Structural classification of MELK inhibitors and prospects for the treatment of tumor resistance: A review

Discovery of a new molecule inducing melanoma cell death: dual AMPK/MELK targeting for novel melanoma therapies

(2021) Emilie Jaune et al.   Cell Death & Disease

Consensus Virtual Screening Identified [1,2,4]Triazolo[1,5‐ b ]isoquinolines As MELK Inhibitor Chemotypes

(2021) Anita Rácz et al.   ChemMedChem

NF1-mutated melanomas reveal distinct clinical characteristics depending on tumour origin and respond favourably to immune checkpoint inhibitors

(2021) Carl M. Thielmann et al.   EUROPEAN JOURNAL OF CANCER

Outer Radial Glia-like Cancer Stem Cells Contribute to Heterogeneity of Glioblastoma

(2020) Aparna Bhaduri et al.   Cell Stem Cell

Mass spectrometry–based selectivity profiling identifies a highly selective inhibitor of the kinase MELK that delays mitotic entry in cancer cells

(2020) Ian M. McDonald et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Phillygenin, a MELK Inhibitor, Inhibits Cell Survival and Epithelial–Mesenchymal Transition in Pancreatic Cancer Cells

(2020) Hongchun Li et al.   OncoTargets and Therapy

MELK mediates the stability of EZH2 through site-specific phosphorylation in extranodal natural killer/T-cell lymphoma

(2019) Boheng Li et al.   BLOOD

Design, synthesis, biological evaluation and molecular modeling of novel 1H-pyrrolo[2,3-b]pyridine derivatives as potential anti-tumor agents

(2019) Ruifeng Wang et al.   BIOORGANIC CHEMISTRY

Targeting the ubiquitin-proteasome pathway to overcome anti-cancer drug resistance

(2019) Silpa Narayanan et al.   DRUG RESISTANCE UPDATES

Phillygenin inhibits LPS-induced activation and inflammation of LX2 cells by TLR4/MyD88/NF-κB signaling pathway

(2019) Naihua Hu et al.   JOURNAL OF ETHNOPHARMACOLOGY

Inhibition of maternal embryonic leucine zipper kinase with OTSSP167 displays potent anti-leukemic effects in chronic lymphocytic leukemia

(2018) Ya Zhang et al.   ONCOGENE

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

(2018) Shu Zhou et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Smad proteins differentially regulate obesity-induced glucose and lipid abnormalities and inflammation via class-specific control of AMPK-related kinase MPK38/MELK activity

(2018) Hyun-A Seong et al.   Cell Death & Disease

MELK expression correlates with tumor mitotic activity but is not required for cancer growth

(2018) Christopher J Giuliano et al.   eLife

Drug resistance in multiple myeloma

(2018) Pawel Robak et al.   CANCER TREATMENT REVIEWS

5-Keto-3-cyano-2,4-diaminothiophenes as selective maternal embryonic leucine zipper kinase inhibitors

(2018) Nicolas Boutard et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2018) Lijs Beke et al.   BIOSCIENCE REPORTS

MELK expression in ovarian cancer correlates with poor outcome and its inhibition by OTSSP167 abrogates proliferation and viability of ovarian cancer cells

(2017) Reto S. Kohler et al.   GYNECOLOGIC ONCOLOGY

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

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

MELK Promotes Melanoma Growth by Stimulating the NF-κB Pathway

(2017) Radoslav Janostiak et al.   Cell Reports

MELK is not necessary for the proliferation of basal-like breast cancer cells

(2017) Hai-Tsang Huang et al.   eLife

CRISPR/Cas9 mutagenesis invalidates a putative cancer dependency targeted in on-going clinical trials

(2017) Ann Lin et al.   eLife

Genome-wide effects of MELK-inhibitor in triple-negative breast cancer cells indicate context-dependent response with p53 as a key determinant

(2017) Marisa Simon et al.   PLoS One

Zinc finger protein ZPR9 functions as an activator of AMPK-related serine/threonine kinase MPK38/MELK involved in ASK1/TGF-β/p53 signaling pathways

(2017) Hyun-A Seong et al.   Scientific Reports

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

Carfilzomib and dexamethasone versus bortezomib and dexamethasone for patients with relapsed or refractory multiple myeloma (ENDEAVOR): a randomised, phase 3, open-label, multicentre study

(2016) Meletios A Dimopoulos et al.   LANCET ONCOLOGY

MELK kinase holds promise as a new radiosensitizing target and biomarker in triple-negative breast cancer

(2016) Carlos S. Moreno   Journal of Thoracic Disease

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

Tunable-Combinatorial Mechanisms of Acquired Resistance Limit the Efficacy of BRAF/MEK Cotargeting but Result in Melanoma Drug Addiction

(2015) Gatien Moriceau et al.   CANCER CELL

Maternal embryonic leucine zipper kinase serves as a poor prognosis marker and therapeutic target in gastric cancer

(2015) Shen Li et al.   Oncotarget

EZH2 Protects Glioma Stem Cells from Radiation-Induced Cell Death in a MELK/FOXM1-Dependent Manner

(2015) Sung-Hak Kim et al.   Stem Cell Reports

Melanoma

(2015) Dirk Schadendorf et al.   Nature Reviews Disease Primers

Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer

(2015) Suyoun Chung et al.   Oncotarget

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

(2015) Houda Alachkar et al.   Oncotarget

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

(2014) Tao Du et al.   Molecular Cancer

Multi-Kinase Inhibitor C1 Triggers Mitotic Catastrophe of Glioma Stem Cells Mainly through MELK Kinase Inhibition

(2014) Mutsuko Minata et al.   PLoS One

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

MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells

(2014) Yubao Wang et al.   eLife

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

(2013) Giulia Canevari et al.   BIOCHEMISTRY

The Somatic Genomic Landscape of Glioblastoma

(2013) Cameron W. Brennan et al.   CELL

MELK inhibitor, novel molecular targeted therapeutics for human cancer stem cells

(2013) Suyoun Chung et al.   CELL CYCLE

Thioredoxin inhibits MPK38-induced ASK1, TGF‐β, and p53 function in a phosphorylation-dependent manner

(2013) Ravi Manoharan et al.   FREE RADICAL BIOLOGY AND MEDICINE

MELK-Dependent FOXM1 Phosphorylation is Essential for Proliferation of Glioma Stem Cells

(2013) Kaushal Joshi et al.   STEM CELLS

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

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

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

Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages

(2012) K. Clark et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Benzo[e]pyridoindoles,  novel inhibitors of the Aurora kinases

(2011) Thi My-Nhung Hoang et al.   CELL CYCLE

Maternal Embryonic Leucine Zipper Kinase Is Upregulated and Required in Mammary Tumor-Initiating Cells In vivo

(2010) L. W. Hebbard et al.   CANCER RESEARCH

Kinase Associated-1 Domains Drive MARK/PAR1 Kinases to Membrane Targets by Binding Acidic Phospholipids

(2010) Katarina Moravcevic et al.   CELL

Murine Protein Serine/Threonine Kinase 38 Stimulates TGF-β Signaling in a Kinase-dependent Manner via Direct Phosphorylation of Smad Proteins

(2010) Hyun-A Seong et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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