Novel treatment
AssigneeSmithKline Beecham Corporation
InventorsGary Christie, Ishrut Hussain, David J. Powell
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Abstract
A method of screening compounds to identify those compounds which inhibit the Asp 1 mediated cleavage of a polypeptide or protein substrate, the method comprising: providing a reaction system comprising Asp 1 and substrate; and measuring the extent of cleavage of the substrate in the presence of test compound as compared with the extent of cleavage in the absence of test compound, and compounds identified thereby as well as compounds which are inhibitors of Asp 1 modulated APP cleavage and their use in therapy including the treatment or prophylaxis of β amyloid protein-related disease including AD.
Claims19
A method of screening compounds to identify those compounds which inhibit the Asp 1 mediated cleavage of a polypeptide or protein substrate, the method comprising:
- providing a reaction system comprising Asp 1 and substrate;
- and measuring the extent of cleavage of the substrate in the presence of test compound as compared with the extent of cleavage in the absence of test compound.
A method according to any preceding claim which is a cell based assay comprising a host cell cotransfected with expression vectors containing DNA encoding Asp 1 and the substrate, and the presence of the cleavage products is detected by assaying the protein content of the host cell by using polyclonal or monoclonal antibodies raised against substrate fragments.
A method of screening compounds to identify those compounds which inhibit the Asp 1 mediated cleavage of a polypeptide or protein substrate, the method comprising:
- providing a reaction system comprising Asp 1 and labelled active site ligand;
- and measuring the extent of binding of labelled ligand in the presence of test compound as compared with the extent of binding of labelled ligand in the absence of test compound in order to determine binding affinity.
A compound which is an inhibitor of Asp 1 modulated APP cleavage.
Dependencies are inferred from the claim text.