Microtubules are essential for the mitotic division of cells and have been an attractive target
for antitumour drugs due to the increased incidence of cancer and significant mitosis rate of tumour cells.
In the past few years, tubulin-colchicine binding site, as one of the three binding pockets including taxol-,
vinblastine- and colchicine-binding sites, has been focused on to design tubulin-destabilizing agents including
inhibitors, antibody-drug conjugates and degradation agents. The present review is the first to
cover a systemic and recent synopsis of tubulin-colchicine binding site agents. We believe that it would
provide an increase in our understanding of receptor-ligand interaction pattern and consciousness of a
series of challenges about tubulin target druggability.
Epigenetics is defined as the stable and heritable alternations in gene expression without
changing the DNA nucleotide sequence. The initiation and progression of cancer result from not only
genetic mutation, but also aberrant epigenetic regulation, such as DNA methylation and histones acetylation.
Although Genetic alternations cannot be reversed, epigenetic modification is a dynamic and reversible
process. Over the past few decades, much progress has been made in the research of epigenetic
medications and a variety of drugs have been developed targeting at epigenetic regulatory proteins,
which are capable of restoring malignant cancer cells to the normal state. The epigenetic drugs currently
approved for cancer treatment mainly target at DNA methylation and histones acetylation. In addition,
there are a great many epigenetic drugs in clinical trials for cancer therapy, such as inhibitors of DNA
methyltransferases, histone deacetylases, histone methyltransferases, lysine specific demethylases, and
BET (bromodomain and extra-terminal domain) family proteins. We will discuss the latest developments
of these inhibitors and their applications in cancer therapy.
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