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Design synthesis and structural studies of inhibitors of metallo-beta-lactamases

Reference	B13539
Principal Investigator / Supervisor	Professor Gordon Roberts
Co-Investigators / Co-Supervisors	Professor Mike Page, Professor Christopher Joseph Schofield
Institution	University of Leicester
Department	Biological NMR Centre
Funding type	Research
Value (£)	337,516
Status	Completed
Type	Research Grant
Start date	01/10/2000
End date	31/12/2003
Duration	39 months

Abstract

Metallo-beta-lactamases (MBLs) form a unique enzyme family, resistant to all inhibitors of serine- beta-lactamases; the spread of MBL-mediated bacterial resistance threatens the effectiveness of all beta-lactam antibiotics. Our aim is to design and synthesise novel substrate analogues and inhibitors of MBLs and to characterise their interaction with the enzyme kinetically and by determining the structures of their complexes by NMR. Particular emphasis will be placed on (i) the role of the two active site zincs in binding and catalysis, and (ii) the importance of mobile loops in the active site in determining substrate and inhibitor specificity. The information obtained will contribute directly to the design of new broad-spectrum MBL inhibitors.

Summary

unavailable

Committee	Closed Committee - Biomolecular Sciences (BMS)
Research Topics	X – not assigned to a current Research Topic
Research Priority	X – Research Priority information not available
Research Initiative	X - not in an Initiative
Funding Scheme	X – not Funded via a specific Funding Scheme

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