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Tuning protein half-life in mouse using sequence-defined biopolymers functionalized with lipids

Koen Vanderschuren, Pol Arranz‐Gibert, Minsoo Khang, Hadar Dagan, Alice Gaudin, Fan Yang, Ewa Folta‐Stogniew, W. Mark Saltzman, Miriam Amiram, Farren J. Isaacs

2022Proceedings of the National Academy of Sciences35 citationsDOIOpen Access PDF

Abstract

-azidophenylalanine (pAzF). Precise lipidation of these pAzF residues generated a set of sequence-defined synthetic biopolymers with programmable binding affinity to albumin without ablating the activity of model fusion proteins, and with tunable blood serum half-lives spanning 5 to 94% of albumin's half-life in a mouse model. Our findings present a proof of concept for the use of genetically encoded bioorthogonal conjugation sites for multisite lipidation to tune protein stability in mouse serum. This work establishes a programmable approach to extend and tune the half-life of protein or peptide therapeutics and a technical foundation to produce functionalized biopolymers endowed with programmable chemical and biophysical properties with broad applications in medicine, materials science, and biotechnology.

Topics & Concepts

Bioorthogonal chemistrySurface modificationChemical modificationAmino acidChemistryPosttranslational modificationBiochemistryCombinatorial chemistryPeptideChemical synthesisSequence (biology)EnzymeClick chemistryIn vitroPhysical chemistryChemical Synthesis and AnalysisMonoclonal and Polyclonal Antibodies ResearchClick Chemistry and Applications
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