An efficient mRNA display protocol yields potent bicyclic peptide inhibitors for FGFR3c: outperforming linear and monocyclic formats in affinity and stability-Reference-Cited by-同舟云学术

An efficient mRNA display protocol yields potent bicyclic peptide inhibitors for FGFR3c: outperforming linear and monocyclic formats in affinity and stability

Published:2024 Issue:16 Volume:15 Page:6122-6129
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Villequey Camille¹^ORCID,Zurmühl Silvana S.¹,Cramer Christian N.¹^ORCID,Bhusan Bhaskar²,Andersen Birgitte³,Ren Qianshen⁴,Liu Haimo⁴,Qu Xinping⁴,Yang Yang⁴,Pan Jia⁴,Chen Qiujia⁴,Münzel Martin¹

Affiliation:

1. Global Research Technologies, Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark

2. Department of Chemistry, Oxford University, Chemistry Research Laboratory, 12 Mansfield Road, Oxford, UK

3. Global Drug Discovery, Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark

4. Novo Nordisk Research Center China, Novo Nordisk A/S, Shengmingyuan West Ring Rd, Changping District, Beijing, China

Abstract

This work presents an efficient mRNA display protocol for making large libraries of bicyclic peptides and evaluating their performance vs. linear and monocyclic formats for affinity, specificity & plasma stability in a selection against FGFR3c.

Publisher

Royal Society of Chemistry (RSC)

Link

http://pubs.rsc.org/en/content/articlepdf/2024/SC/D3SC04763F

Reference40 articles.

1. How proteins bind macrocycles

2. Chemical Modifications Designed to Improve Peptide Stability: Incorporation of Non-Natural Amino Acids, Pseudo-Peptide Bonds, and Cyclization

3. Orally Active Peptides: Is There a Magic Bullet?

4. Understanding Cell Penetration of Cyclic Peptides

5. Macrocyclic Peptides as Drug Candidates: Recent Progress and Remaining Challenges

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