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research article

De novo development of proteolytically resistant therapeutic peptides for oral administration

Kong, Xu-Dong  
•
Moriya, Jun
•
Carle, Vanessa  
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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.

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Type
research article
DOI
10.1038/s41551-020-0556-3
Web of Science ID

WOS:000531760800001

Author(s)
Kong, Xu-Dong  
Moriya, Jun
Carle, Vanessa  
Pojer, Florence  
Abriata, Luciano A.  
Deyle, Kaycie  
Heinis, Christian  
Date Issued

2020-05-11

Published in
Nature Biomedical Engineering
Volume

4

Start page

560

End page

571

Subjects

Engineering, Biomedical

•

Engineering

•

stability

•

delivery

•

selection

•

protein

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
LPPT  
UPCOL  
FunderGrant Number

FNS

157842

FNS-NCCR

NCCR Chemical Biology

FNS

169526

Available on Infoscience
May 24, 2020
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/168916
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