EPSRC Reference: |
GR/M74696/01 |
Title: |
NOVEL APPROACHES TO LACTACYSTIN & ITS ANALOGUES |
Principal Investigator: |
Hayes, Professor CJ |
Other Investigators: |
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Researcher Co-Investigators: |
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Project Partners: |
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Department: |
Sch of Chemistry |
Organisation: |
University of Nottingham |
Scheme: |
Standard Research (Pre-FEC) |
Starts: |
06 October 1999 |
Ends: |
05 October 2002 |
Value (£): |
52,702
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EPSRC Research Topic Classifications: |
Biological & Medicinal Chem. |
Chemical Synthetic Methodology |
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EPSRC Industrial Sector Classifications: |
Pharmaceuticals and Biotechnology |
No relevance to Underpinning Sectors |
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Related Grants: |
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Panel History: |
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Summary on Grant Application Form |
The natural product lactacystin was discovered because of its ability to induce neurite outgrowth in the murine neuroblastoma cell line Neuro-2a and it was later shown that lactacystin was an inhibitor of the 20S proteasome. The proteasome is a multi-subunit protein present in most cell types and is responsible for the degradation of most cellular proteins. It is involved in a large number of cellular processes including cell cycle control, cell differentiation and the immune response. Because of this biological activity there is much interest in developing therapeutics based upon the structure of lactacystin. Our research will involve developing novel synthetic methodology for the rapid synthesis of lactacystin and a range of designed structural analogues which may be of therapeutic value. We plan to use a regio- and stereoselective alkylidene carbene-mediated 1, 5 C-H insertion reaction as the key stratagem for the asymmetric synthesis of the a, a -dialkyl-a-amino acid moiety present in lactacystin.
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Key Findings |
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Potential use in non-academic contexts |
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Impacts |
Description |
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Summary |
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Date Materialised |
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Sectors submitted by the Researcher |
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Project URL: |
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Further Information: |
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Organisation Website: |
http://www.nottingham.ac.uk |