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  • Carle, VanessaInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)

Development of Selective FXIa Inhibitors Based on Cyclic Peptides and Their Application for Safe Anticoagulation

  • Article/chapterEnglish2021

Publisher, publication year, extent ...

  • 2021-05-11
  • American Chemical Society (ACS),2021
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:umu-186256
  • https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-186256URI
  • https://doi.org/10.1021/acs.jmedchem.1c00056DOI

Supplementary language notes

  • Language:English
  • Summary in:English

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  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • Coagulation factor XI (FXI) has emerged as a promising target for the development of safer anticoagulation drugs that limit the risk of severe and life-threatening bleeding. Herein, we report the first cyclic peptide-based FXI inhibitor that selectively and potently inhibits activated FXI (FXIa) in human and animal blood. The cyclic peptide inhibitor (Ki = 2.8 ± 0.5 nM) achieved anticoagulation effects that are comparable to that of the gold standard heparin applied at a therapeutic dose (0.3-0.7 IU/mL in plasma) but with a substantially broader estimated therapeutic range. We extended the plasma half-life of the peptide via PEGylation and demonstrated effective FXIa inhibition over extended periods in vivo. We validated the anticoagulant effects of the PEGylated inhibitor in an ex vivo hemodialysis model with human blood. Our work shows that FXI can be selectively targeted with peptides and provides a promising candidate for the development of a safe anticoagulation therapy.

Subject headings and genre

Added entries (persons, corporate bodies, meetings, titles ...)

  • Wu, YutengInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Mukherjee, RakeshInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Kong, Xu-DongInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Rogg, ChloéInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Laurent, QuentinInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Cecere, EnzaInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Villequey, CamilleInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Konakalla, Madhuree S.Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Maric, TamaraInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Lamers, ChristinaInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Díaz-Perlas, CristinaInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Butler, KaycieInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Goto, JunkoUmeå universitet,Avdelningen för medicin(Swepub:umu)jugo0005 (author)
  • Stegmayr, Bernd,1949-Umeå universitet,Avdelningen för medicin(Swepub:umu)best0006 (author)
  • Heinis, ChristianInstitute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland (author)
  • Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, SwitzerlandAvdelningen för medicin (creator_code:org_t)

Related titles

  • In:Journal of Medicinal Chemistry: American Chemical Society (ACS)64:10, s. 6802-68130022-26231520-4804

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