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Microtubule and tubulin inhibitors bind tubulin and either stabilize microtubules or block their assembly. Microtubules are dynamic polymers of α/β-tubulin dimers that build the mitotic spindle and serve as tracks for intracellular transport. Compounds that alter their dynamics arrest cells in mitosis and are standard tools in cell division research. Taxanes such as paclitaxel, docetaxel and cabazitaxel stabilize microtubules, and paclitaxel was shown in 1979 to promote tubulin assembly in vitro. Epothilone B and ixabepilone also stabilize microtubules through the taxane binding region of β-tubulin. The vinca alkaloids vincristine and vinorelbine, colchicine and eribulin act in the opposite direction and suppress polymerization.
QC-01-175 is a heterobifunctional PROTAC molecule designed to degrade aberrant tau protein. It effectively reduces levels of A152T and P301L mutant tau, mitigates tau-mediated neurotoxicity, and enhances neuronal survival.
ER Degrader 7 is a selective degrader of estrogen receptors ERα and ERβ, promoting their degradation to inhibit estrogen signaling. This compound demonstrates significant cytotoxicity in various breast cancer cell lines, with IC50 values of 0.06 µM in MCF-7, 2.56 µM in T47D, and varying values in other cell types. Additionally, ER Degrader 7 has been shown to impede tubulin polymerization, contributing to its effectiveness in inhibiting breast cancer tumor growth. This makes it a valuable tool for research into targeted therapies for hormone-driven malignancies.
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