Multiple sensor-containing active modified polypeptides, preparation and uses thereof
OwnerTom Muir, Graham Cottoninventors
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Abstract
Compositions and methods are provided for identifying conformational changes in polypeptides related to the activity or biological state of the polypeptide. Semisynthetic polypeptides are prepared comprising at least two proximity-sensor peptides, the resultant composition capable of detectably indicating the activity of biological state of the polypeptide. Such compositions may be used to identify modulators of the polypeptides as well as modulators of molecules which interact with the polypeptide, such as protein kinases which act on protein kinase targets.
Claims19
1-50. (canceled)
A composition for detecting the effect of an enzyme on a peptide substrate, the activity of said enzyme being effective to convert said peptide substrate, w/o cleavage, from an unmodified state to a modified state, said composition comprising a functional peptide substrate for said enzyme, having a first detectable proximity-sensor peptide incorporated into a first position of said substrate and a second detectable proximity-sensor peptide incorporated into a second position of said substrate, thereby providing a semi-synthetic multiple labeled polypeptide substrate having a first structural conformation in said unmodified state and a second structural conformation in said modified state, said proximity sensors being spaced apart in said first structural conformation at a distance which is characteristic of said unmodified state and being spaced apart in said second structural conformation at a distance which is characteristic of said modified state, detection of one of said structural conformations being indicative of the effect of said enzyme on said substrate.
The composition as shown in SEQ ID NO:
- 9.
Dependencies are inferred from the claim text.