MPT0B014, a Tubulin Polymerization Inhibitor Induces Cancer Cell Apoptosis
Microtubules are polymers of microtubule proteins that form part of the cytoskeleton and provide structure and shape for eukaryotic cells. Specifically, Microtubules play an important role in many cellular processes. They participate in maintaining cellular structure and form the cytoskeleton together with microfilaments and intermediate filaments. Besides, Microtubes are...
Talotrexin, A RFC Specific Inhibitor, Targets DHFR to Inhibit Tumor Growth
In this article, we will introduce a potent RFC (reduced folate carrier) specific inhibitor Talotrexin (PT523). Talotrexin, an analog of Aminopterin, is a nonpolyglutamatable classic antifolate. Additionally, it selectively inhibits RFC transport. Mammals cannot synthesize folates de novo, their cellular uptake from the extracellular milieu is essential. Besides, The...
MC2590, a Potent HDAC Inhibitor, inhibits HDAC1-3, -6, -8, and -10
Histone deacetylase (HDAC) is an epigenetic enzyme that regulates gene expression through histone deacetylation. It leads to more closed chromatin structure and gene expression inhibition. Many non-histones are also targets of HDAC, such as α Microtubulin, heat shock protein (HSP) 90, and hypoxia-inducible factor HIF-1 α. Specifically, HDAC is...
Brusatol (NSC 172924) is a Nrf2 Inhibitor
Keap1-Nrf2 is the major regulator of cytoprotective responses to electrophilic chemicals or reactive oxygen species (ROS). Upregulation of Nrf2 inducing by inactivation of Keap1 is often observed in cancer cells. Aberrant activation of Nrf2 in cancer cells accelerates proliferation and metabolism. Meanwhile, Nrf2 is a transcription factor that regulates cellular...
Rapamycin is a Specific mTOR Inhibitor
mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. In addition, mTOR links with other proteins and serves as a core...
GGTI-2154 is a Selective Geranylgeranyltransferase I (GGTase I) Inhibitor
The Ras superfamily of low molecular weight GDP/GTP-binding GTPases is critical in the regulation of many important biological events. They include the cell division cycle, survival and death, differentiation, and development. These GTPases also show a relation with oncogenesis, Ras and Rho proteins mediate malignant transformation, invasion, and metastasis....
PTC-209 is a Specific BMI-1 Inhibitor and Impairs the Tumor Microenvironment
Glioblastoma multiforme (GBM) is the most common and aggressive brain tumor and refractory to existing therapies. BMI-1 is part of the polycomb repressive complex 1 (PRC1). There is a statistically significant correlation between the high frequency of BMI-1-positive tumor cells and poor prognosis of patients according to the data...