Microtubule-targeting agents: strategies to hijack the cytoskeleton

MO Steinmetz, AE Prota - Trends in cell biology, 2018 - cell.com
Microtubule-targeting agents (MTAs) such as paclitaxel and the vinca alkaloids are among
the most important medical weapons available to combat cancer. MTAs interfere with …

Marine natural products with high anticancer activities

D Matulja, K Wittine, N Malatesti… - Current medicinal …, 2020 - ingentaconnect.com
This review covers recent literature from 2012-2019 concerning 170 marine natural products
and their semisynthetic analogues with strong anticancer biological activities. Reports that …

Structural insight into the stabilization of microtubules by taxanes

AE Prota, D Lucena-Agell, Y Ma, J Estevez-Gallego… - Elife, 2023 - elifesciences.org
Paclitaxel (Taxol) is a taxane and a chemotherapeutic drug that stabilizes microtubules.
While the interaction of paclitaxel with microtubules is well described, the lack of high …

[HTML][HTML] Microtubule-targeting agents and neurodegeneration

Z Boiarska, D Passarella - Drug Discovery Today, 2021 - Elsevier
Highlights•Dysregulation of microtubule dynamics triggers neurodegeneration and
neurotoxicity.•MTAs are able to restore MT dynamics and disease-related pathology in …

Antitubulin sulfonamides: The successful combination of an established drug class and a multifaceted target

A Vicente‐Blázquez, M González… - Medicinal research …, 2019 - Wiley Online Library
Tubulin, the microtubules and their dynamic behavior are amongst the most successful
antitumor, antifungal, antiparasitic, and herbicidal drug targets. Sulfonamides are exemplary …

An overview of tubulin modulators deposited in protein data bank

H Guo, X Li, Y Guo, L Zhen - Medicinal Chemistry Research, 2019 - Springer
Microtubules are cytoskeletal polymers of tubulin and composed of α-and β-tubulin
heterodimers, which are regarded as one of the most important, promising and successful …

A series of enthalpically optimized docetaxel analogues exhibiting enhanced antitumor activity and water solubility

YT Ma, Y Yang, P Cai, DY Sun… - Journal of Natural …, 2018 - ACS Publications
A dual-purpose strategy aimed at enhancing the binding affinity for microtubules and
improving the water solubility of docetaxel led to the design and synthesis of a series of C-2 …

Structural basis of microtubule stabilization by discodermolide

AE Prota, K Bargsten, M Redondo‐Horcajo… - …, 2017 - Wiley Online Library
Microtubule‐stabilizing agents (MSAs) are widely used in chemotherapy. Using X‐ray
crystallography we elucidated the detailed binding modes of two potent MSAs,(+) …

Crystal structure of the cyclostreptin-tubulin adduct: Implications for tubulin activation by taxane-site ligands

FA Balaguer, T Mühlethaler, J Estévez-Gallego… - International journal of …, 2019 - mdpi.com
It has been proposed that one of the mechanisms of taxane-site ligand-mediated tubulin
activation is modulation of the structure of a switch element (the M-loop) from a disordered …

Targeting and extending the eukaryotic druggable genome with natural products: Cytoskeletal targets of natural products

AL Risinger, L Du - Natural product reports, 2020 - pubs.rsc.org
Covering: 2014–2019 We review recent progress on natural products that target cytoskeletal
components, including microtubules, actin, intermediate filaments, and septins and highlight …