Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity

SKLB060 Reversibly Binds to Colchicine Site of Tubulin and Possesses Efficacy in Multidrug-Resistant Cell Lines

(2018) Wei Yan et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

The compound millepachine and its derivatives inhibit tubulin polymerization by irreversibly binding to the colchicine-binding site in β-tubulin

(2018) Jianhong Yang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361)

(2018) Michael P. Smolinski et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fighting tubulin-targeting anticancer drug toxicity and resistance

(2017) Roberta Visconti et al.   ENDOCRINE-RELATED CANCER

Dual Src Kinase/Pretubulin Inhibitor KX-01, Sensitizes ERα-negative Breast Cancers to Tamoxifen through ERα Reexpression

(2017) Muralidharan Anbalagan et al.   MOLECULAR CANCER RESEARCH

Antitumor Effect of KX-01 through Inhibiting Src Family Kinases and Mitosis

(2017) Seongyeong Kim et al.   Cancer Research and Treatment

Microtubule destabilising agents: far more than just antimitotic anticancer drugs

(2016) Darcy Bates et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Sustained Accumulation of Microtubule-Binding Chemotherapy Drugs in the Peripheral Nervous System: Correlations with Time Course and Neurotoxic Severity

(2016) K. M. Wozniak et al.   CANCER RESEARCH

Pironetin Binds Covalently to αCys316 and Perturbs a Major Loop and Helix of α-Tubulin to Inhibit Microtubule Formation

(2016) Andrea E. Prota et al.   JOURNAL OF MOLECULAR BIOLOGY

Pironetin reacts covalently with cysteine-316 of α-tubulin to destabilize microtubule

(2016) Jianhong Yang et al.   Nature Communications

Antimitotic drugs in the treatment of cancer

(2015) Rustelle Janse van Vuuren et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

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

(2015) Yuxi Wang et al.   FEBS Journal

The γ-tubulin-specific inhibitor gatastatin reveals temporal requirements of microtubule nucleation during the cell cycle

(2015) Takumi Chinen et al.   Nature Communications

Isogambogenic acid induces apoptosis-independent autophagic cell death in human non-small-cell lung carcinoma cells

(2015) Jianhong Yang et al.   Scientific Reports

Structural Basis of Microtubule Stabilization by Laulimalide and Peloruside A

(2014) Andrea E. Prota et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Recent developments in tubulin polymerization inhibitors: An overview

(2014) Ramandeep Kaur et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Transformation of taxol-stabilized microtubules into inverted tubulin tubules triggered by a tubulin conformation switch

(2014) Miguel A. Ojeda-Lopez et al.   NATURE MATERIALS

A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs

(2014) A. E. Prota et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A phase 2 study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer

(2013) Emmanuel S. Antonarakis et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Targeting Src and Tubulin in Mucinous Ovarian Carcinoma

(2013) T. Liu et al.   CLINICAL CANCER RESEARCH

A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies

(2013) Aung Naing et al.   INVESTIGATIONAL NEW DRUGS

Molecular Mechanism of Action of Microtubule-Stabilizing Anticancer Agents

(2013) A. E. Prota et al.   SCIENCE

KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor α positive breast cancer

(2011) Muralidharan Anbalagan et al.   BREAST CANCER RESEARCH AND TREATMENT

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Quick and Simple Detection Technique to Assess the Binding of Antimicrotubule Agents to the Colchicine-Binding Site

(2010) Sébastien Fortin et al.   BIOLOGICAL PROCEDURES ONLINE

A Phase Ib dose-escalation study to evaluate safety and tolerability of the addition of the aminopeptidase inhibitor tosedostat (CHR-2797) to paclitaxel in patients with advanced solid tumours

(2010) C M L van Herpen et al.   BRITISH JOURNAL OF CANCER

Eribulin Induces Irreversible Mitotic Blockade: Implications of Cell-Based Pharmacodynamics forIn vivoEfficacy under Intermittent Dosing Conditions

(2010) Murray J. Towle et al.   CANCER RESEARCH

Chemotherapy-induced peripheral neuropathy: clinical features, diagnosis, prevention and treatment strategies

(2010) Gerardo Gutiérrez-Gutiérrez et al.   Clinical & Translational Oncology

MolProbity: all-atom structure validation for macromolecular crystallography

(2009) Vincent B. Chen et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Transporter-Mediated Protection against Thiopurine-Induced Hematopoietic Toxicity

(2008) P. Krishnamurthy et al.   CANCER RESEARCH