Structure-based discovery of new maternal embryonic leucine zipper kinase inhibitors

“Addition” and “Subtraction”: Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors

(2017) Xin Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

NMR-filtered virtual screening leads to non-metal chelating metallo-β-lactamase inhibitors

(2017) Guo-Bo Li et al.   Chemical Science

MELK is an oncogenic kinase essential for early hepatocellular carcinoma recurrence

(2016) Hongping Xia et al.   CANCER LETTERS

Maternal Embryonic Leucine Zipper Kinase (MELK) as a Novel Mediator and Biomarker of Radioresistance in Human Breast Cancer

(2016) C. Speers et al.   CLINICAL CANCER RESEARCH

Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight

(2016) B. Barry Touré et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug Discovery against Psoriasis: Identification of a New Potent FMS-like Tyrosine Kinase 3 (FLT3) Inhibitor, 1-(4-((1H-Pyrazolo[3,4-d]pyrimidin-4-yl)oxy)-3-fluorophenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea, That Showed Potent Activity in a Psoriatic Animal Model

(2016) Guo-Bo Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of new p300 histone acetyltransferase inhibitors from natural products by a customized virtual screening method

(2016) Guo-Bo Li et al.   RSC Advances

MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells

(2015) L. Beke et al.   BIOSCIENCE REPORTS

LEADOPT: An automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors

(2015) Guo-Bo Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Structure–Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer

(2015) Chun-Hui Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Virtual screening in small molecule discovery for epigenetic targets

(2015) Guo-Bo Li et al.   METHODS

Preclinical Evaluation of a Novel Orally Available SRC/Raf/VEGFR2 Inhibitor, SKLB646, in the Treatment of Triple-Negative Breast Cancer

(2015) M.-W. Zheng et al.   MOLECULAR CANCER THERAPEUTICS

Preclinical efficacy of maternal embryonic leucine-zipper kinase (MELK) inhibition in acute myeloid leukemia

(2015) Houda Alachkar et al.   Oncotarget

A preclinical evaluation of a novel multikinase inhibitor, SKLB-329, as a therapeutic agent against hepatocellular carcinoma

(2014) Lei Zhong et al.   INTERNATIONAL JOURNAL OF CANCER

Maternal embryonic leucine zipper kinase enhances gastric cancer progression via the FAK/Paxillin pathway

(2014) Tao Du et al.   Molecular Cancer

Fragment-Based Discovery of Type I Inhibitors of Maternal Embryonic Leucine Zipper Kinase

(2014) Christopher N. Johnson et al.   ACS Medicinal Chemistry Letters

Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase

(2014) Christopher N. Johnson et al.   ACS Medicinal Chemistry Letters

Structural Insight into Maternal Embryonic Leucine Zipper Kinase (MELK) Conformation and Inhibition toward Structure-Based Drug Design

(2013) Giulia Canevari et al.   BIOCHEMISTRY

ID-Score: A New Empirical Scoring Function Based on a Comprehensive Set of Descriptors Related to Protein–Ligand Interactions

(2013) Guo-Bo Li et al.   Journal of Chemical Information and Modeling

Structure–Activity Relationship Studies of Pyrazolo[3,4-d]pyrimidine Derivatives Leading to the Discovery of a Novel Multikinase Inhibitor That Potently Inhibits FLT3 and VEGFR2 and Evaluation of Its Activity against Acute Myeloid Leukemia in Vitro and in Vivo

(2013) Ling-Ling Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tumor-Specific Activation of the C-JUN/MELK Pathway Regulates Glioma Stem Cell Growth in a p53-Dependent Manner

(2013) Chunyu Gu et al.   STEM CELLS

Murine Protein Serine-threonine Kinase 38 Activates p53 Function through Ser15Phosphorylation

(2012) Hyun-A Seong et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The maternal embryonic leucine zipper kinase (MELK) is upregulated in high-grade prostate cancer

(2012) Ruprecht Kuner et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Resistance of colorectal cancer cells to radiation and 5-FU is associated with MELK expression

(2011) Seungho Choi et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Siomycin A targets brain tumor stem cells partially through a MELK-mediated pathway

(2011) I. Nakano et al.   NEURO-ONCOLOGY

Zebrafish developmental toxicity assay: A fishy solution to reproductive toxicity screening, or just a red herring?

(2011) Kathleen Van den Bulck et al.   REPRODUCTIVE TOXICOLOGY

Establishment and characterization of 13 human colorectal carcinoma cell lines: mutations of genes and expressions of drug-sensitivity genes and cancer stem cell markers

(2010) Ja-Lok Ku et al.   CARCINOGENESIS

Murine Protein Serine/Threonine Kinase 38 Activates Apoptosis Signal-regulating Kinase 1 via Thr838Phosphorylation

(2008) Haiyoung Jung et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Maternal embryonic leucine zipper kinase is a key regulator of the proliferation of malignant brain tumors, including brain tumor stem cells

(2007) Ichiro Nakano et al.   JOURNAL OF NEUROSCIENCE RESEARCH