Topoisomeric membrane-active peptides: A review of the last two decades

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  • dc.contributor.author Carrera-Aubesart, Adam
  • dc.contributor.author Gallo, María, 1989-
  • dc.contributor.author Defaus, Sira
  • dc.contributor.author Todorovski, Toni
  • dc.contributor.author Andreu Martínez, David
  • dc.date.accessioned 2023-12-04T07:19:56Z
  • dc.date.available 2023-12-04T07:19:56Z
  • dc.date.issued 2023
  • dc.description.abstract In recent decades, bioactive peptides have been gaining recognition in various biomedical areas, such as intracellular drug delivery (cell-penetrating peptides, CPPs) or anti-infective action (antimicrobial peptides, AMPs), closely associated to their distinct mode of interaction with biological membranes. Exploiting the interaction of membrane-active peptides with diverse targets (healthy, tumoral, bacterial or parasitic cell membranes) is opening encouraging prospects for peptides in therapeutics. However, ordinary peptides formed by L-amino acids are easily decomposed by proteases in biological fluids. One way to sidestep this limitation is to use topoisomers, namely versions of the peptide made up of D-amino acids in either canonic (enantio) or inverted (retroenantio) sequence. Rearranging peptide sequences in this fashion provides a certain degree of native structure mimicry that, in appropriate contexts, may deliver desirable biological activity while avoiding protease degradation. In this review, we will focus on recent accounts of membrane-active topoisomeric peptides with therapeutic applications as CPP drug delivery vectors, or as antimicrobial and anticancer candidates. We will also discuss the most common modes of interaction of these peptides with their membrane targets.
  • dc.description.sponsorship Work supported by funds from the La Caixa Health Foundation (project HR17_00409) and European Union (H2020-FETOPEN-2018-2019-2020-01 grant No. 828774).
  • dc.format.mimetype application/pdf
  • dc.identifier.citation Carrera-Aubesart A, Gallo M, Defaus S, Todorovski T, Andreu D. Topoisomeric membrane-active peptides: A review of the last two decades. Pharmaceutics. 2023 Oct 12;15(10):2451. DOI: 10.3390/pharmaceutics15102451
  • dc.identifier.doi http://dx.doi.org/10.3390/pharmaceutics15102451
  • dc.identifier.issn 1999-4923
  • dc.identifier.uri http://hdl.handle.net/10230/58433
  • dc.language.iso eng
  • dc.publisher MDPI
  • dc.relation.ispartof Pharmaceutics. 2023 Oct 12;15(10):2451
  • dc.relation.projectID info:eu-repo/grantAgreement/EC/H2020/828774
  • dc.rights © 2023 by the authors. 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 (https://creativecommons.org/licenses/by/4.0/).
  • dc.rights.accessRights info:eu-repo/semantics/openAccess
  • dc.rights.uri http://creativecommons.org/licenses/by/4.0/
  • dc.subject.keyword Anticancer peptides
  • dc.subject.keyword Antimicrobial peptides
  • dc.subject.keyword Cell-penetrating peptides
  • dc.subject.keyword Enantio
  • dc.subject.keyword Membrane-active peptides
  • dc.subject.keyword Retro
  • dc.subject.keyword Retroenantio
  • dc.subject.keyword Topoisomery
  • dc.title Topoisomeric membrane-active peptides: A review of the last two decades
  • dc.type info:eu-repo/semantics/article
  • dc.type.version info:eu-repo/semantics/publishedVersion