Concept

Mitotic inhibitor

Related publications (97)

A benzamide-dependent ftsZ mutant reveals residues crucial for Z-ring assembly

In almost all bacteria, cell division is co-ordinated by the essential tubulin homologue FtsZ and represents an attractive but as yet unexploited target for new antibiotics. The benzamides, e.g. PC190723, are potent FtsZ inhibitors that have the potential ...

Wiley-Blackwell2016

How many lives does CLIMP-63 have?

Françoise Gisou van der Goot Grunberg, Patrick Alain Sandoz

In 1995, in the Biochemical Society Transactions, Mundy published the first review on CLIMP-63 (cytoskeletonlinking membrane protein 63) or CKPA4 (cytoskeleton-associated protein 4), initially just p63 [1]. Here we review the following 20 years of research ...

2015

Protein ruthenation and DNA alkylation: chlorambucil-functionalized RAPTA complexes and their anticancer activity

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov, Olivier Pierre Zava

Chemotherapeutics for the treatment of tumorigenic conditions that feature novel modes of action are highly sought after to overcome the limitations of current chemotherapies. Herein, we report the conjugation of the alkylating agent chlorambucil to the RA ...

2015

Improved Angiostatic Activity of Dasatinib by Modulation with Hydrophobic Chains

Paul Joseph Dyson, Patrycja Nowak-Sliwinska, Catherine Marie Amélie Clavel, Emilia Paunescu

Dasatinib is an orally active nonselective tyrosine kinase inhibitor used to treat certain types of adult leukemia. By inhibiting PDGFR-beta and SFKs in both tumor cells and tumor associated endothelial cells, dasatinib inhibits tumor growth and angiogenes ...

Amer Chemical Soc2015

Investigating the Optimal Size of Anticancer Nanomedicine

Li Tang, Hui Wang

Nanomedicines (NMs) offer new solutions for cancer diagnosis and therapy. However, extension of progression-free interval and overall survival time achieved by Food and Drug Administration-approved NMs remain modest. To develop next generation NMs to achie ...

2014

Optimization of the analogue-sensitive Cdc2/Cdk1 mutant by in vivo selection eliminates physiological limitations to its use in cell cycle analysis

Viesturs Simanis

Analogue-sensitive (as) mutants of kinases are widely used to selectively inhibit a single kinase with few off-target effects. The analogue-sensitive mutant cdc2-as of fission yeast (Schizosaccharomyces pombe) is a powerful tool to study the cell cycle, bu ...

Royal Society, The2014

Ligand substitutions between ruthenium-cymene compounds can control protein versus DNA targeting and anticancer activity

Paul Joseph Dyson, Ursula Röthlisberger, Wee Han Ang, Alexey Nazarov, Pablo Campomanes Ramos, Catherine Marie Amélie Clavel, Michael Groessl

Ruthenium compounds have become promising alternatives to platinum drugs by displaying specific activities against different cancers and favourable toxicity and clearance properties. Nonetheless, their molecular targeting and mechanism of action are poorly ...

2014

Synthesis and evaluation of new polynuclear organometallic Ru(II), Rh(III) and Ir(III) pyridyl ester complexes as in vitro antiparasitic and antitumor agents

Paul Joseph Dyson, Tina Riedel

New polynuclear organometallic Platinum Group Metal (PGM) complexes containing di- and tripyridyl ester ligands have been synthesised and characterised using analytical and spectroscopic techniques including H-1, C-13 NMR and infrared spectroscopy. Reactio ...

2014

Fluorogenic probes for live-cell imaging of the cytoskeleton

Kai Johnsson, Luc Reymond, Grazvydas Lukinavicius, Mathias Fournier, Anastasiya Masharina

We introduce far-red, fluorogenic probes that combine minimal cytotoxicity with excellent brightness and photostability for fluorescence imaging of actin and tubulin in living cells. Applied in stimulated emission depletion (STED) microscopy, they reveal t ...

Nature Publishing Group2014

SAS-1 Is a C2 Domain Protein Critical for Centriole Integrity in C. elegans

Pierre Gönczy, Graham Knott, Simon Blanchoud, Lukas von Tobel, Tamara Mikeladze-Dvali

Centrioles are microtubule-based organelles important for the formation of cilia, flagella and centrosomes. Despite progress in understanding the underlying assembly mechanisms, how centriole integrity is ensured is incompletely understood, including in sp ...

Public Library of Science2014

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