Rapid screening method for effectors of signal transduction
AssigneeTerrapin Technologies, Inc.
InventorsDaria Mochly-Rosen, Dorit Ron, Lawrence M. Kauvar, Eugene W. Napolitano
Life of this patent
Estimating the term…
Abstract
Methods for assessing libraries of candidate modulators of intracellular signaling transmission pathways are described. The methods assess the ability of candidates from the library to inhibit the binding of peptides which represent participants in the signaling pathways as either a signal-generating protein or its cognate partner binding at a noncatalytic site. Specific peptides useful in this regard have been identified.
Claims12
A method to ascertain a modulator of intracellular signal transduction mediated by the signal-generating protein, protein kinase C (PKC), from a library of candidate molecules, which method comprises
- providing the cognate receptor for activated kinase C (RACK) or a peptide derived from said PKC or the cognate RACK which binds specifically to the catalytically active PKC via a noncatalytic site of said PKC;
- testing the candidate molecules of said library for the ability to modulate positively or negatively the binding of said cognate RACK or said peptide to the PKC in an assay not dependent on purity of the cognate RACK or PKC;
- and
- ascertaining as said modulator any candidate molecule that enhances or diminishes said binding.
The peptide .beta.C2-1, .beta.C2-2, .beta.C2-4, .theta.V1-1, .theta.V1-2, .theta.V1-3, .theta.V1-4, .delta.V1-1, .delta.V1-2, .delta.V1-3, .theta.V1-4, .epsilon.V1-1, .epsilon.V1-2, .epsilon.V1-3, .epsilon.V1-4, .epsilon.V1-5, .epsilon.V1-6, .epsilon.V1-7, .eta.V1-1, .eta.V1-2, .eta.V1-3, .eta.V1-4, .eta.V1-5, .eta.V1-6, .eta.V1-7, .mu.V1-1, .mu.V1-2, .lambda.V1-1, .lambda.V1-2, .zeta.V1-1, .zeta.V1-2 or .zeta.V1-3.
Dependencies are inferred from the claim text.