Enigmatic Histamine Receptor H4 for Potential Treatment of Multiple Inflammatory, Autoimmune, and Related Diseases
Open Access
- 23 April 2020
- Vol. 10 (4), 50
- https://doi.org/10.3390/life10040050
Abstract
The histamine H4 receptor, belonging to the family of G-protein coupled receptors, is an increasingly attractive drug target. It plays an indispensable role in many cellular pathways, and numerous H4R ligands are being studied for the treatment of several inflammatory, allergic, and autoimmune disorders, including pulmonary fibrosis. Activation of H4R is involved in cytokine production and mediates mast cell activation and eosinophil chemotaxis. The importance of this receptor has also been shown in inflammatory models: peritonitis, respiratory tract inflammation, colitis, osteoarthritis, and rheumatoid arthritis. Recent studies suggest that H4R acts as a modulator in cancer, neuropathic pain, vestibular disorders, and type-2 diabetes, however, its role is still not fully understood.Keywords
Funding Information
- National Science Centre, Poland (OPUS 2017/25/B/NZ7/02788)
This publication has 99 references indexed in Scilit:
- Combinatorial roles for histamine H1‐H2 and H3‐H4 receptors in autoimmune inflammatory disease of the central nervous systemEuropean Journal of Immunology, 2012
- Role of H4 receptor in histamine-mediated responses in human melanomaMelanoma Research, 2011
- Agonist-Biased Signaling at the Histamine H4 Receptor: JNJ7777120 Recruits β-Arrestin without Activating G ProteinsMolecular Pharmacology, 2010
- Copy number variations of the human histamine H4 receptor gene are associated with systemic lupus erythematosusBritish Journal of Dermatology, 2010
- Molecular Determinants of Ligand Binding to H4R Species VariantsMolecular Pharmacology, 2010
- Characterization of histamine H3 receptors in Alzheimer's Disease brain and amyloid over‐expressing TASTPM miceBritish Journal of Pharmacology, 2009
- Role of histamine H4 receptor in breast cancer cell proliferationFrontiers in Bioscience-Elite, 2009
- Binding mode analysis and enrichment studies on homology models of the human histamine H4 receptorEuropean Journal of Medicinal Chemistry, 2008
- Decreased expression of histamine H1 and H4 receptors suggests disturbance of local regulation in human colorectal tumours by histamineEuropean Journal of Cell Biology, 2008
- Construction of a sequence motif characteristic of aminergic G protein–coupled receptorsProtein Science, 2003