Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification

A chemoselective peptide functionalisation strategy via photocatalytic tryptophan (Trp) modification has been developed. The versatility of the reaction is demonstrated by tethering a variety of difluoroalkyl groups to Trp using an organic photocatalyst and short irradiation times with visible light...

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Main Author: Lee, Joanna
Format: Thesis (University of Nottingham only)
Language:English
Published: 2024
Subjects:
Online Access:https://eprints.nottingham.ac.uk/78245/
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author Lee, Joanna
author_facet Lee, Joanna
author_sort Lee, Joanna
building Nottingham Research Data Repository
collection Online Access
description A chemoselective peptide functionalisation strategy via photocatalytic tryptophan (Trp) modification has been developed. The versatility of the reaction is demonstrated by tethering a variety of difluoroalkyl groups to Trp using an organic photocatalyst and short irradiation times with visible light. Due to the mild and biocompatible reaction conditions, a range of complex peptides have been successfully functionalised to give a diverse library of small molecule-peptide conjugates. Results have confirmed site-selectivity for Trp in the presence of other amino acids, illustrating that this transformation can expand the field of chemoselective photo-bioconjugation. Applications of the methodology have been explored including protein modification and peptide stapling. For the latter, incorporation of the bromodifluorocarbonyl moiety into the peptide sequence during solid phase peptide synthesis (SPPS), enabled the synthesis of macrocyclic peptides.
first_indexed 2025-11-14T21:01:28Z
format Thesis (University of Nottingham only)
id nottingham-78245
institution University of Nottingham Malaysia Campus
institution_category Local University
language English
last_indexed 2025-11-14T21:01:28Z
publishDate 2024
recordtype eprints
repository_type Digital Repository
spelling nottingham-782452024-07-24T04:43:55Z https://eprints.nottingham.ac.uk/78245/ Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification Lee, Joanna A chemoselective peptide functionalisation strategy via photocatalytic tryptophan (Trp) modification has been developed. The versatility of the reaction is demonstrated by tethering a variety of difluoroalkyl groups to Trp using an organic photocatalyst and short irradiation times with visible light. Due to the mild and biocompatible reaction conditions, a range of complex peptides have been successfully functionalised to give a diverse library of small molecule-peptide conjugates. Results have confirmed site-selectivity for Trp in the presence of other amino acids, illustrating that this transformation can expand the field of chemoselective photo-bioconjugation. Applications of the methodology have been explored including protein modification and peptide stapling. For the latter, incorporation of the bromodifluorocarbonyl moiety into the peptide sequence during solid phase peptide synthesis (SPPS), enabled the synthesis of macrocyclic peptides. 2024-07-24 Thesis (University of Nottingham only) NonPeerReviewed application/pdf en cc_by https://eprints.nottingham.ac.uk/78245/1/Lee%20Joanna%2014249733%20Corrections.pdf Lee, Joanna (2024) Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification. PhD thesis, University of Nottingham. peptides peptide functionalisation biomolecules
spellingShingle peptides
peptide functionalisation
biomolecules
Lee, Joanna
Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification
title Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification
title_full Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification
title_fullStr Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification
title_full_unstemmed Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification
title_short Photocatalytic Tryptophan Alkylation for Chemoselective Peptide Modification
title_sort photocatalytic tryptophan alkylation for chemoselective peptide modification
topic peptides
peptide functionalisation
biomolecules
url https://eprints.nottingham.ac.uk/78245/