Tag: Tubulin

Rosabulin is a Potent Microtubule Inhibitor

Chemotherapy is a cornerstone in the development of present-day cancer therapy. Moreover, Chemotherapy is one of the most effective and potent strategies to treat malignant tumors. However, Chemotherapy resistance occurs when cancers that have been responding to therapy suddenly begin to grow. Rosabulin is a potent tubulin inhibitor. In...

ENMD-1198, an Orally Active Tubulin-Binding Agent, Reduces HIF-1α and STAT3 Activity

Hepatocellular carcinoma (HCC) is the fifth most cancer worldwide, with a continuously increasing incidence. HCC represents a hyper vascularized tumor and its progression is closely related to angiogenesis. Hepatocellular carcinoma overexpresses the vascular endothelial growth factor (VEGF). The transcription factor HIF-1α also plays a central role in HCC progression...

VERU-111 is an Orally Bioavailable α and β Tubulin Inhibitor

Tubulins play a major role in cell dynamics, thus are important molecular targets for cancer therapy. VERU-111 preferentially represses clinically important, βIII and βIV tubulin isoforms via restoring the expression of miR-200c. VERU-111 (ABI-231) displays optimum activity and has an average IC50 value of 5.2 nM against a large...

S516 is a Potent Tubulin Polymerization Inhibitor

The microtubules act as an attractive target for anticancer drug discovery nowadays. Disruption of microtubules can induce cell cycle arrest in the G2-M phase and formation of abnormal mitotic spindles. The tubulin polymerization inhibitors have emerged as one of promising anticancer therapeutics because of their dual mechanism of action,...

VERU-111 is an Orally Active Tubulin Inhibitor

Microtubules play a critical role in the proliferation of cancer cells. Meanwhile, microtubule dynamics is therefore one of the most productive therapeutic targets for cancer treatment. Microtubule-targeting agents can interfere with functions of microtubules, thereby disrupting the formation of the mitotic spindle, eventually leading to mitotic arrest at the...

CCB02, a Tubulin Binder Inhibits Cancer Cells with Extra Centrosomes

Centrosome is an important organelle. It acts as the main microtubule organizing center (MTOC), regulates cell-cycle progression in mammalian cells. In normal cells, centrosome duplication occurs in the early phase of cell cycle. It ensures each daughter cell to have one centrosome after cell division. CPAP (centrosomal P4.1-associated protein)...