inhibitors of proteins of the rho gef family

摘要

The present invention relates to the use of an aptamer library for determining inhibitors of any one of the proteins from the Rho-GEFs family, by an appropriate screening process. ??The present invention also relates to a process for determining inhibitors of any one of the proteins from the Rho-GEFs family, comprising a step of contacting said protein for which an inhibitor is sought with the peptides from an aptamer library, a step of recovering a first group of peptides which specifically bind to said protein, particularly to the catalytic domain of the GEF region of said protein, a step of recovering, among the first group of peptide as mentioned above, the peptide which specifically inhibits the in vitro exchange activity of said protein towards any one of the proteins from the Rho-GTPases family, as determined for example in the GEF assay, and a step of testing the peptide as mentioned above for its capacity to inhibit in intact cells the activity of the Rho-GEF on the appropriate GTPase, using for example the GTPase activity assay.