ArticleCells2019
Small-Molecule Host-Defense Peptide Mimetic Antibacterial and Antifungal Agents Activate Human and Mouse Mast Cells via Mas-Related GPCRs.
Article in Cells, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
15 citing papers in PubMed, 30 citations in OpenAlex.
- Mutations ofThe journal of allergy and clinical immunology. Global · 2025Review
- Synthetic peptides targeting a mast cell-specific G protein-coupled receptor MRGPRB2 display anti-infective potential.Cell biomaterials · 2025Article
- Antimicrobial Peptide Signaling in Skin Diseases.JID innovations : skin science from molecules to population health · 2025Review
- The development of murine bone marrow-derived mast cells expressing functional human MRGPRX2 forFrontiers in immunology · 2024Article
- Mast cell MrgprB2 in neuroimmune interaction in IgE-mediated airway inflammation and its modulation by β-arrestin2.Frontiers in immunology · 2024Article
- Role of MrgprB2 in Rosacea-Like Inflammation in Mice: Modulation by β-Arrestin 2.The Journal of investigative dermatology · 2022Article
- Guanidine-Containing Antifungal Agents against Human-Relevant Fungal Pathogens (2004-2022)-A Review.Journal of fungi (Basel, Switzerland) · 2022Review
- Inhibition of MRGPRX2 but not FcεRI or MrgprB2-mediated mast cell degranulation by a small molecule inverse receptor agonist.Frontiers in immunology · 2022Article
- Multifaceted MRGPRX2: New insight into the role of mast cells in health and disease.The Journal of allergy and clinical immunology · 2021Review
- The Multifaceted Mas-Related G Protein-Coupled Receptor Member X2 in Allergic Diseases and Beyond.International journal of molecular sciences · 2021Review
- MRGPRX2 Activation by Rocuronium: Insights from Studies with Human Skin Mast Cells and Missense Variants.Cells · 2021Article
- Inhibition of Orai Channel Function Regulates Mas-Related G Protein-Coupled Receptor-Mediated Responses in Mast Cells.Frontiers in immunology · 2021Article
- Murepavadin, a Small Molecule Host Defense Peptide Mimetic, Activates Mast CellsFrontiers in immunology · 2021Article
- Roles of a Mast Cell-Specific Receptor MRGPRX2 in Host Defense and Inflammation.Journal of dental research · 2020Article
- Inhibitory Effects of AF-343, a Mixture ofMolecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Host-defense peptides (HDPs) have an important therapeutic potential against microbial infections but their metabolic instability and cellular cytotoxicity have limited their utility. To overcome these limitations, we utilized five small-molecule, nonpeptide HDP mimetics (smHDPMs) and tested their effects on cytotoxicity, antimicrobial activity, and mast cell (MC) degranulation. None of the smHDPMs displayed cytotoxicity against mouse 3T3 fibroblasts or human transformed liver HepG2 cells. However, one compound had both antifungal and antibacterial activity. Surprisingly, all five compounds induced degranulation in a human MC line, LAD2, and this response was substantially reduced in Mas-related G protein-coupled receptor (GPCR)-X2 (MRGPRX2)-silenced cells. Furthermore, all five compounds induced degranulation in RBL-2H3 cells expressing MRGPRX2 but this response was abolished in cells expressing naturally occurring loss-of-function missense variants G165E (rs141744602) and D184H (rs372988289). Mrgprb2 is the likely mouse ortholog of human MRGPRX2, which is expressed in connective tissue MCs (CTMCs) such as cutaneous and peritoneal MCs (PMCs). All five smHDPMs induced degranulation in wild-type PMCs but not in cells derived from Mrgprb2⁻/⁻ mice. These findings suggest that smHDPMs could serve as novel targets for the treatment of drug-resistant fungal and bacterial infections because of their ability to harness CTMCs' host defense functions.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.