Verucopeptin, a HIF-1 and v-ATPase ATP6V1G Inhibitor, Exhibits Antitumor Activity Against MDR Cancers
ATP6V1G, a subunit of the vacuolar H+-ATPase (v-ATPase). In this article, we will introduce a potent ATP6V1G inhibitor, Verucopeptin. Firstly, in vitro. Verucopeptin shows excellent antitumor activity against K562R cells, with an IC50 of 388 nM. Although these cells exhibit resistance to some other chemotherapeutic agents, such as Taxol...
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,...
TTT-28 Antagonizes Multidrug Resistance by Selectively Inhibiting the Efflux Activity of ABCB1
Cancer is a rapidly progressing disease. Chemotherapy is one of the treatment choices apart from surgery and radiation. However, during chemotherapy, a unique phenomenon called multidrug resistance (MDR) emerges. The cancer cells develop resistance to drugs with different chemical structures and mechanisms of action. On the other hand, MDR...
CHMFL-ABL-039, a Selective Type II Native and Drug-Resistant Mutant BCR-ABL Inhibitor for Chronic Myeloid Leukemia
Chronic myeloid leukemia (CML) is a white blood cell disorder, accounting for about 15% of adult leukemias. The critical driving force of pathogenesis of CML identified is BCR gene and ABL kinase gene fusion. It results in the constitutive activation of ABL kinase. And the activation is essential for...
SSE15206 is a Microtubule Polymerization Inhibitor
Microtubule, a highly dynamic structure, forms spindle fibers during mitosis. Several key cellular processes such as vesicular trafficking, intracellular signalling, cell motility and mitotic cell division depend on microtubules. In recent years, emerging studies have demonstrated the role of microtubule in targeted cancer therapy. For example, Paclitaxel, the most...