Repository logo

Infoscience

  • English
  • French
Log In
Logo EPFL, École polytechnique fédérale de Lausanne

Infoscience

  • English
  • French
Log In
  1. Home
  2. Academic and Research Output
  3. Journal articles
  4. De novo development of proteolytically resistant therapeutic peptides for oral administration
 
research article

De novo development of proteolytically resistant therapeutic peptides for oral administration

Kong, Xu-Dong  
•
Moriya, Jun
•
Carle, Vanessa  
Show more
May 11, 2020
Nature Biomedical Engineering

The oral administration of peptide drugs is hampered by their metabolic instability and limited intestinal uptake. Here, we describe a method for the generation of small target-specific peptides (less than 1,600 Da in size) that resist gastrointestinal proteases. By using phage display to screen large libraries of genetically encoded double-bridged peptides on protease-resistant fd bacteriophages, we generated a peptide inhibitor of the coagulation Factor XIa with nanomolar affinity that resisted gastrointestinal proteases in all regions of the gastrointestinal tract of mice after oral administration, enabling more than 30% of the peptide to remain intact, and small quantities of it to reach the blood circulation. We also developed a gastrointestinal-protease-resistant peptide antagonist for the interleukin-23 receptor, which has a role in the pathogenesis of Crohn's disease and ulcerative colitis. The de novo generation of targeted peptides that resist proteolytic degradation in the gastrointestinal tract should help the development of effective peptides for oral delivery.

  • Files
  • Details
  • Metrics
Loading...
Thumbnail Image
Name

Kong_et_al_Nature_Biomedical_Engineering_2020_Preprint.pdf

Type

Preprint

Version

http://purl.org/coar/version/c_71e4c1898caa6e32

Access type

embargo

Embargo End Date

2020-11-11

License Condition

CC BY

Size

1.82 MB

Format

Adobe PDF

Checksum (MD5)

af10dafef1199570d496ed22a803fcc3

Logo EPFL, École polytechnique fédérale de Lausanne
  • Contact
  • infoscience@epfl.ch

  • Follow us on Facebook
  • Follow us on Instagram
  • Follow us on LinkedIn
  • Follow us on X
  • Follow us on Youtube
AccessibilityLegal noticePrivacy policyCookie settingsEnd User AgreementGet helpFeedback

Infoscience is a service managed and provided by the Library and IT Services of EPFL. © EPFL, tous droits réservés