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Synthesis of substrates and inhibitors for the Ser-Thr protein phosphatases 1 and 2A and their use in kinetic mechanistic and structural studies

ReferenceB07992
Principal Investigator / Supervisor Professor David Gani
Co-Investigators /
Co-Supervisors
Institution University of Birmingham
DepartmentSchool of Chemistry
Funding typeResearch
Value (£) 160,554
StatusCompleted
TypeResearch Grant
Start date 11/08/1997
End date 11/10/2000
Duration38 months

Abstract

A programme to delineate the kinetics, substrate specificity, mechanism and inhibition of ser- thr protein phosphatases PP1 and PP2A is outlined. Initially we will probe the determinants for inhibition by synthetic nodularins and microcystins, prepared using in-house solution and solid-phase techniques in order to establish inhibitor SARs quickly. A major objective is to identify specific inhibitors which would be valuable biochemical tools in elucidating the role of specific PPs in vivo. A new reliable activity assay based upon 14C-labelled phosphorylated peptides will be used to gain the first quantitative kinetic information on substrate specificity (for each enzyme), allow the binding/debinding order of various species to be determined and allow the chemical mechanism for phosphoryl transfer to be probed.

Summary

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