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. Improving the binding affinity of in-vitro-evolved cyclic peptides by inserting atoms into the macrocycle backbone
 
research article

Improving the binding affinity of in-vitro-evolved cyclic peptides by inserting atoms into the macrocycle backbone

Wilbs, Jonas  
•
Middendorp, Simon J.  
•
Heinis, Christian  
2016
Chembiochem

Cyclic peptides binding to targets of interest can be generated efficiently with powerful in vitro display techniques, such as phage display or mRNA display. The cyclic peptide libraries screened with these methods are generated by altering in a combinatorial fashion the amino acid sequence of the peptides, the number of amino acids in the macrocycle rings, and the cyclization chemistry. A structural element that cannot easily be varied in the cyclic peptides is the backbone, which is built from amino acids, each of which contributes three atoms to the macrocyclic ring structure. Here, we proposed to improve the affinity of a phage-selected bicyclic peptide inhibitor of coagulation factor XII (FXII) by screening variants with one or two carbon atoms inserted into different positions of the backbone, and thus tapping into a structural space that was not sampled by phage display. Two mutants showed 4.7- and 2.5-fold improved K-i values. The better one blocked FXII with a Ki of 1.5 +/- 0.1 nm and inhibited activation of the intrinsic coagulation pathway (EC2x 1.7 mm). The strategy of ring size variation by one or several atoms should be generally applicable for the affinity maturation of in-vitro-evolved cyclic peptides.

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

Wilbs_ChemBioChem_2016_Preprint.pdf

Type

Preprint

Version

Submitted version (Preprint)

Access type

openaccess

Size

563.58 KB

Format

Adobe PDF

Checksum (MD5)

98db864ed25cbefac070ed5b290c6e90

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