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

Discovery of 2,4‐diaminopyrimidine derivatives targeting p21‐activated kinase 4: Biological evaluation and docking studies

(2020) Qiaohua Qin et al.   ARCHIV DER PHARMAZIE

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 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

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

Cep131 overexpression promotes centrosome amplification and colon cancer progression by regulating Plk4 stability

(2019) Dong Hyun Kim et al.   Cell Death & Disease

PLK4: a promising target for cancer therapy

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

Cytochrome P450 research and The Journal of Biological Chemistry

(2018) F. Peter Guengerich   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Novel pyrazolo[3,4- d ]pyrimidine with 4-(1 H -benzimidazol-2-yl)-phenylamine as broad spectrum anticancer agents: Synthesis, cell based assay, topoisomerase inhibition, DNA intercalation and bovine serum albumin studies

(2017) Prinka Singla et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PLK4: a link between centriole biogenesis and cancer

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

TRIM37, a novel E3 ligase for PEX5-mediated peroxisomal matrix protein import

(2017) Wei Wang et al.   JOURNAL OF CELL BIOLOGY

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

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

(2016) Ines Lohse et al.   Oncotarget

Expression of Polo-Like Kinase 4(PLK4) in Breast Cancer and Its Response to Taxane-Based Neoadjuvant Chemotherapy

(2016) Zhenhua Li et al.   Journal of Cancer

Understanding the Polo Kinase machine

(2015) V Archambault et al.   ONCOGENE

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

(2015) Y. L. Wong et al.   SCIENCE

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

Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors

(2013) Jin-Jun Liu et al.   ACS Medicinal Chemistry Letters

Preclinical evaluation of the novel multi-targeted agent R1530

(2011) Kenneth Kolinsky et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Role of Human Liver Microsomes in In Vitro Metabolism of Drugs—A Review

(2009) Sepuri Asha et al.   APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY