{
  "abstract": "Kn2-7, an α-helical antimicrobial peptide, enhances the activation of mouse macrophage-like RAW264.7 cells in response to DNA containing unmethylated cytosine-guanine motifs (CpG DNA). We previously showed that high amphipathicity is an important determinant of the CpG DNA response-enhancing activity of short α-helical peptides. However, whether this principle applies to non-α-helical or larger amphipathic molecules is not clear. In the present study, polymyxin B (PMB), a non-α-helical amphipathic antimicrobial peptide, enhanced CpG DNA-induced activation of RAW264.7 cells, whereas PMB nonapeptide, which lacks the hydrophobic tail of PMB, did not. We also synthesized dimeric Kn2-7 peptides, Kn-Gly-Kn, Kn-(Gly)3-Kn, and Kn-(Gly)5-Kn, in which two Kn2-7 molecules are linked by one, three, or five glycine residues, respectively. Kn-(Gly)3-Kn and Kn-(Gly)5-Kn, but not Kn-Gly-Kn, retained CpG DNA response-enhancing activity. Peptide structure prediction using PEP-FOLD3 suggested that, in Kn-Gly-Kn, the hydrophobic faces of the two Kn2-7 domains are oriented toward each other, resulting in a less distinct overall amphipathic molecular organization. In contrast, the longer glycine linkers in Kn-(Gly)3-Kn and Kn-(Gly)5-Kn may increase conformational flexibility, allowing each α-helical Kn2-7 domain to function as an independent amphipathic unit. These findings suggest that amphipathic molecular organization is an important factor in enhancing CpG DNA-induced responses and that such enhancement can also occur with a non-α-helical peptide, as demonstrated for PMB.",
  "abstract_shown": true,
  "affiliations": [],
  "article_type": null,
  "arxiv": null,
  "author_total": 4,
  "authors": [
    {
      "name": "Saeka Nishihara"
    },
    {
      "name": "Eriko Maekawa"
    },
    {
      "name": "Hironori Katoh"
    },
    {
      "name": "Kiyoshi Kawasaki"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/6hraxzqhjm1vs.bib",
  "cited_by": 0,
  "doi": "10.1248/bpb.b26-00432",
  "fulltext_url": "https://www.jstage.jst.go.jp/article/bpb/49/10/49_b26-00432/_article",
  "id": "6hraxzqhjm1vs",
  "issns": [
    "1347-5215",
    "0918-6158"
  ],
  "landing_url": "https://www.jstage.jst.go.jp/article/bpb/49/10/49_b26-00432/_article",
  "language": null,
  "licence": "CC-BY-NC",
  "licence_label": "CC BY-NC",
  "licence_source": "journal",
  "licence_url": "https://creativecommons.org/licenses/by-nc/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "jstage-journal",
      "medicine/pharmacology-toxicology"
    ],
    [
      "openalex",
      "2403|Immune Response and Inflammation"
    ]
  ],
  "openalex": "W7222963284",
  "pdf_url": "https://www.jstage.jst.go.jp/article/bpb/49/10/49_b26-00432/_pdf",
  "pmcid": null,
  "pmid": null,
  "published": "2026-10-20",
  "publisher": null,
  "ris": "https://research.draconitic.com/paper/6hraxzqhjm1vs.ris",
  "sources": [
    {
      "first_seen": "2026-10-30T12:17:32Z",
      "native_id": "10.1248/bpb.b26-00432",
      "source": "jstage",
      "url": "https://www.jstage.jst.go.jp/article/bpb/49/10/49_b26-00432/_article"
    }
  ],
  "subjects": [
    {
      "field": "biology",
      "origin": "openalex:2403|Immune Response and Inflammation",
      "subfield": "immunology"
    }
  ],
  "title": "Structure–Activity Relationships of Glycine-Linked Kn2-7 Dimers and Polymyxin B-Related Peptides in the Enhancement of CpG DNA-Induced Macrophage Activation",
  "title_text": "Structure–Activity Relationships of Glycine-Linked Kn2-7 Dimers and Polymyxin B-Related Peptides in the Enhancement of CpG DNA-Induced Macrophage Activation",
  "type": "peer-reviewed",
  "updated_at": "2026-10-30T12:17:32Z",
  "url": "https://research.draconitic.com/paper/6hraxzqhjm1vs",
  "venue": "Biological and Pharmaceutical Bulletin",
  "versions": []
}