.

  1994influential reference

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  2025cites this paper
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• ALX/FPR2 Receptor Activation by Inflammatory (fMLFII) and Pro-resolving (LXA4 and RvD3) Agonists

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  2025cites this paper
• FPR2 Agonism Attenuates Restenosis by Mitigating Neointimal Hyperplasia via ELOVL6

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• Formylpeptide receptors in GtoPdb v.2025.3

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• Lipoxins as Modulators of Diseases

  2025cites this paper
• Formylpeptide receptors in GtoPdb v.2025.1

  2025cites this paper
• Formyl peptide receptor modulators: a patent review and potential applications for inflammatory diseases (2021–2024)

  2025cites this paper
• Formylpeptide receptors: A novel target to treat cardiometabolic complications.

  2025cites this paper
• Advances in immunomodulation for organ transplantation: The role of the Annexin A1/FPR axis

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• Recent Advances in Studies of Serum Amyloid A: Implications in Inflammation, Immunity and Tumor Metastasis

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