N-acetyl-S-geranylgeranyl-L-Cysteine is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.
Geranylgeranyl pyrophosphate, a key metabolite in protein geranylgeranylation, serves as the universal precursor for diterpenoids, such as Paclitaxel. Its role in cancer research stems from this critical function.
FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
FTI-2148 is an inhibitor of RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) (IC50s: 1.4 nM and 1.7 μM, respectively).
Geranyl pyrophosphate is an intermediate in the mevalonate pathway. It is formed from dimethylallyl pyrophosphate and isopentenyl pyrophosphate by geranyl pyrophosphate synthase. Geranyl pyrophosphate is used in the biosynthesis of farnesyl pyrophosphate , geranylgeranyl pyrophosphate , cholesterol, terpenes, and terpenoids.
GGTI-2166 is a geranylgeranyl transferase I inhibitor. GGTI-2166 inhibit the pOC formation induced by RANKL or TNF-alpha in cultures of both mouse marrow-derived macrophage-colony-stimulating factor (M-CSF) dependent monocytes (MD cells) and the mouse monocyte cell line RAW 264.7 (RAW cells). GGTI-2166 inhibited TRAP activity induced by RANKL or TNF-alpha in both cell cultures and prevented the incorporation of [3H]all-trans geranylgeraniol into prenylated proteins in RAW cells.
GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM). The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 µM) without affecting the farnesylation of H-Ras (IC50= >30 µM). Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. When administered intraperitoneally at 5 mg/kg per day, it prevents eosinophil infiltration into the airways in a mouse model of allergic bronchial asthma, although it does not reduce chemokine levels. Additionally, GGTI 2133 thwarts naloxone-induced contraction of ileum in rats experiencing morphine withdrawal syndrome and mitigates the severity of withdrawal symptoms in vivo (ED50= 0.076 mg/kg).