Over the years, the Burgess group has been focusing on the preparation and
testing of small molecules that mimic protein secondary structures for protein-protein
interactions. The most successful compounds made are C10 peptide macrocycles that
effectively mimic β-turns and have given promising results from biological testing. These
peptide macrocycles have also been dimerized to give even more effective ligands for
protein-protein interaction.
The successes of the peptide macrocycles have enabled us to look into increasing
the chemical diversity of our libraries. This we believe will not only improve our ability
to obtain high affinity ligands for the receptors of interest, but will also allow us to
investigate other receptors. To achieve this, peptoids were incorporated into the C10
system to replace the peptides in the i+1 and i+2 positions. With the help of Microwave
irradiation, semi-peptoid macrocycles were synthesized with a total reaction time of less
than 2 h. These compounds were characterized and found to mimic β-turn, and show
promising biological activity towards the Insulin-like growth factor 1 receptor (IGF-IR).
| Identifer | oai:union.ndltd.org:tamu.edu/oai:repository.tamu.edu:1969.1/ETD-TAMU-1710 |
| Date | 02 June 2009 |
| Creators | Nnanabu, Ernest |
| Contributors | Burgess, Kevin |
| Source Sets | Texas A and M University |
| Language | en_US |
| Detected Language | English |
| Type | Book, Thesis, Electronic Thesis, text |
| Format | electronic, application/pdf, born digital |
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