Category: Gliocytoma

M8891 is an Orally Active and Brain Penetrant MetAP-2 Inhibitor

Removal of N-terminal methionine by methionine aminopeptidases (MetAP) is a crucial step in the maturation of proteins during protein biosynthesis. Besides, MetAP-2 is one of the two cytoplasmic methionine aminopeptidases expressed in mammalian cells. Moreover, MetAP-2 acts as a target of the highly potent and irreversible inhibitor fumagillin to...

Gboxin is an Oxidative Phosphorylation Inhibitor That Targets Glioblastoma

According to the World Health Organization (WHO), Glioblastoma is the most common primary brain neoplasm. It comprises 15% of all intracranial neoplasms and 60-75% of astrocytic tumors. Unfortunately, Glioblastoma is the most aggressive and prevalent primary malignant brain tumor of the central nervous system. Glioblastoma derives specifically from 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...

JR-AB2-011, a Potential Inhibitor of mTORC2 Activity in Glioblastoma Multiforme (GBM)

Glioblastoma multiforme (GBM) are highly malignant and invasive tumors. It not only can prevent total surgical resection, but also render these neoplasms refractory to cheJR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011...

Cevipabulin (TTI-237) is a Microtubule-Active Antitumor Compound

Microtubules are part of the mitotic spindle, the complex and dynamic structure that mediates chromosome separation during mitosis. Therefore, microtubules are a proven target in cancer treatment. There have been many clinical drugs designed to target microtubule, including Paclitaxel and Vinblastine. Vincristine binds at one of three known pharmacologic...