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Morphological profiling by means of the Cell Painting assay enables identification of tubulin-targeting compounds.

Cell chemical biology

Akbarzadeh M, Deipenwisch I, Schoelermann B, Pahl A, Sievers S, Ziegler S, Waldmann H.
PMID: 34968420
Cell Chem Biol. 2021 Dec 21; doi: 10.1016/j.chembiol.2021.12.009. Epub 2021 Dec 21.

In phenotypic compound discovery, conclusive identification of cellular targets and mode of action are often impaired by off-target binding. In particular, microtubules are frequently targeted in cellular assays. However, in vitro tubulin binding assays do not correctly reflect the...

High content screening of diverse compound libraries identifies potent modulators of tubulin dynamics.

ACS medicinal chemistry letters

Laraia L, Stokes J, Emery A, McKenzie GJ, Venkitaraman AR, Spring DR.
PMID: 24900887
ACS Med Chem Lett. 2014 Feb 24;5(5):598-603. doi: 10.1021/ml5000564. eCollection 2014 May 08.

Tubulin modulating agents such as the taxanes are among the most effective antimitotic cancer drugs, although resistance and toxicity present significant problems in their clinical use. However, most tubulin modulators are derived from complex natural products, which can make...

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