Current assessment of polo-like kinases as anti-tumor drug targets

Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1)

(2013) Zhe Nie et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An open-label, single-arm, phase 2 trial of the polo-like kinase inhibitor volasertib (BI 6727) in patients with locally advanced or metastatic urothelial cancer

(2013) Walter M. Stadler et al.   CANCER

Polo-like kinase 1 inhibitors, mitotic stress and the tumor suppressor p53

(2013) Mourad Sanhaji et al.   CELL CYCLE

Optimization of Non-ATP Competitive CDK/Cyclin Groove Inhibitors through REPLACE-Mediated Fragment Assembly

(2013) Shu Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Discovery of PLK4 Inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as Novel Antiproliferative Agents

(2013) Radoslaw Laufer et al.   JOURNAL OF MEDICINAL CHEMISTRY

In vivo modulation of polo-like kinases supports a key role for PLK2 in Ser129 α-synuclein phosphorylation in mouse brain

(2013) M. Bergeron et al.   NEUROSCIENCE

Enabling and Disabling Polo-like Kinase 1 Inhibition through Chemical Genetics

(2012) Mark E. Burkard et al.   ACS Chemical Biology

In vivo tumor imaging using polo-box domain of polo-like kinase 1 targeted peptide

(2012) Sung-Min Kim et al.   BIOMATERIALS

 p53 is not directly relevant to the response of Polo-like kinase 1 inhibitors

(2012) Mourad Sanhaji et al.   CELL CYCLE

Targeting Subcellular Localization through the Polo-Box Domain: Non-ATP Competitive Inhibitors Recapitulate a PLK1 Phenotype

(2012) C. McInnes et al.   MOLECULAR CANCER THERAPEUTICS

The functions and regulation of the PTEN tumour suppressor

(2012) Min Sup Song et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Polo-Box Domain Inhibitor Poloxin Activates the Spindle Assembly Checkpoint and Inhibits Tumor Growth in Vivo

(2011) Juping Yuan et al.   AMERICAN JOURNAL OF PATHOLOGY

Nuclear PTEN Regulates the APC-CDH1 Tumor-Suppressive Complex in a Phosphatase-Independent Manner

(2011) Min Sup Song et al.   CELL

From Plk1 to Plk5

(2011) Guillermo de Cárcer et al.   CELL CYCLE

Phase I Study of GSK461364, a Specific and Competitive Polo-like Kinase 1 Inhibitor, in Patients with Advanced Solid Malignancies

(2011) D. Olmos et al.   CLINICAL CANCER RESEARCH

PLK1 as an oncology target: current status and future potential

(2011) Campbell McInnes et al.   DRUG DISCOVERY TODAY

Polo-like Kinase 1 Facilitates Loss of Pten Tumor Suppressor-induced Prostate Cancer Formation

(2011) X. Shawn Liu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Plk5, a Polo Box Domain-Only Protein with Specific Roles in Neuron Differentiation and Glioblastoma Suppression

(2011) G. de Carcer et al.   MOLECULAR AND CELLULAR BIOLOGY

TAK-960, a Novel, Orally Available, Selective Inhibitor of Polo-Like Kinase 1, Shows Broad-spectrum Preclinical Antitumor Activity in Multiple Dosing Regimens

(2011) Y. Hikichi et al.   MOLECULAR CANCER THERAPEUTICS

Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel

(2011) Fa Liu et al.   Nature Chemical Biology

Toxicity modelling of Plk1-targeted therapies in genetically engineered mice and cultured primary mammalian cells

(2011) Monika Raab et al.   Nature Communications

Polo-Like Kinase 1 as Predictive Marker and Therapeutic Target for Radiotherapy in Rectal Cancer

(2010) Franz Rödel et al.   AMERICAN JOURNAL OF PATHOLOGY

Human Plk4 phosphorylates Cdc25C

(2010) Sepal Bonni et al.   CELL CYCLE

Polo-like kinase 1 (Plk1) in non-melanoma skin cancers

(2010) Travis Schmit et al.   CELL CYCLE

p53-dependent repression of polo-like kinase-1 (PLK1)

(2010) Lynsey McKenzie et al.   CELL CYCLE

An Open-Label, Phase I Study of the Polo-like Kinase-1 Inhibitor, BI 2536, in Patients with Advanced Solid Tumors

(2010) R.-D. Hofheinz et al.   CLINICAL CANCER RESEARCH

Polo-like kinase 1 phosphorylation of G2 and S-phase-expressed 1 protein is essential for p53 inactivation during G2 checkpoint recovery

(2010) X Shawn Liu et al.   EMBO REPORTS

Multicentric parallel phase II trial of the polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research and Treatment of Cancer (EORTC) Network Of Core Institutes (NOCI)

(2010) Patrick Schöffski et al.   EUROPEAN JOURNAL OF CANCER

Regulation of PTEN Stability and Activity by Plk3

(2010) Dazhong Xu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cep152 interacts with Plk4 and is required for centriole duplication

(2010) Emily M. Hatch et al.   JOURNAL OF CELL BIOLOGY

The Efficacy and Safety of BI 2536, a Novel Plk-1 Inhibitor, in Patients with Stage IIIB/IV Non-small Cell Lung Cancer Who Had Relapsed after, or Failed, Chemotherapy: Results from an Open-Label, Randomized Phase II Clinical Trial

(2010) Martin Sebastian et al.   Journal of Thoracic Oncology

Sensitivity of Cancer Cells to Plk1 Inhibitor GSK461364A Is Associated with Loss of p53 Function and Chromosome Instability

(2010) Y. Degenhardt et al.   MOLECULAR CANCER THERAPEUTICS

The novel mouse Polo-like kinase 5 responds to DNA damage and localizes in the nucleolus

(2010) Zdenek Andrysik et al.   NUCLEIC ACIDS RESEARCH

Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding

(2009) Kyle A. Emmitte et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Gene expression patterns in heterozygous Plk4 murine embryonic fibroblasts

(2009) Alan Morettin et al.   BMC GENOMICS

A Genome-wide RNAi Screen Identifies Multiple Synthetic Lethal Interactions with the Ras Oncogene

(2009) Ji Luo et al.   CELL

BI 6727, A Polo-like Kinase Inhibitor with Improved Pharmacokinetic Profile and Broad Antitumor Activity

(2009) D. Rudolph et al.   CLINICAL CANCER RESEARCH

Plk1-mediated Phosphorylation of Topors Regulates p53 Stability

(2009) Xiaoming Yang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeted Depletion of Polo-Like Kinase (Plk) 1 Through Lentiviral shRNA or a Small-Molecule Inhibitor Causes Mitotic Catastrophe and Induction of Apoptosis in Human Melanoma Cells

(2009) Travis L. Schmit et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Structural and functional analyses of minimal phosphopeptides targeting the polo-box domain of polo-like kinase 1

(2009) Sang-Moon Yun et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

A panel of isogenic human cancer cells suggests a therapeutic approach for cancers with inactivated p53

(2009) S. Sur et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Polo-like Kinase 3 Functions as a Tumor Suppressor and Is a Negative Regulator of Hypoxia-Inducible Factor-1  under Hypoxic Conditions

(2008) Y. Yang et al.   CANCER RESEARCH

Inhibition of Polo-like Kinase 1 by Blocking Polo-Box Domain-Dependent Protein-Protein Interactions

(2008) Wolfgang Reindl et al.   CHEMISTRY & BIOLOGY

Deficiency in Chromosome Congression by the Inhibition of Plk1 Polo Box Domain-dependent Recognition

(2008) Nobumoto Watanabe et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Phase I Dose Escalation and Pharmacokinetic Study of BI 2536, a Novel Polo-Like Kinase 1 Inhibitor, in Patients With Advanced Solid Tumors

(2008) Klaus Mross et al.   JOURNAL OF CLINICAL ONCOLOGY

Polo-Like Kinase 1 Is Essential for Early Embryonic Development and Tumor Suppression

(2008) L.-Y. Lu et al.   MOLECULAR AND CELLULAR BIOLOGY