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Optimisation of reduced-charge inhibitors for inositol monophosphatase and other phosphatases

Reference	B13490
Principal Investigator / Supervisor	Professor Rudolf Allemann
Co-Investigators / Co-Supervisors
Institution	University of Birmingham
Department	School of Chemistry
Funding type	Research
Value (£)	169,800
Status	Completed
Type	Research Grant
Start date	01/05/2000
End date	01/05/2003
Duration	36 months

Abstract

The 6-OH group of the substrate D-Ins 1-P H-bonds to a Mg2+2-bound water to activate it as an acid, and Mg2+1 activates the nucleophile. A new proposed mechanism accommodates all features of the new system and provides significant new insight. We now wish to synthesise and evaluate nine new classes of reduced charged inhibitors for IMPase using a knowledge of the mechanism and the role of the substrates 6-OH group. The most promising series will be optimised to provide inhibitors for IMPase and other related phosphatases. The information will extend our understanding, such that we can begin to address, the generic difficulties associated with designing low-charge phosphate group replacements. The work will also support X-ray crystallographic studies of the structure, mechanism and inhibition of IMPase and HAL2 through the provision of synthetic inhibitors and SAR data.

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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