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Protein prenyltransferase inhibitors here mainly target geranylgeranyltransferase type I (GGTase-I). Prenyltransferases attach isoprenoid lipids to C-terminal cysteines, which anchors small GTPases and other proteins to membranes. Farnesyltransferase and GGTase-I were shown in 1991 to share a common alpha subunit, while their beta subunits select a 15-carbon or 20-carbon chain. GGTase-I modifies Rho family GTPases ending in a cysteine-aliphatic-aliphatic-X (CAAX) motif with a C-terminal leucine. Rab GTPases are instead modified by Rab geranylgeranyltransferase (GGTase-II), whose escort protein was linked in 1992 to the choroideremia gene. GGTI298 and GGTI-2418 are CAAX peptidomimetic inhibitors of GGTase-I, and BAY-593 is a more recent GGTase-I inhibitor. Inhibitors of protein farnesylation are listed separately under Farnesyl Transferase.
GGTI-2418 is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I) that appears to induce apoptosis by downregulating several pivotal oncogenic and tumor survival pathways.
Synonyms: GGTI 298
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
GGTI-2154 hydrochloride is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), exhibiting an IC50 of 21 nM. It demonstrates over 200-fold selectivity for GGTase I compared to farnesyltransferase (FTase), which has an IC50 of 5600 nM. This compound is utilized in cancer research to explore the role of GGTase I in tumorigenesis and related signaling pathways.
GGTI-2417 is a selective inhibitor of GGTase I, targeting geranylgeranylation processes within cells. This compound has been shown to inhibit Cdk2-mediated phosphorylation of p27Kip1 at Thr187, resulting in the accumulation of p27Kip1 in the nucleus. Additionally, GGTI-2417 induces apoptosis in breast cancer cells, making it valuable for research in cancer biology and therapeutic applications.
GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), exhibiting an IC50 of 21 nM. This compound demonstrates over 200-fold selectivity for GGTase I relative to farnesyltransferase (FTase), with an IC50 of 5600 nM. GGTI-2154 is valuable for research related to cancer, particularly in studying the role of protein geranylgeranylation in tumorigenesis and cancer progression.
BAY-593 is an orally active inhibitor of geranylgeranyltransferase I (GGTase-I), targeting the post-translational modification critical for protein function. This compound effectively disrupts YAP1/TAZ signaling pathways, which are often associated with cancer progression. BAY-593 has demonstrated potential antitumor activity, making it a valuable tool for research into cancer biology and therapeutic interventions.
(7S)-BAY-593 is a potent inhibitor of geranylgeranyltransferase I (GGTase-I), specifically the S-enantiomer of BAY-593. This compound effectively disrupts YAP1/TAZ signaling pathways, demonstrating significant antitumor activity in animal models. It serves as a valuable tool for cancer research, particularly in studies focused on the regulation of the Hippo signaling pathway and its implications in tumorigenesis.
BAY-593 hydrochloride is a potent GGTase-I inhibitor, effectively disrupting YAP1/TAZ signaling pathways. This compound demonstrates significant antitumor activity in preclinical models, making it a valuable tool for cancer research. Its oral bioavailability enhances its application in vivo, facilitating studies on the mechanistic role of GGTase-I in tumor biology and potential therapeutic strategies.
GGTI-286 is a selective inhibitor of geranylgeranyl transferase I (GGTase I) with an IC50 of 2 μM, demonstrating 25-fold increased potency compared to its methyl ester derivative. It effectively inhibits the geranylgeranylation of Rap1A while displaying a lower impact on the farnesylation of H-Ras, with IC50 values of 2 μM and >30 μM, respectively. Additionally, GGTI-286 shows strong inhibition of oncogenic K-Ras4B stimulation, with an IC50 of 1 μM, making it a valuable tool for research in cancer biology and signaling pathways.
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GGTI-286 hydrochloride is a selective inhibitor of geranylgeranyltransferase I (GGTase I) with a potency that is 25-fold greater than the methyl ester of FTI-276 (IC50 = 2 μM). This compound demonstrates a strong preference for inhibiting the geranylgeranylation of Rap1A over the farnesylation of H-Ras in NIH3T3 cells (IC50s = 2 μM and >30 μM, respectively). Additionally, GGTI-286 hydrochloride effectively inhibits the stimulation of oncogenic K-Ras4B, with an IC50 of 1 μM, making it a valuable tool for research in cancer biology and signal transduction pathways.
GGTI-297 is an inhibitor of geranylgeranyl transferase I (GGTase-1), exhibiting IC50 values of 56 nM for GGTase-1 and 203 nM for farnesyl transferase (FTase). This compound specifically inhibits the geranylgeranylation of the protein Rap1A, effectively disrupting its processing while leaving the farnesylated protein H-Ras unaffected. GGTI-297 is valuable for research applications focused on protein prenylation and its implications in cellular signaling pathways.
GGTI-2147 is a potent inhibitor of geranylgeranyl transferase I (GGTase I). It effectively blocks the geranyl-geranylation of the small GTPase Rap1A, leading to a reduction in Rac1 activity and mitigation of OGD/R-induced neuronal apoptosis. This compound is valuable for research into neurodevelopmental disorders, including autism, depression, and schizophrenia.
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