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 …

An overview of tubulin inhibitors that interact with the colchicine binding site

Y Lu, J Chen, M Xiao, W Li, DD Miller - Pharmaceutical research, 2012 - Springer
Tubulin dynamics is a promising target for new chemotherapeutic agents. The colchicine
binding site is one of the most important pockets for potential tubulin polymerization …

Role of tau as a microtubule-associated protein: structural and functional aspects

P Barbier, O Zejneli, M Martinho, A Lasorsa… - Frontiers in aging …, 2019 - frontiersin.org
Microtubules (MTs) play a fundamental role in many vital processes such as cell division
and neuronal activity. They are key structural and functional elements in axons, supporting …

High-resolution microtubule structures reveal the structural transitions in αβ-tubulin upon GTP hydrolysis

GM Alushin, GC Lander, EH Kellogg, R Zhang, D Baker… - Cell, 2014 - cell.com
Dynamic instability, the stochastic switching between growth and shrinkage, is essential for
microtubule function. This behavior is driven by GTP hydrolysis in the microtubule lattice and …

Molecular interactions at the colchicine binding site in tubulin: An X-ray crystallography perspective

J Wang, DD Miller, W Li - Drug discovery today, 2022 - Elsevier
Highlights•Colchicine binding site inhibitors (CBSIs) emerge as new generations of tubulin
inhibitors.•CBSIs are less susceptible to multidrug resistance than FDA-approved tubulin …

Structures of a diverse set of colchicine binding site inhibitors in complex with tubulin provide a rationale for drug discovery

Y Wang, H Zhang, B Gigant, Y Yu, Y Wu… - The FEBS …, 2016 - Wiley Online Library
Microtubules are dynamic assemblies of αβ‐tubulin heterodimers and have been
recognized as highly attractive targets for cancer chemotherapy. A broad range of agents …

Identification of pyrrolo [3′, 4': 3, 4] cyclohepta [1, 2-d][1, 2] oxazoles as promising new candidates for the treatment of lymphomas

M Barreca, V Spanò, R Rocca, R Bivacqua… - European journal of …, 2023 - Elsevier
Unsatisfactory outcomes for relapsed/refractory lymphoma patients prompt continuing efforts
to develop new therapeutic strategies. Our previous studies on pyrrole-based anti …

Anti-microtubule drugs

S Florian, TJ Mitchison - The Mitotic Spindle: Methods and Protocols, 2016 - Springer
Small molecule drugs that target microtubules (MTs), many of them natural products, have
long been important tools in the MT field. Indeed, tubulin (Tb) was discovered, in part, as the …

Structural basis of tubulin tyrosination by tubulin tyrosine ligase

AE Prota, MM Magiera, M Kuijpers, K Bargsten… - Journal of Cell …, 2013 - rupress.org
Tubulin tyrosine ligase (TTL) catalyzes the post-translational retyrosination of detyrosinated
α-tubulin. Despite the indispensable role of TTL in cell and organism development, its …

Blocking blood flow to solid tumors by destabilizing tubulin: an approach to targeting tumor growth

MJ Pérez-Pérez, EM Priego, O Bueno… - Journal of medicinal …, 2016 - ACS Publications
The unique characteristics of the tumor vasculature offer the possibility to selectively target
tumor growth and vascularization using tubulin-destabilizing agents. Evidence accumulated …