Old Polyanionic Drug Suramin Suppresses Detrimental Cytotoxicity of the Host Defense Peptide LL-37

Mayra Quemé-Peña, Maria Ricci, Tünde Juhász, Kata Horváti, Szilvia Bösze, Beáta Biri-Kovács, Bálint Szeder, Ferenc Zsila, Tamás Beke-Somfai (Lead / Corresponding author)

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)


The host defense peptide LL-37 is the only human cathelicidin, characterized by pleiotropic activity ranging from immunological to anti-neoplastic functions. However, its overexpression has been associated with harmful inflammatory responses and apoptosis. Thus, for the latter cases, the development of strategies aiming to reduce LL-37 toxicity is highly desired as these have the potential to provide a viable solution. Here, we demonstrate that the reduction of LL-37 toxicity might be achieved by the impairment of its cell surface binding through interaction with small organic compounds that are able to alter the peptide conformation and minimize its cell penetration ability. In this regard, the performed cell viability and internalization studies showed a remarkable attenuation of LL-37 cytotoxicity toward colon and monocytic cells in the presence of the polysulfonated drug suramin. The mechanistic examinations of the molecular details indicated that this effect was coupled with the ability of suramin to alter LL-37 secondary structure via the formation of peptide-drug complexes. Moreover, a comparison with other therapeutic agents having common features unveiled the peculiar ability of suramin to optimize the binding to the peptide sequence. The newly discovered suramin action is hoped to inspire the elaboration of novel repurposing strategies aimed to reduce LL-37 cytotoxicity under pathological conditions.

Original languageEnglish
Pages (from-to)155-167
Number of pages13
JournalACS Pharmacology and Translational Science
Issue number1
Early online date3 Dec 2020
Publication statusPublished - 12 Feb 2021


  • cathelicidins
  • helical folding
  • molecular mechanisms
  • reduced cytotoxicity
  • suramin

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology


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