The microtubule cytoskeleton: An old validated target for novel therapeutic drugs

L Lafanechère - Frontiers in Pharmacology, 2022 - frontiersin.org
Compounds targeting microtubules are widely used in cancer therapy with a proven efficacy.
However, because they also target non-cancerous cells, their administration leads to …

[HTML][HTML] Tubulin inhibitors. Selected scaffolds and main trends in the design of novel anticancer and antiparasitic agents

M Podolak, S Holota, Y Deyak, K Dziduch… - Bioorganic …, 2024 - Elsevier
Abstract Design of tubulin inhibitors as anticancer drugs dynamically developed over the
past 20 years. The modern arsenal of potential tubulin-targeting anticancer agents is …

Watching the release of a photopharmacological drug from tubulin using time-resolved serial crystallography

M Wranik, T Weinert, C Slavov, T Masini… - Nature …, 2023 - nature.com
The binding and release of ligands from their protein targets is central to fundamental
biological processes as well as to drug discovery. Photopharmacology introduces chemical …

Rational design of a novel tubulin inhibitor with a unique mechanism of action

T Mühlethaler, L Milanos, JA Ortega… - Angewandte …, 2022 - Wiley Online Library
In this study, we capitalized on our previously performed crystallographic fragment screen
and developed the antitubulin small molecule Todalam with only two rounds of …

The tubulin superfamily in apicomplexan parasites

N Morrissette, I Abbaali, C Ramakrishnan, AB Hehl - Microorganisms, 2023 - mdpi.com
Microtubules and specialized microtubule-containing structures are assembled from
tubulins, an ancient superfamily of essential eukaryotic proteins. Here, we use bioinformatic …

Purification of functional Plasmodium falciparum tubulin allows for the identification of parasite-specific microtubule inhibitors

WG Hirst, D Fachet, B Kuropka, C Weise, KJ Saliba… - Current Biology, 2022 - cell.com
Cytoskeletal proteins are essential for parasite proliferation, growth, and transmission, and
therefore have the potential to serve as drug targets. 1–5 While microtubules and their …

[HTML][HTML] Structure-based discovery and rational design of microtubule-targeting agents

MO Steinmetz, AE Prota - Current Opinion in Structural Biology, 2024 - Elsevier
Microtubule-targeting agents (MTAs) have demonstrated remarkable efficacy as antitumor,
antifungal, antiparasitic, and herbicidal agents, finding applications in the clinical, veterinary …

Structural Changes, Biological Consequences, and Repurposing of Colchicine Site Ligands

F Montecinos, DL Sackett - Biomolecules, 2023 - mdpi.com
Microtubule-targeting agents (MTAs) bind to one of several distinct sites in the tubulin dimer,
the subunit of microtubules. The binding affinities of MTAs may vary by several orders of …

Cytoskeletal dynamics in parasites

S Reber, M Singer, F Frischknecht - Current Opinion in Cell Biology, 2024 - Elsevier
Cytoskeletal dynamics are essential for cellular homeostasis and development for both
metazoans and protozoans. The function of cytoskeletal elements in protozoans can diverge …

Unveiling the Possible Oryzalin-Binding Site in the α-Tubulin of Toxoplasma gondii

R Aguayo-Ortiz, L Dominguez - ACS omega, 2022 - ACS Publications
Dinitroaniline derivatives have been widely used as herbicidal agents to control weeds and
grass. Previous studies demonstrated that these compounds also exhibit good antiparasitic …