Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
Results
Showing 1 to 8 of 8 for “"macrocyclic peptides"”.
-
Directed Evolution of Macrocyclic Peptides For Inhibition of Autophagy
… Resistant (SUPR) mRNA display to develop macrocyclic peptides targeting the autophagy protein LC3. The resulting peptides bound LC3A and LC3B—two essential components of the autophagosome maturation machinery—with mid-nanomolar affinities and disrupted protein-protein interactions (PPIs) …
-
Cysteine arylation
… reactions are applied to the synthesis of macrocyclic peptides and antibody-drug conjugates (ADCs). Long unprotected macrocyclic peptides up to forty residues are efficiently synthesized using the GST enzyme. Using bispalladium reagents, macrocyclic peptides bearing aryl linkers are …
-
Palladium reagents for bioconjugation
… for a divergent macrocyclization of unprotected peptides by crosslinking two cysteine residues with bis-palladium organometallic reagents. These synthetic intermediates are prepared in a single step from commercially available aryl bis-halides. Two bioactive linear peptides with cysteine residues …
-
Applications of Hypervalent Iodine Reagents: From Enantioselective Copper-Catalysed Arylation-Semipinacol Cascade to Methionine Functionalisation for Peptide Macrocyclisation
… process for the macrocyclisation of native peptides via a non-natural linkage is developed. This study exploits previous work conducted in the group on the use of aryliodonium salts as methionine-selective diazoacetate transfer reagents. The functionalised methionine is in turn used for an …
-
Organometallic Palladium Reagents for Polypeptide Bioconjugation and Macrocyclization
Chapter 1: Bicyclic peptides have been developed to mimic good binders that structurally resemble antibody mimetics. The identity of the linker plays a critical role in enforcing the structure of the cyclic entity. Palladium-mediated arylation has enabled cysteine-specific modifications with a …
-
Stapling and Unstapling Peptides and Proteins With S-Tetrazine
… techniques to introduce s-tetrazine into peptides and proteins. The s-tetrazine molecule is effective for restricting peptides/proteins to macrocyclic conformations (i.e. stapling). Importantly, the incorporated s-tetrazine chromophore will undergo photodisassociation upon absorp-tion of a …
-
Peptide conjugation to enhance oligonucleotide delivery
… delivery, with hundreds of different peptides and modifications reported to improve cellular uptake. In this thesis, CPPs were systematically investigated and chemically altered to facilitate the delivery of antisense oligonucleotides. To accurately compare the existing CPPs, 64 CPP …
-
The synthesis of bimane constrained peptides and their fluorescent and structural properties
… protein-protein interactions however constrained peptides, have shown to have great therapeutic potential. Short peptides display little secondary structure in aqueous solution and as such, peptide sequences derived from a protein-protein interaction interface for use as a protein-protein …