GGTI-2418

Geranylgeranyltransferase I Inhibitor PTX-100 is a small molecule and synthetic peptidomimetic inhibitor of the protein geranylgeranyltransferase type 1 (GGTase-I; GGT-1), with potential antineoplastic activity. Upon administration, GGTase-I inhibitor PTX-100 targets and binds to GGTase-I, an enzyme involved in the posttranslational modification of numerous oncogenic GTPases, including K-Ras, N-Ras, RhoA, RhoC, Cdc42, RalA, RalB, Rap1 and Rac1. Inhibition of geranylgeranylation (GG), inhibits the post-translational modification of these oncogenic proteins, inhibits their membrane localization and oncogenic activity. This prevents Ras-mediated signaling and prevents Ras-mediated cancer cell proliferation, migration, invasion, and metastasis. This may result in cell cycle arrest and induce apoptosis. In addition, PTX-100 may also downregulate a variety of other activated cancer survival pathways. Protein geranylgeranylation, catalyzed by GGTase-I, plays a critical role in malignant transformation and cancer cell proliferation, migration, and invasion.