Microtubules are an essential part of cellular structure and are involved in many important cellular processes. One of the most important actions of antivascular drugs is to disrupt tubulin-microtubule dynamics, induce mitotic arrest and lead to cell death. Therefore, tubulin has also been a major target for anticancer drug discovery over the past few decades. Tubulin has three distinct small molecule binding sites, the taxane-binding site, the vinblastine-binding site, and the colchicine-binding site. Taxanes and vinca alkaloids have been successfully used in the clinical treatment of cancer. Dual-target tubulin inhibitors that regulate multiple tumor-related targets have attracted the attention of scientists. In addition to tubulin-c-MET dual-target inhibitors and tivantinib, we are also working hard to study tubulin and Hsp90 A dual-target inhibitor of targets such as , Src, PI3K, TDO/IDO and topoisomerase.
Microtubules are cytoskeletal filaments that assemble from and disassemble into their αβ-tubulin isoforms. Since microtubules are involved in several important cellular activities, including cell division, cell motility, and intracellular transport, drugs that interfere with microtubule function have been very successfully developed as chemotherapeutic agents against different malignancies.
Since the design of dual-target drugs is more complex than that of single-target drugs, our scientists use various design strategies, including drug repurposing, backbone design of dual-target inhibitors, pharmacophore-based combination and Computational methods to have further enhanced the development of dual-target drugs.
In addition to applying traditional drug discovery strategies, our scientists continue to use many new methods for the rational design of dual-target inhibitors, for example, by predicting the structural similarity between the tubulin binding pocket and other anti-tumor targets Signal network analysis, computer pharmacophore modeling, artificial intelligence technology, etc.
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