Chemical synthesis and biological evaluation of conotoxin peptides

Lead Research Organisation: University of Glasgow
Department Name: School of Chemistry

Abstract

Peptides derived from natural sources are useful lead compounds to develop therapeutics. The structural diversity of naturally occurring peptides covers a large section of chemical space that sits between more traditional small molecules (<500 daltons) and biologics (typically proteins). Peptides typically have excellent selectivity and binding affinity for their targets. However, they have physicochemical issues that limit their development as drugs. These include poor blood plasma stability due to proteolytic degradation and limited bioavailability because they are unable to cross membrane structures, due to their inherent polarity. The Jamieson Group's ongoing research program (Chem. Sci., 2019, 10, 1671) is focused on the development of new peptidomimetic chemistries that can be used to overcome the physicochemical limitations of peptides and facilitate peptide drug discovery. This is achieved by chemically modifying the peptide structure; removing the vulnerable functionality and introducing chemical mimic structures to retain the overall 3-dimensional structure of the peptide. Using these synthetic molecules we are investigating the nature of molecular recognition between conotoxins and the nicotinic acetylcholine receptor (nAChR).

Publications

10 25 50

Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/R513222/1 30/09/2018 29/09/2023
2607113 Studentship EP/R513222/1 30/09/2021 30/03/2025 Kirsty Arnott
EP/T517896/1 30/09/2020 29/09/2025
2607113 Studentship EP/T517896/1 30/09/2021 30/03/2025 Kirsty Arnott