Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia

Polo‐like kinase 4 inhibitor CFI‐400945 suppresses liver cancer through cell cycle perturbation and eliciting antitumor immunity

(2022) Cerise Yuen‐Ki Chan et al.   HEPATOLOGY

Species-Selective Targeting of Fungal Hsp90: Design, Synthesis, and Evaluation of Novel 4,5-Diarylisoxazole Derivatives for the Combination Treatment of Azole-Resistant Candidiasis

(2022) Wenbo Yin et al.   JOURNAL OF MEDICINAL CHEMISTRY

PLK4 is upregulated in prostate cancer and its inhibition reduces centrosome amplification and causes senescence

(2022) Chandra K. Singh et al.   PROSTATE

Role of Polo-like Kinases Plk1 and Plk4 in the Initiation of Centriole Duplication—Impact on Cancer

(2022) Ingrid Hoffmann   Cells

Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer

(2022) Yin Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study

(2022) Yin Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-based discovery of 1-(3-fluoro-5-(5-(3-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)phenyl)-3-(pyrimidin-5-yl)urea as a potent and selective nanomolar type-II PLK4 inhibitor

(2022) Yin Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Polo-Like Kinase 4’s Critical Role in Cancer Development and Strategies for Plk4-Targeted Therapy

(2021) Xiaoyang Zhang et al.   Frontiers in Oncology

Future prospects for mitosis-targeted antitumor therapies

(2021) Alfonso Serrano-del Valle et al.   BIOCHEMICAL PHARMACOLOGY

Anticancer effects of radiation therapy combined with Polo-Like Kinase 4 (PLK4) inhibitor CFI-400945 in triple negative breast cancer

(2021) Armen Parsyan et al.   BREAST

Multifunctional inhibitors of SARS-CoV-2 by MM/PBSA, essential dynamics, and molecular dynamic investigations

(2021) K. Amith Kumar et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Targeting Polo-like Kinase 4 Triggers Polyploidy and Apoptotic Cell Death in TP53-Mutant Acute Myeloid Leukemia

(2021) Edward Ayoub et al.   BLOOD

Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors

(2021) Tianxiao Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Cyclin-Dependent Kinase Inhibitors and Their Therapeutic Potential in Colorectal Cancer Treatment

(2021) Oana-Maria Thoma et al.   Frontiers in Pharmacology

YLZ-F5, a novel polo-like kinase 4 inhibitor, inhibits human ovarian cancer cell growth by inducing apoptosis and mitotic defects

(2020) Yongxia Zhu et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

MiR-654-3p Suppresses Non-Small Cell Lung Cancer Tumourigenesis by Inhibiting PLK4

(2020) Jiang-tao Pu et al.   OncoTargets and Therapy

Targeting TRIM37-driven centrosome dysfunction in 17q23-amplified breast cancer

(2020) Zhong Y. Yeow et al.   NATURE

TRIM37 controls cancer-specific vulnerability to PLK4 inhibition

(2020) Franz Meitinger et al.   NATURE

Centrosomes in mitotic spindle assembly and orientation

(2020) Ingrid Hoffmann   CURRENT OPINION IN STRUCTURAL BIOLOGY

Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer

(2019) Amreena Suri et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Cytochrome P450 research and The Journal of Biological Chemistry

(2018) F. Peter Guengerich   JOURNAL OF BIOLOGICAL CHEMISTRY

Polo-like kinase 4 mediates epithelial–mesenchymal transition in neuroblastoma via PI3K/Akt signaling pathway

(2018) Xiangdong Tian et al.   Cell Death & Disease

Polo-like kinases and acute leukemia

(2018) Oksana Goroshchuk et al.   ONCOGENE

CFI-400945 is not a selective cellular PLK4 inhibitor

(2018) Karen Oegema et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

YLT-11, a novel PLK4 inhibitor, inhibits human breast cancer growth via inducing maladjusted centriole duplication and mitotic defect

(2018) Qian Lei et al.   Cell Death & Disease

PLK4 is a determinant of temozolomide sensitivity through phosphorylation of IKBKE in glioblastoma

(2018) Zuoxin Zhang et al.   CANCER LETTERS

PLK4: a link between centriole biogenesis and cancer

(2017) Radhika Radha Maniswami et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors

(2017) Chenzhou Hao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of (E)-4-(3-arylvinyl-1H-indazol-6-yl)pyrimidin-2-amine derivatives as PLK4 inhibitors for the treatment of breast cancer

(2017) Zhihao Liu et al.   RSC Advances

Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia

(2016) Xiaofei Liang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Aurora-A Kinase: A Potent Oncogene and Target for Cancer Therapy

(2016) Min Yan et al.   MEDICINAL RESEARCH REVIEWS

Discovery and characterization of a novel potent type II native and mutant BCR-ABL inhibitor (CHMFL-074) for Chronic Myeloid Leukemia (CML)

(2016) Feiyang Liu et al.   Oncotarget

Activity of the novel polo-like kinase 4 inhibitor CFI-400945 in pancreatic cancer patient-derived xenografts

(2016) Ines Lohse et al.   Oncotarget

Targeting Mitosis in Cancer: Emerging Strategies

(2015) Carmen Dominguez-Brauer et al.   MOLECULAR CELL

Transient PLK4 overexpression accelerates tumorigenesis in p53-deficient epidermis

(2015) Özdemirhan Serçin et al.   NATURE CELL BIOLOGY

Autoinhibition and relief mechanism for Polo-like kinase 4

(2015) Joseph E. Klebba et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Reversible centriole depletion with an inhibitor of Polo-like kinase 4

(2015) Y. L. Wong et al.   SCIENCE

Pyrazolopyrimidines Establish MurC as a Vulnerable Target in Pseudomonas aeruginosa and Escherichia coli

(2014) Shahul Hameed P et al.   ACS Chemical Biology

The Discovery of Polo-Like Kinase 4 Inhibitors: Identification of (1R,2S)-2-(3-((E)-4-(((cis)-2,6-Dimethylmorpholino)methyl)styryl)-1H-indazol-6-yl)-5′-methoxyspiro[cyclopropane-1,3′-indolin]-2′-one (CFI-400945) as a Potent, Orally Active Antitumor Agent

(2014) Peter B. Sampson et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Discovery of Polo-Like Kinase 4 Inhibitors: Design and Optimization of Spiro[cyclopropane-1,3′[3H]indol]-2′(1′H)-ones as Orally Bioavailable Antitumor Agents

(2014) Peter B. Sampson et al.   JOURNAL OF MEDICINAL CHEMISTRY

PLK4 overexpression and its effect on centrosome regulation and chromosome stability in human gastric cancer

(2014) Kazuya Shinmura et al.   MOLECULAR BIOLOGY REPORTS

Polo-like kinases: structural variations lead to multiple functions

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

Polo-like Kinase 4 Shapes Up

(2014) Michelle S. Levine et al.   STRUCTURE

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

Polo-like kinase 4 transcription is activated via CRE and NRF1 elements, repressed by DREAM through CDE/CHR sites and deregulated by HPV E7 protein

(2013) Martin Fischer et al.   NUCLEIC ACIDS RESEARCH

SAPK pathways and p53 cooperatively regulate PLK4 activity and centrosome integrity under stress

(2013) Takanori Nakamura et al.   Nature Communications

Cell cycle regulation by the NEK family of protein kinases

(2012) A. M. Fry et al.   JOURNAL OF CELL SCIENCE

The SCF–FBXW5 E3-ubiquitin ligase is regulated by PLK4 and targets HsSAS-6 to control centrosome duplication

(2011) Anja Puklowski et al.   NATURE CELL BIOLOGY