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Synthesis of bryostatin scaffold molecules and studies of their interactions with protein kinase C

Reference	B09691
Principal Investigator / Supervisor	Professor Karl Joseph Hale
Co-Investigators / Co-Supervisors	Professor Andy Gescher, Professor Gordon Roberts
Institution	University College London
Department	Chemistry
Funding type	Research
Value (£)	258,472
Status	Completed
Type	Research Grant
Start date	15/09/1998
End date	31/05/2002
Duration	45 months

Abstract

The ultimate aim of this project is to generate entirely novel and patentable anti- signalling drugs of potential use in the treatment of cancer. We propose to synthesise simplified analogues of the protein kinase C modulator bryostatin 1, and elucidate their mode of interaction with the enzyme to guide the synthesis of further analogues. Bryostatins, like phorbol esters, bind to cysteine-rich domains of PKC. We will define the 3D-solution structures of drug-PKC CRD complexes by high field NMR, and use this information to design other even more simplified yet highly potent PKC- modulators. These will be evaluated pharmacologically in animals in a subsequent study. Their cytostatic and cytotoxic effects in animals and cells will be determined, as will their immunostimulatory properties, and myalgic activity.

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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