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      Enigmatic Histamine Receptor H 4 for Potential Treatment of Multiple Inflammatory, Autoimmune, and Related Diseases

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          Abstract

          The histamine H 4 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 H 4R ligands are being studied for the treatment of several inflammatory, allergic, and autoimmune disorders, including pulmonary fibrosis. Activation of H 4R 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 H 4R acts as a modulator in cancer, neuropathic pain, vestibular disorders, and type-2 diabetes, however, its role is still not fully understood.

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          Coronavirus infections and immune responses

          Geng Li, Yaohua Fan, Yanni Lai … (2020)
          Abstract Coronaviruses (CoVs) are by far the largest group of known positive‐sense RNA viruses having an extensive range of natural hosts. In the past few decades, newly evolved Coronaviruses have posed a global threat to public health. The immune response is essential to control and eliminate CoV infections, however, maladjusted immune responses may result in immunopathology and impaired pulmonary gas exchange. Gaining a deeper understanding of the interaction between Coronaviruses and the innate immune systems of the hosts may shed light on the development and persistence of inflammation in the lungs and hopefully can reduce the risk of lung inflammation caused by CoVs. In this review, we provide an update on CoV infections and relevant diseases, particularly the host defense against CoV‐induced inflammation of lung tissue, as well as the role of the innate immune system in the pathogenesis and clinical treatment.
          Article 0 comments Cited 860 times – based on 0 reviews     Review now
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            Common activation mechanism of class A GPCRs

            Qingtong Zhou, Dehua Yang, Meng Chia Wu … (2019)
            Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human physiology. Understanding receptor activation mechanism is critical for discovering novel therapeutics since about one-third of all marketed drugs target members of this family. GPCR activation is an allosteric process that couples agonist binding to G-protein recruitment, with the hallmark outward movement of transmembrane helix 6 (TM6). However, what leads to TM6 movement and the key residue level changes of this movement remain less well understood. Here, we report a framework to quantify conformational changes. By analyzing the conformational changes in 234 structures from 45 class A GPCRs, we discovered a common GPCR activation pathway comprising of 34 residue pairs and 35 residues. The pathway unifies previous findings into a common activation mechanism and strings together the scattered key motifs such as CWxP, DRY, Na+ pocket, NPxxY and PIF, thereby directly linking the bottom of ligand-binding pocket with G-protein coupling region. Site-directed mutagenesis experiments support this proposition and reveal that rational mutations of residues in this pathway can be used to obtain receptors that are constitutively active or inactive. The common activation pathway provides the mechanistic interpretation of constitutively activating, inactivating and disease mutations. As a module responsible for activation, the common pathway allows for decoupling of the evolution of the ligand binding site and G-protein-binding region. Such an architecture might have facilitated GPCRs to emerge as a highly successful family of proteins for signal transduction in nature.
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              The Role of Histamine and Histamine Receptors in Mast Cell-Mediated Allergy and Inflammation: The Hunt for New Therapeutic Targets

              Elden Berla Thangam, Ebenezer Angel Jemima, Himadri Singh … (2018)
              Histamine and its receptors (H1R–H4R) play a crucial and significant role in the development of various allergic diseases. Mast cells are multifunctional bone marrow-derived tissue-dwelling cells that are the major producer of histamine in the body. H1R are expressed in many cells, including mast cells, and are involved in Type 1 hypersensitivity reactions. H2R are involved in Th1 lymphocyte cytokine production. H3R are mainly involved in blood–brain barrier function. H4R are highly expressed on mast cells where their stimulation exacerbates histamine and cytokine generation. Both H1R and H4R have important roles in the progression and modulation of histamine-mediated allergic diseases. Antihistamines that target H1R alone are not entirely effective in the treatment of acute pruritus, atopic dermatitis, allergic asthma, and other allergic diseases. However, antagonists that target H4R have shown promising effects in preclinical and clinical studies in the treatment of several allergic diseases. In the present review, we examine the accumulating evidence suggesting novel therapeutic approaches that explore both H1R and H4R as therapeutic targets for histamine-mediated allergic diseases.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Life (Basel)
                Journal ID (iso-abbrev): Life (Basel)
                Journal ID (publisher-id): life
                Title: Life
                Publisher: MDPI
                ISSN (Electronic): 2075-1729
                Publication date (Electronic): 24 April 2020
                Publication date Collection: April 2020
                Volume: 10
                Issue: 4
                Electronic Location Identifier: 50
                Affiliations
                [1 ]Faculty of Chemistry, Biological and Chemical Research Centre, University of Warsaw, 02-093 Warsaw, Poland or pakhurimehta@ 123456gmail.com (P.M.); pmiszta@ 123456chem.uw.edu.pl (P.M.)
                [2 ]Department of General and Experimental Pathology, Medical University of Warsaw, 02-091 Warsaw, Poland; przemyslaw.rzodkiewicz@ 123456wum.edu.pl
                [3 ]Łukasiewicz Research Network-Pharmaceutical Research Institute, 01-793 Warsaw, Poland; o.michalak@ 123456ifarm.eu (O.M.); p.krzeczynski@ 123456ifarm.eu (P.K.)
                Author notes
                Author information
                https://orcid.org/0000-0003-2317-273X
                https://orcid.org/0000-0002-1067-4223
                https://orcid.org/0000-0002-4978-5887
                https://orcid.org/0000-0003-3147-3858
                Article
                Publisher ID: life-10-00050
                DOI: 10.3390/life10040050
                PMC ID: 7235846
                PubMed ID: 32344736
                SO-VID: a3e38caf-c156-4975-a082-4da8d45ff3f3
                Copyright © © 2020 by the authors.
                License:

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                Date received : 31 March 2020
                Date accepted : 20 April 2020
                Categories
                Subject: Review

                Keywords: histamine h4 receptor,g protein-coupled receptors,allergic diseases,inflammatory diseases,autoimmune disorders,neuropathic pain,cancer
                Data availability:
                Keywords: histamine h4 receptor, g protein-coupled receptors, allergic diseases, inflammatory diseases, autoimmune disorders, neuropathic pain, cancer

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