geranylgeranyltransferase I inhibitor

Geranylgeranyltransferase I inhibitors (GGTIs) are a class of small molecule anticancer agents that target the enzyme geranylgeranyltransferase I (GGTase I). This enzyme catalyzes the post-translational lipid modification known as geranylgeranylation, which is essential for the membrane association and functional activity of various proteins, including members of the Rho and Ras GTPase families. By inhibiting GGTase I, these compounds disrupt oncogenic signaling pathways involved in cell proliferation, survival, and migration. The most clinically advanced member of this class is GGTI-2418 (also known as PTX-100), a peptidomimetic small molecule developed by Prescient Therapeutics. GGTI-2418 has been evaluated in Phase I clinical trials for advanced solid tumors, including melanoma, prostate cancer, and glioblastoma. Recent research also suggests that GGTIs can enhance the persistence and efficacy of CAR-T cell therapies by reducing T-cell exhaustion and promoting a central memory-like phenotype. Other research-stage compounds in this class include P61A6 and GGTI-DU40.

Other names

GGTIGGTase I inhibitorgeranylgeranyltransferase type 1 inhibitor