Genetically-encoded discovery of proteolytically stable bicyclic inhibitors for morphogen NODAL

Author:

Wong Jeffrey Y.-K.1234ORCID,Mukherjee Raja1234,Miao Jiayuan1567ORCID,Bilyk Olena8234,Triana Vivian1234,Miskolzie Mark1234,Henninot Antoine9107,Dwyer John J.9107,Kharchenko Serhii111213,Iampolska Anna111213,Volochnyuk Dmitriy M.111213,Lin Yu-Shan1567ORCID,Postovit Lynne-Marie8234,Derda Ratmir1234ORCID

Affiliation:

1. Department of Chemistry

2. University of Alberta

3. Edmonton

4. Canada

5. Tufts University

6. Medford

7. USA

8. Department of Experimental Oncology

9. Ferring Research Institute

10. San Diego

11. Enamine Ltd.

12. Kyiv 02094

13. Ukraine

Abstract

A two-fold symmetric linchpin (TSL) converts readily available phage-displayed disulfide peptide libraries to proteolytically stable bicyclic peptides. The bicyclic phage library was screened to discover an antagonist of NODAL morphogen.

Funder

Ferring Research Institute

Natural Sciences and Engineering Research Council of Canada

Canadian Institutes of Health Research

National Institutes of Health

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

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