[HTML][HTML] 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
… Here, we used covalent taxane-site ligands, including cyclostreptin, to gain … pore site 1,
which has been postulated to facilitate the entry of taxane-site ligands to their luminal binding site

[HTML][HTML] Drugs that changed society: microtubule-targeting agents belonging to taxanoids, macrolides and non-ribosomal peptides

SB Christensen - Molecules, 2022 - mdpi.com
… , at the inner surface of the microtubule lumen [21]. It has a … and cyclostreptin bind covalently
to the binding site [60]. … taxoid 2α-benzoyltransferase, taxoid 10β-acetyltransferase and …

Zampanolide binding to tubulin indicates cross-talk of taxane site with colchicine and nucleotide sites

JJ Field, B Pera, JE Gallego, E Calvo… - Journal of natural …, 2017 - ACS Publications
… is a marine macrolide that binds to the taxoid binding site on β-tubulin in a covalent fashion,
in … to the pore type I site, since zampanolide-saturated microtubules cannot bind cyclostreptin

Microtubule targeting agents in cancer therapy: elucidating the underlying molecular mechanisms

M Hasanpourghadi, AK Pandurangan… - Molecular oncology …, 2017 - Springer
… accesses its binding site inside the microtubule lumen is by … III which is an inactive taxoid
precursor isolated from needles of … showed cyclostreptin covalently binds to microtubule with …

[HTML][HTML] Unravelling the covalent binding of zampanolide and taccalonolide AJ to a minimalist representation of a human microtubule

PA Sánchez-Murcia, A Mills, Á Cortés-Cabrera… - Journal of computer …, 2019 - Springer
Cyclostreptin (CyS, Fig. 1), the first drug known to … tubulin at the pore site both in vitro and
in cells, thereby producing the same cytotoxic effects as drugs binding to the luminal site [30], …

Imatinib overrides taxane resistance by selective inhibition of novel CLIP1 variant obstructing the microtubule pore

K Kita, PV Thakkar, G Galletti, N Madhukar, EV Navarro… - bioRxiv, 2019 - biorxiv.org
… On the other hand, cyclostreptin is known to bind covalently to both the MT pores and
luminal taxoid binding site 33,35 and strongly inhibits taxane binding. We quantified Flutax-2 …

[PDF][PDF] Triazolopyrimidines are microtubule-stabilizing agents that bind the Vinca inhibitor site of tubulin

G Sáez-Calvo, A Sharma, F de Asís Balaguer… - Cell chemical …, 2017 - cell.com
bind to a complex formed between tubulin and the stathmin-like protein RB3. RB3 sequesters
two longitudinally aligned tubulinbind to its binding site in the context of atomic models of …

Microtubule-stabilizing agents: new drug discovery and cancer therapy

Y Zhao, X Mu, G Du - Pharmacology & Therapeutics, 2016 - Elsevier
… to be a pocket adjacent to the taxoid-binding site on β-tubulin at the outer surface of the …
on the binding modes revealed that cyclostreptin covalently binds to a pore region of β-tubulin, …

PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin

D Lucena-Agell, MJ Guillén, R Matesanz… - Journal of Medicinal …, 2024 - ACS Publications
… α-tubulin, or alternatively bind deeply in the β monomer, making no contacts with α-… tubulin
βIII isotype, as it is not affected by the Cys239 to Ser239 change in the colchicine binding site. …

Characterization of Tau and Anticancer Drug Interactions with Microtubules via Cryo-Electron Microscopy Studies

N Hejab - 2016 - escholarship.org
binding sites include a proposed imidazole site in β-tubulin … was shown to covalently bind
to H7 of β-tubulin via H230. In … can bind inside the lumen of MTs we polymerized tubulin in …