GGTI-2418 is a Highly Potent, Competitive, and Selective GGTase I inhibitor
Members of the Ras and Rho family of GTPases are signal transducers that regulate many biological processes, including cell cycle progression, cell survival, and cell differentiation. When persistently activated, GTPases promote several oncogenic events, including uncontrolled proliferation, resistance to apoptosis, sustained angiogenesis, invasion, and metastasis. The ability of the...
RIPGBM is a Selective Inducer of Apoptosis in Glioblastoma Multiforme Cancer Stem Cells
Glioblastoma multiforme is the most prevalent and aggressive form of primary brain cancer. Glioblastoma multiforme is the most hostile type of brain cancer. Its aggressiveness is due to increased invasion, migration, proliferation, angiogenesis, and a decreased apoptosis. Crucially, a sub-population of multi-potent cells term glioblastoma multiforme cancer stem cells...
CFI-402257 is a Highly Selective and Orally Active Inhibitor of Mps1/TTK
The spindle assembly checkpoint (SAC) is important for cell survival. Its inactivation generates lethal genomic instability in cancer cells. Inhibition of SAC signaling through targeting of Mps1 has provided an indication of the feasibility of such an approach. Mps1 is also an essential, dual-specificity kinase that functions as an...
TAS-114, a Dual dUTPase/DPD Inhibitor, Improves Therapeutic Efficacy of Fluoropyrimidine-Based Chemotherapy
The fluoropyrimidine 5-fluorouracil (5-FU) is an antimetabolite drug that is widely used for the treatment of cancer, particularly for colorectal cancer. Fluorouracil is part of a group of chemotherapy drugs known as anti-metabolites. Anti-metabolites are similar to normal body molecules but they have a slightly different structure. These differences...
MDL-800, a Selective SIRT6 Activator, Increases SIRT6 Deacetylation Activity
Sirtuins are evolutionarily conserved epigenetic proteins involved in diverse cellular processes in both prokaryotes and eukaryotes. Among them, Sirtuin 6 (SIRT6) is a member of the sirtuin family of NAD+-dependent deacetylases. SIRT6 regulates glucose homeostasis in the liver. The overexpression of SIRT6 inhibits the phosphorylation of ERK1/2 and thus...
SNIPER(TACC3)-1, a Novel Small Molecule Degrading the TACC3 Protein via the Ubiquitin-proteasome Pathway
Recently, the specific and nongenetic IAP-dependent protein eraser (SNIPER) is a novel approach to the treatment of various diseases, including cancer. SNIPER composes of two different ligands connected by a linker; one is a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) and the other a ligand for...
BGT226 is a Dual PI3K/mTOR Inhibitor
The phosphoinositide 3-kinase (PI3K) pathway has key roles in regulating physiologic functions, including cellular proliferation, growth, metabolism, and survival. The PI3K pathway frequently activats in cancer cells, via several mechanisms, including mutation of PI3K signaling components and downstream effectors. One example is the aberrant expression of phosphoinositide 3-kinase (PI3K)/AKT/mTOR....