Month: May 2019

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 Oral 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...

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...

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....