Mps1 inhibitors synergise with low doses of taxanes in promoting tumour cell death by enhancement of errors in cell division

Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer

(2017) Jacqueline M. Mason et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK

(2016) Radoslaw Laufer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Living in CIN: Mitotic Infidelity and Its Consequences for Tumor Promotion and Suppression

(2016) Laura C. Funk et al.   DEVELOPMENTAL CELL

Mps1/TTK: a novel target and biomarker for cancer

(2016) Yuan Xie et al.   JOURNAL OF DRUG TARGETING

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach

(2016) Paolo Innocenti et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity

(2016) A. M. Wengner et al.   MOLECULAR CANCER THERAPEUTICS

Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent

(2016) Yong Liu et al.   ACS Medicinal Chemistry Letters

Inhibition of the spindle assembly checkpoint kinase TTK enhances the efficacy of docetaxel in a triple-negative breast cancer model

(2015) A. R. R. Maia et al.   ANNALS OF ONCOLOGY

A unique hinge binder of extremely selective aminopyridine-based Mps1 (TTK) kinase inhibitors with cellular activity

(2015) Ken-ichi Kusakabe et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of Imidazo[1,2-b]pyridazine Derivatives: Selective and Orally Available Mps1 (TTK) Kinase Inhibitors Exhibiting Remarkable Antiproliferative Activity

(2015) Ken-ichi Kusakabe et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents

(2015) Yong Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular basis underlying resistance to Mps1/TTK inhibitors

(2015) A Koch et al.   ONCOGENE

Mitotic Checkpoint Kinase Mps1 Has a Role in Normal Physiology which Impacts Clinical Utility

(2015) Ricardo Martinez et al.   PLoS One

Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides

(2014) Radoslaw Laufer et al.   BIOORGANIC & MEDICINAL CHEMISTRY

How Taxol/paclitaxel kills cancer cells

(2014) Beth A. Weaver   MOLECULAR BIOLOGY OF THE CELL

Cytotoxicity of Paclitaxel in Breast Cancer Is due to Chromosome Missegregation on Multipolar Spindles

(2014) L. M. Zasadil et al.   Science Translational Medicine

Characterization of novel MPS1 inhibitors with preclinical anticancer activity

(2013) M Jemaà et al.   CELL DEATH AND DIFFERENTIATION

Indazole-Based Potent and Cell-Active Mps1 Kinase Inhibitors: Rational Design from Pan-Kinase Inhibitor Anthrapyrazolone (SP600125)

(2013) Ken-ichi Kusakabe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of Orally Bioavailable 1H-Pyrrolo[3,2-c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

(2013) Sébastien Naud et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effects of the Selective MPS1 Inhibitor MPS1-IN-3 on Glioblastoma Sensitivity to Antimitotic Drugs

(2013) Bakhos A. Tannous et al.   JNCI-Journal of the National Cancer Institute

Taxane benefit in breast cancer—a role for grade and chromosomal stability

(2013) Roger P. A'Hern et al.   Nature Reviews Clinical Oncology

2n or not 2n: Aneuploidy, polyploidy and chromosomal instability in primary and tumor cells

(2013) Lauren M. Zasadil et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

The MPS1 Family of Protein Kinases

(2012) Xuedong Liu et al.   Annual Review of Biochemistry

Genetic instability: tipping the balance

(2012) A Janssen et al.   ONCOGENE

Diaminopyridine-Based Potent and Selective Mps1 Kinase Inhibitors Binding to an Unusual Flipped-Peptide Conformation

(2012) Ken-ichi Kusakabe et al.   ACS Medicinal Chemistry Letters

Loss of 53BP1 Causes PARP Inhibitor Resistance in Brca1 -Mutated Mouse Mammary Tumors

(2012) Janneke E. Jaspers et al.   Cancer Discovery

Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors

(2011) Marina Caldarelli et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Relationship of Extreme Chromosomal Instability with Long-term Survival in a Retrospective Analysis of Primary Breast Cancer

(2011) R. Roylance et al.   CANCER EPIDEMIOLOGY BIOMARKERS & PREVENTION

Paradoxical Relationship between Chromosomal Instability and Survival Outcome in Cancer

(2011) N. J. Birkbak et al.   CANCER RESEARCH

Characterization of the Cellular and Antitumor Effects of MPI-0479605, a Small-Molecule Inhibitor of the Mitotic Kinase Mps1

(2011) K. D. Tardif et al.   MOLECULAR CANCER THERAPEUTICS

Targeting the Mitotic Checkpoint for Cancer Therapy with NMS-P715, an Inhibitor of MPS1 Kinase

(2010) R. Colombo et al.   CANCER RESEARCH

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function

(2010) Nicholas Kwiatkowski et al.   Nature Chemical Biology

Elevating the frequency of chromosome mis-segregation as a strategy to kill tumor cells

(2009) Aniek Janssen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective Inhibition of BRCA2-Deficient Mammary Tumor Cell Growth by AZD2281 and Cisplatin

(2008) B. Evers et al.   CLINICAL CANCER RESEARCH