Epothilone B is a Microtubule Stabilizer
Microtubules are polymers of tubulin, which is one of several members of a small family of globular proteins. The tubulin superfamily includes five distinct families, the α-, β-, γ-, δ-, and ε-tubulins and a sixth family which is present only in kinetoplastid protozoa. The most common members α-tubulin and...
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,...
MPT0B392 Induces Apoptosis via Inhibiting Tubulin Polymerization and Inducing c-JNK Activation
Acute leukemia is a neoplastic disease characterized by a rapid accumulation of primitive hematopoietic cells. MPT0B392 acts as a potential anticancer drug for the treatment of acute leukemia. MPT0B392 is a strong microtubule binding and depolymerizing agent but not a p-gp substrate. To determine the antitumor activity of MPT0B392,...
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...