| EPSRC Reference: |
EP/C000552/1 |
| Title: |
Tools for metallopeptide synthesis |
| Principal Investigator: |
Blower, Professor P |
| Other Investigators: |
|
| Researcher Co-Investigators: |
|
| Project Partners: |
|
| Department: |
Sch of Biosciences |
| Organisation: |
University of Kent |
| Scheme: |
Standard Research (Pre-FEC) |
| Starts: |
21 November 2004 |
Ends: |
20 November 2007 |
Value (£): |
211,406
|
| EPSRC Research Topic Classifications: |
| Biological & Medicinal Chem. |
Drug Formulation & Delivery |
| Medical science & disease |
|
|
| EPSRC Industrial Sector Classifications: |
| Healthcare |
Pharmaceuticals and Biotechnology |
|
| Related Grants: |
|
| Panel History: |
|
|
Summary on Grant Application Form |
|
The fastest growing class of radiopharmaceuticals for in vivo clinical imaging, and for targeted radionuclide therapy of cancer, are radiolabelled small peptides (e.g. octreotide). The conventional synthetic approach to these agents is to synthesise a peptide using solid phase methods, then attach a bifunctional molecule such as a metal chelator, either after cleavage from the resin (typically at a lysine side chain) or as the last step before cleavage. We propose that a far more flexible approach, providing potential for labelling at any specific location (for better control of biological properties of the conjugates) would be to design appropriate chelators containing pendant aminoacids, and incorporate them into the peptide during the solid phase synthesis. This approach would enable a chelator to be incorporated at any position (not just native lysines) whilst native lysines and the N-terminus could be unmodified. The chelator could be inserted in place of any aminoacid or in addition to the native ones. The approach would be better suited to combinatorial development of peptide based radiopharmaceuticals than conventional methods, because libraries of peptides incorporating chelators at a variety of locations could be radiolabelled quickly and easily with the appropriate radionuclide (the same as the one intended for the ultimate medical use, e.g. Tc, Cu, In) and subjected to high throughput screening. These tools would in the future be useful for building advanced materials containing ordered arrays of functional metal complexes exploiting the controllable secondary structures (alpha helix, beta sheet) of peptides.
|
|
Key Findings |
|
This information can now be found on Gateway to Research (GtR) http://gtr.rcuk.ac.uk
|
|
Potential use in non-academic contexts |
|
This information can now be found on Gateway to Research (GtR) http://gtr.rcuk.ac.uk
|
|
Impacts |
|
| Description |
This information can now be found on Gateway to Research (GtR) http://gtr.rcuk.ac.uk |
| Summary |
|
| Date Materialised |
|
|
|
|
Sectors submitted by the Researcher |
|
This information can now be found on Gateway to Research (GtR) http://gtr.rcuk.ac.uk
|
| Project URL: |
|
| Further Information: |
|
| Organisation Website: |
http://www.kent.ac.uk |