Novel cyclic peptide constructs for targeted biomolecular imaging

Over 40 cyclic peptides are used in the clinic for a wide range of applications, such as somatostatin and ciclosporin. Cyclic peptides have enormous potential for disrupting protein-protein interactions and are therefore being pursued as drug candidates for treating a number of unmet medical needs. However, cyclisation of peptides remains a challenging synthetic process. This project seeks to achieve a breakthrough by developing a new grafting technique based on the use of metal chelators as a general method for cyclising peptides. The supervisor, Professor Zanda, is an expert of peptides and peptidomimetics for biomedical use, including therapy and imaging. Skills and competences acquired in this project will represent a major asset for a future career in medicinal chemistry, and drug design/development of peptide-based therapeutics and diagnostics.

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Full Project Detail
The macrocyclisation of peptides is an area of intense research which aims at the development of cyclo-peptide diagnostics, drug candidates and biological tools. Compared to their linear counterparts, cyclic peptides exhibit a restricted conformation, which can result in an increased binding affinity for their target receptor. They can also have reduced polarity and increased metabolic stability. Most existing methodologies to cyclise peptides heavily rely on the use of protecting groups and generally show low efficiency. The student will develop a new grafting technique based on the use of metal chelators as a general method for cyclising peptides. Bioactive peptide sequences will be synthesised, cyclised and functionalised with metal units carrying chemical groups enabling their use for biomedical imaging and – in perspective – for targeted therapy of human diseases, such as cancer. The resulting constructs will be tested for their biological activity.

Find out more:
https://www.lboro.ac.uk/science/study/postgraduate-research/studentships/

Entry requirements
Applicants should have, or expect to achieve, at least a 2:1 Honours degree (or equivalent) in organic chemistry or a related subject. A relevant Master’s degree and/or experience in one or more of the following will be an advantage: peptide synthesis/chemistry.

Contact details
Name: Professor Matteo Zanda
Email address: [Email Address Removed]

How to apply
All applications should be made online at http://www.lboro.ac.uk/study/apply/research/. Under programme name, select ‘Chemistry’.

Please quote reference number: MZ/CM/2019.