Spotlight on Volasertib: Preclinical and Clinical Evaluation of a Promising Plk1 Inhibitor

A phase I, dose-escalation study of volasertib combined with nintedanib in advanced solid tumors

(2015) F. de Braud et al.   ANNALS OF ONCOLOGY

BI 6727 and GSK461364 suppress growth and radiosensitize osteosarcoma cells, but show limited cytotoxic effects when combined with conventional treatments

(2015) Rodrigo F.E. Bogado et al.   ANTI-CANCER DRUGS

Activation of the endomitotic spindle assembly checkpoint and thrombocytopenia in Plk1-deficient mice

(2015) M. Trakala et al.   BLOOD

A phase I study of volasertib combined with afatinib, in advanced solid tumors

(2015) Jean-Pascal Machiels et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Phase I trial of volasertib, a Polo-like kinase inhibitor, in Japanese patients with acute myeloid leukemia

(2015) Yukio Kobayashi et al.   CANCER SCIENCE

Identification of synthetic lethality of PLK1 inhibition and microtubule-destabilizing drugs

(2015) M Hugle et al.   CELL DEATH AND DIFFERENTIATION

A Randomized, Open-Label Phase II Trial of Volasertib as Monotherapy and in Combination With Standard-Dose Pemetrexed Compared With Pemetrexed Monotherapy in Second-Line Treatment for Non–Small-Cell Lung Cancer

(2015) Peter M. Ellis et al.   Clinical Lung Cancer

Synergistic induction of apoptosis by a polo-like kinase 1 inhibitor and microtubule-interfering drugs in Ewing sarcoma cells

(2015) Lilly Magdalena Weiß et al.   INTERNATIONAL JOURNAL OF CANCER

Phase I trial of volasertib, a Polo-like kinase inhibitor, plus platinum agents in solid tumors: safety, pharmacokinetics and activity

(2015) Ahmad Awada et al.   INVESTIGATIONAL NEW DRUGS

Therapeutic polo-like kinase 1 inhibition results in mitotic arrest and subsequent cell death of blasts in the bone marrow of AML patients and has similar effects in non-neoplastic cell lines

(2015) Claudia Münch et al.   LEUKEMIA RESEARCH

Human ATP-Binding Cassette Transporter ABCB1 Confers Resistance to Volasertib (BI 6727), a Selective Inhibitor of Polo-like Kinase 1

(2015) Chung-Pu Wu et al.   MOLECULAR PHARMACEUTICS

Understanding the Polo Kinase machine

(2015) V Archambault et al.   ONCOGENE

Targeting Polo-Like Kinases: A Promising Therapeutic Approach for Cancer Treatment

(2015) Xiaoqi Liu   Translational Oncology

Battle of the eternal rivals: restoring functional p53 and inhibiting Polo-like kinase 1 as cancer therapy

(2015) Frank Louwen et al.   Oncotarget

Randomized, phase 2 trial of low-dose cytarabine with or without volasertib in AML patients not suitable for induction therapy

(2014) H. Dohner et al.   BLOOD

Polo-like kinase-1 in DNA damage response

(2014) Sun-Yi Hyun et al.   BMB Reports

A phase I study of two dosing schedules of volasertib (BI 6727), an intravenous polo-like kinase inhibitor, in patients with advanced solid malignancies

(2014) C-C Lin et al.   BRITISH JOURNAL OF CANCER

Kinome-wide Functional Screen Identifies Role of PLK1 in Hormone-Independent, ER-Positive Breast Cancer

(2014) N. E. Bhola et al.   CANCER RESEARCH

Therapeutic targeting of Polo-like kinase-1 and Aurora kinases in T-cell acute lymphoblastic leukemia

(2014) Antonino Maria Spartà et al.   CELL CYCLE

Thoughts on the current assessment of Polo-like kinase inhibitor drug discovery

(2014) Klaus Strebhardt et al.   Expert Opinion on Drug Discovery

Large-Scale Label-Free Comparative Proteomics Analysis of Polo-Like Kinase 1 Inhibition via the Small-Molecule Inhibitor BI 6727 (Volasertib) in BRAFV600E Mutant Melanoma Cells

(2014) Brian D. Cholewa et al.   JOURNAL OF PROTEOME RESEARCH

Discovery and development of the Polo-like kinase inhibitor volasertib in cancer therapy

(2014) B T Gjertsen et al.   LEUKEMIA

Mitotic arrest and slippage induced by pharmacological inhibition of Polo-like kinase 1

(2014) Monika Raab et al.   Molecular Oncology

Polo-like kinases: structural variations lead to multiple functions

(2014) Sihem Zitouni et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

A novel role for Plk4 in regulating cell spreading and motility

(2014) C O Rosario et al.   ONCOGENE

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

In vitro targeting of Polo-like kinase 1 in bladder carcinoma

(2013) María Sol Brassesco et al.   CANCER BIOLOGY & THERAPY

Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma

(2013) J A Pezuk et al.   CANCER GENE THERAPY

The Role of Polo-like Kinase 1 in Carcinogenesis: Cause or Consequence?

(2013) B. D. Cholewa et al.   CANCER RESEARCH

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

(2013) Mourad Sanhaji et al.   CELL CYCLE

Plk1: unexpected roles in DNA replication

(2013) Ranadip Mandal et al.   CELL RESEARCH

Targeting prostate cancer cell lines with polo-like kinase 1 inhibitors as a single agent and in combination with histone deacetylase inhibitors

(2013) Michel D. Wissing et al.   FASEB JOURNAL

Polo-like kinase 2 is a mediator of hedgehog survival signaling in cholangiocarcinoma

(2013) Christian D. Fingas et al.   HEPATOLOGY

Initial testing (stage 1) of the polo-like kinase inhibitor volasertib (BI 6727), by the Pediatric Preclinical Testing Program

(2013) Richard Gorlick et al.   PEDIATRIC BLOOD & CANCER

A High-Content Small Molecule Screen Identifies Sensitivity of Glioblastoma Stem Cells to Inhibition of Polo-Like Kinase 1

(2013) Davide Danovi et al.   PLoS One

Simultaneous PLK1 inhibition improves local tumour control after fractionated irradiation

(2013) Mechthild Krause et al.   RADIOTHERAPY AND ONCOLOGY

Outlier Kinase Expression by RNA Sequencing as Targets for Precision Therapy

(2013) Vishal Kothari et al.   Cancer Discovery

Abstract 2557: Preclinical synergy of Plk1 inhibitors and HDACIs

(2012) Channing J. Paller et al.   CANCER RESEARCH

Abstract 2829: Preclinical characterization of TKM-080301, a lipid nanoparticle formulation of a small interfering RNA directed against polo-like kinase 1

(2012) Sean C. Semple et al.   CANCER RESEARCH

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

(2012) Mourad Sanhaji et al.   CELL CYCLE

Phase i study of the Plk1 inhibitor BI 2536 administered intravenously on three consecutive days in advanced solid tumours

(2012) A. Frost et al.   Current Oncology

The Structure of the Plk4 Cryptic Polo Box Reveals Two Tandem Polo Boxes Required for Centriole Duplication

(2012) Lauren K. Slevin et al.   STRUCTURE

From Plk1 to Plk5

(2011) Guillermo de Cárcer et al.   CELL CYCLE

PLK1 as an oncology target: current status and future potential

(2011) Campbell McInnes et al.   DRUG DISCOVERY TODAY

A phase I, dose-escalation study of the novel Polo-like kinase inhibitor volasertib (BI 6727) in patients with advanced solid tumours

(2011) Patrick Schöffski et al.   EUROPEAN JOURNAL OF CANCER

Polo-like kinases and DNA damage checkpoint: beyond the traditional mitotic functions

(2011) El Mustapha Bahassi   EXPERIMENTAL BIOLOGY AND MEDICINE

Polo-like kinase 1 inhibitors in mono- and combination therapies: a new strategy for treating malignancies

(2011) Daniel C Christoph et al.   Expert Review of Anticancer Therapy

Overexpression of polo-like kinase 1 and its clinical significance in human non-small cell lung cancer

(2011) Zhao-Xia Wang et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

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

Polo-like kinase1 (Plk1) knockdown enhances cisplatin chemosensitivity via up-regulation of p73α in p53 mutant human epidermoid squamous carcinoma cells

(2010) Shilpa Tyagi et al.   BIOCHEMICAL PHARMACOLOGY

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

Future Prospect of RNA Interference for Cancer Therapies

(2010) Eishi Ashihara et al.   CURRENT DRUG TARGETS

Identification of 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazoline Derivatives as a New Class of Orally and Selective Polo-Like Kinase 1 Inhibitors

(2010) Italo Beria et al.   JOURNAL OF MEDICINAL CHEMISTRY

Multifaceted polo-like kinases: drug targets and antitargets for cancer therapy

(2010) Klaus Strebhardt   NATURE REVIEWS DRUG DISCOVERY

Plk4 is required for cytokinesis and maintenance of chromosomal stability

(2010) C. O. Rosario et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Distinct Concentration-Dependent Effects of the Polo-like Kinase 1-Specific Inhibitor GSK461364A, Including Differential Effect on Apoptosis

(2009) A. G. Gilmartin et al.   CANCER RESEARCH

A Pan-Specific Inhibitor of the Polo-Box Domains of Polo-like Kinases Arrests Cancer Cells in Mitosis

(2009) Wolfgang Reindl et al.   CHEMBIOCHEM

Identification and Validation of a Potent Type II Inhibitor of Inactive Polo-like Kinase 1

(2009) Sarah Keppner et al.   ChemMedChem

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

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

The small organic compound HMN-176 delays satisfaction of the spindle assembly checkpoint by inhibiting centrosome-dependent microtubule nucleation

(2009) M. A. DiMaio et al.   MOLECULAR CANCER THERAPEUTICS

Polo-like kinases: conservation and divergence in their functions and regulation

(2009) Vincent Archambault et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

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

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

(2008) Wolfgang Reindl et al.   CHEMISTRY & BIOLOGY

Polo on the Rise—from Mitotic Entry to Cytokinesis with Plk1

(2008) Mark Petronczki et al.   DEVELOPMENTAL CELL

Overexpression of PLK1 is associated with poor survival by inhibiting apoptosis via enhancement of survivin level in esophageal squamous cell carcinoma

(2008) Yan-Bin Feng et al.   INTERNATIONAL JOURNAL OF CANCER

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

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

RNA interference-mediated silencing of thepolo-like kinase 1gene enhances chemosensitivity to gemcitabine in pancreatic adenocarcinoma cells

(2008) C. Yu et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

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

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