FARNESYL-PROTEIN TRANSFERASE ASSAY FOR IDENTIFYING COMPOUNDSTHAT BLOCK NEOPLASTIC TRANSFORMATION

摘要

FARNESYL-PROTEIN TRANSFERASE ASSAY FOR DC6 IDENTIFYING COMPOUNDS THAT BLOCK NEOPLASTIC TRANSFORMATION Assays for farnesyl-protein transferase (FT) which can be used to identify substances that block the farnesylation of ras oncogene products are described. Because farnesylation is required for ras oncogene activity, inhibitory compounds identified in the assays of the invention can block neoplastic transformation mediated by the ras oncogene. The assays of the invention are targeted for a step subsequent to the synthesis of farnesyl pyrophosphate (FPP), the donor of the farnesyl residue, and an intermediate in cholesterol synthesis and other important cellular pathways. Therefore, compounds which inhibit ras mediated transformation, yet do not cause major disruptions of important cell pathways that require FPP as an intermediate may be identified using the assays of the invention.