Targeting the cell cycle in breast cancer: towards the next phase

KL Thu, I Soria-Bretones, TW Mak, DW Cescon - Cell Cycle, 2018 - Taylor & Francis
Deregulation of the cell cycle is a hallmark of cancer that enables limitless cell division. To
support this malignant phenotype, cells acquire molecular alterations that abrogate or …

Evolving therapeutic strategies to exploit chromosome instability in cancer

LL Thompson, LMP Jeusset, CC Lepage, KJ McManus - Cancers, 2017 - mdpi.com
Cancer is a devastating disease that claims over 8 million lives each year. Understanding
the molecular etiology of the disease is critical to identify and develop new therapeutic …

The spindle assembly checkpoint is a therapeutic vulnerability of CDK4/6 inhibitor–resistant ER+ breast cancer with mitotic aberrations

I Soria-Bretones, KL Thu, J Silvester, J Cruickshank… - Science …, 2022 - science.org
Inhibitors of cyclin-dependent kinases 4 and 6 (CDK4/6i) are standard first-line treatments
for metastatic ER+ breast cancer. However, acquired resistance to CDK4/6i invariably …

TTK inhibition radiosensitizes basal-like breast cancer through impaired homologous recombination

BC Chandler, L Moubadder, CL Ritter… - The Journal of …, 2020 - Am Soc Clin Investig
Increased rates of locoregional recurrence are observed in patients with basal-like breast
cancer (BC) despite the use of radiation therapy (RT); therefore, approaches that result in …

Effects of tumor treating fields (TTFields) on glioblastoma cells are augmented by mitotic checkpoint inhibition

AF Kessler, GE Frömbling, F Gross, M Hahn… - Cell death …, 2018 - nature.com
Tumor treating fields (TTFields) are approved for glioblastoma (GBM) therapy. TTFields
disrupt cell division by inhibiting spindle fiber formation. Spindle assembly checkpoint (SAC) …

TTK inhibition increases cisplatin sensitivity in high-grade serous ovarian carcinoma through the mTOR/autophagy pathway

G Qi, H Ma, Y Li, J Peng, J Chen, B Kong - Cell Death & Disease, 2021 - nature.com
High-grade serous ovarian cancer (HGSOC) is the most lethal gynecological malignancy.
However, the molecular mechanisms underlying HGSOC development, progression …

Development of MPS1 inhibitors: recent advances and perspectives

Y Zeng, X Ren, P Jin, Y Zhang, M Zhuo… - Journal of Medicinal …, 2023 - ACS Publications
Monopolar spindle kinase 1 (MPS1) plays a pivotal role as a dual-specificity kinase
governing spindle assembly checkpoint activation and sister chromatid separation in …

TTK Inhibitors as a Targeted Therapy for CTNNB1 (β-catenin) Mutant Cancers

GJR Zaman, JADM de Roos, MAA Libouban… - Molecular cancer …, 2017 - AACR
The spindle assembly checkpoint kinase TTK (Mps1) is a key regulator of chromosome
segregation and is the subject of novel targeted therapy approaches by small-molecule …

The discovery of a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor for the treatment of triple negative breast cancer initiated from a phenotypic screen

JR Riggs, M Nagy, J Elsner, P Erdman… - Journal of medicinal …, 2017 - ACS Publications
Triple negative breast cancer (TNBC) remains a serious unmet medical need with
discouragingly high relapse rates. We report here the synthesis and structure–activity …

High proliferation rate and a compromised spindle assembly checkpoint confers sensitivity to the MPS1 inhibitor BOS172722 in triple-negative breast cancers

SJ Anderhub, GWY Mak, MD Gurden, A Faisal… - Molecular Cancer …, 2019 - AACR
Abstract BOS172722 (CCT289346) is a highly potent, selective, and orally bioavailable
inhibitor of spindle assembly checkpoint kinase MPS1. BOS172722 treatment alone induces …