Microtubules as a target for anticancer drugs. Nat Rev Cancer 4, 253–265 (2004). 22. Cortese, F., Bhattacharyya, B. & Wolff, J. Podophyllotoxin as a probe for the colchicine binding site of tubulin. The Journal of biological chemistry 252, 1134–1140 (1977). 23. Bernstein, P. S.,...
The emphasis of this chapter is on microtubule targeting drugs that are currently used clinically for cancer therapy as well as agents that are being evaluated in clinical trials. A few agents in preclinical development that have a unique binding site or mechanism of action are also described....
Microtubules are dynamic polymers that play crucial roles in a large number of cellular functions. Their pivotal role in mitosis makes them a target for the development of anticancer drugs. Microtubule-damaging agents suppress microtubule dynamics, leading to disruption of the mitotic spindle in dividin...
Our previous research has shown that CEP20 is a centrosomal protein and a newly identified microtubule-associated protein involved in ciliogenesis, indicating its potential as a new target for lung cancer treatment. Our future experiments will also examine the protein structure of CEP20 and its ...
At the same time, HIF-1α is critically important for RCC disease progression, as ∼70–80% of RCCs have loss-of-function mutations in the von Hippel Lindau (VHL) protein (13), which is responsible for HIF-1α degradation in normoxia. As a result, HIF-1α and its target genes are...
Microtubules as a target for anticancer drugs. Jordan MA, Wilson L. MA Jordan,L Wilson - 《Nature Reviews Cancer》 被引量: 4483发表: 2004年 Taxol stabilizes microtubules in mouse fibroblast cells Taxol, a potent inhibitor of human HeLa and mouse fibroblast cell replication, blocked cells in th...
The D1 binding site is shown as a reference. (D) The crystallization helpers target tubulin surfaces (red and blue stars) to prevent the tubulin self-association into straight (top, right) or curved (bottom, right) assemblies. Although fruitful, the use of SLDs as tubulin-crystallization ...
The overexpression of Aurora kinases in multiple tumors makes these kinases appealing targets for the development of anticancer therapies. This study identified two small molecules with a furanopyrimidine core, IBPR001 and IBPR002, that target Aurora kinases and induce a DFG conformation change at th...
Microtubules polymerise from tubulin proteins and play a significant role in the growth and proliferation of eukaryotic cells. In yeasts, most studies on microtubules and tubulins have utilised the budding yeast Saccharomyces cerevisiae and fission yeast
As western blot measures both free and polymerized tubulin, and the majority of tubulin in striated muscle is in the free pool10,32, immunofluorescence is a more accurate indicator of the status of the polymerized network. We also examined the effects of PTL on other common MT PTMs, namely,...