NOVEL PHARMACEUTICALLY ACTIVE COMPOUNDS INTERACTING WITH GTP-BINDING PROTEINS

摘要

The present invention relates to compounds that bind to the surface of normal or mutated GTP binding proteins and reduce the activation energy of the GTPase activity thereof by introduction of at least one functional group into the active site of said proteins. Said compounds are of synthetic or semi-synthetic origin. Preferably, the functional group referred to above is an arginine finger or a derivative thereof or a compound that mimics the activity of an arginine finger that is obtained, for example, by peptidomimetics. The invention further relates to a pharmaceutical composition comprising the compound of the invention as well as to methods for treating patients suffering from oncogenic activations of Ras genes, from tumors caused by malfunction of G proteins or from neurofibromatosis. Additionally, the present invention relates to kits comprising the compound of the invention as well as to methods for devising said compound. Finally, the invention relates to methods for devising lead compounds for the development of the compounds of the invention.