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

Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as novel and potent TBK1 inhibitors: design, synthesis, biological evaluation, and molecular docking study

(2022) Yin Sun et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

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

(2022) Chandra K. Singh et al.   PROSTATE

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

Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo

(2022) Tianxiao Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3β

(2021) Matthew P. Davies et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation

(2021) Wei Yan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor

(2021) Malcolm P. Huestis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of novel 1H-Pyrazolo[3,4-b]pyridine derivatives as DYRK 1A/1B inhibitors

(2021) Areum Park et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration

(2021) Bent Pfaffenrot et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis

(2021) Dana M. Klug et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Inhibition of Polo-like kinase 4 induces mitotic defects and DNA damage in diffuse large B-cell lymphoma

(2021) Yi Zhao et al.   Cell Death & Disease

Intermolecular insights into allosteric inhibition of histone lysine-specific demethylase 1

(2021) Xiangyu Zhang et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A

(2021) Lars Wortmann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular docking, 3D-QSAR, and molecular dynamics simulations of thieno[3,2-b]pyrrole derivatives against anticancer targets of KDM1A/LSD1

(2020) Xiangyu Zhang et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

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

Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants

(2020) Beilei Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant

(2020) Xiaoyang Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Emerging insights into symmetry breaking in centriole duplication: updated view on centriole duplication theory

(2020) Shohei Yamamoto et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Patterns of Genomic Instability in Breast Cancer

(2019) Murugan Kalimutho et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Centriole assembly at a glance

(2019) Pierre Gönczy et al.   JOURNAL OF CELL SCIENCE

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

PLK4: a promising target for cancer therapy

(2019) Yi Zhao et al.   JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY

Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents

(2019) Baowen Qi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives

(2019) Chunlin Zhuang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors

(2019) Ruifeng Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

In silico insight into voltage-gated sodium channel 1.7 inhibition for anti-pain drug discovery

(2018) Mingxing Wang et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Centriole Overduplication is the Predominant Mechanism Leading to Centrosome Amplification in Melanoma

(2018) Ryan A. Denu et al.   MOLECULAR CANCER RESEARCH

Downregulation of miR-10B* is correlated with altered expression of mitotic kinases in osteosarcoma

(2018) Gabriela Molinari Roberto et al.   PATHOLOGY RESEARCH AND PRACTICE

Polo-like kinase 4 inhibition produces polyploidy and apoptotic death of lung cancers

(2018) Masanori Kawakami et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Polo-like kinases and acute leukemia

(2018) Oksana Goroshchuk et al.   ONCOGENE

Targeting the centrosome and polo-like kinase 4 in osteosarcoma

(2018) Fergal C Kelleher et al.   CARCINOGENESIS

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: 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

Pyrazolylamine Derivatives Reveal the Conformational Switching between Type I and Type II Binding Modes of Anaplastic Lymphoma Kinase (ALK)

(2016) Chih-Hsiang Tu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recurrent genetic defects in classical Hodgkin lymphoma cell lines

(2016) S. David Hudnall et al.   LEUKEMIA & LYMPHOMA

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

(2016) Ines Lohse et al.   Oncotarget

Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: Success and challenges

(2015) Bin Yu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Polo-like Kinase 4 Inhibition: A Strategy for Cancer Therapy?

(2014) Andrew J. Holland et al.   CANCER CELL

Discovery of novel type II c-Met inhibitors based on BMS-777607

(2014) Wei Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Nek2 and Plk4: prognostic markers, drivers of breast tumorigenesis and drug resistance

(2014) Mihaela Marina   Frontiers in Bioscience-Landmark

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

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