Property Summary

NCBI Gene PubMed Count 36
PubMed Score 72.18
PubTator Score 54.97

Knowledge Summary

Patent (25,749)

Expression

  Differential Expression (26)

Disease log2 FC p
malignant mesothelioma 1.500 5.6e-07
psoriasis 3.200 6.0e-05
glioblastoma 3.400 3.1e-06
posterior fossa group A ependymoma 1.900 1.1e-06
group 3 medulloblastoma 3.700 1.6e-09
atypical teratoid/rhabdoid tumor 3.600 2.3e-16
medulloblastoma, large-cell 3.000 1.0e-06
primitive neuroectodermal tumor 3.100 5.3e-06
Atopic dermatitis 1.500 2.9e-05
adrenocortical carcinoma 2.637 5.0e-05
non-small cell lung cancer 3.422 1.3e-37
intraductal papillary-mucinous carcinoma... 3.500 1.6e-04
intraductal papillary-mucinous neoplasm ... 4.500 6.2e-04
lung cancer 3.200 8.8e-06
colon cancer 1.900 4.1e-04
pancreatic cancer 1.600 4.2e-06
interstitial cystitis 1.400 2.2e-02
lung adenocarcinoma 2.000 1.7e-08
pediatric high grade glioma 3.200 8.1e-08
nasopharyngeal carcinoma 1.400 1.1e-04
Endometriosis 1.627 7.3e-03
Breast cancer 3.400 3.7e-25
breast carcinoma 1.900 2.7e-39
ductal carcinoma in situ 2.300 2.1e-03
invasive ductal carcinoma 2.700 8.6e-04
ovarian cancer 2.300 1.9e-03

MLP Assay (1)

AID Type Active / Inconclusive / Inactive Description
1982 other 0 / 0 / 0 Kinase inhibition selectivity assay for compound SID-48409448

Gene RIF (22)

PMID Text
26431963 targeting MELK by the inhibition of both its catalytic activity and its protein stability might sensitize tumours to DNA-damaging agents or radiation therapy by lowering the DNA-damage threshold
25601206 EZH2 protects glioma stem cells from radiation-induced cell death in a MELK/FOXM1-dependent manner
25365263 we report characterization of possible roles of MELK in acute myeloid leukemia
25017123 insight has been brought by the discovery of a protein complex of FOXM1 with the mitotic kinase MELK in cancer stem cells in brain cancers, as this protein complex appears to be cancer-specific
24885567 MELK promotes cell migration and invasion via the FAK/Paxillin pathway, and plays an important role in the occurrence and development of gastric cancer.
24844244 Together, these data indicate that MELK is a normally non-essential kinase, but is critical for basal-like breast cancer.
24795222 advanced cancers with OTSSP167 started in 2013, as the first-in-class MELK inhibitor. This review summarizes the current molecular understanding of MELK and the recent preclinical studies about MELK as a cancer therapeutic target.
24185907 our current knowledge of MELK function and recent discoveries in MELK signaling pathway were discussed.
23922895 The structural and biochemical analyses unravel the molecular mechanisms for the autophosphorylation/activation of MELK and the dependence of its catalytic activity on reducing agents.
23836907 glioblastoma cells have elevated MELK protein levels to better cope with replication stress during unperturbed S phase.
23357462 Data indicate that expression-based risk indices of three genes UBE2C, TPX2, and MELK were more strongly associated with poor 5-year survival in adenocarcinoma patients.
23283305 Report MELK inhibitor that suppresses the growth of a wide range of human tumor cell lines.
22945237 MELK is upregulated in high-grade prostate cancer
21806965 MELK could be associated with increased resistance of colorectal cancer cells against radiation and 5-FU.
21558073 High MELK is associated with brain tumor.
20433920 HIV-1 Tat-peptide(48-60) inhibits AGC-family kinases (PKB, SGK1, S6K1, MSK1), CAMK-family kinases (CAMK1 and MELK) and a STE family kinase (MKK1)
19671159 MELK expression is increased in breast cancer tissue and this is associated with poor survival. The most important factors controlling Bcl-G activity are post-translational modification by Fau & MELK.
17960622 Maternal embryonic leucine zipper kinase transcript abundance correlates with malignancy grade in astrocytomas
17722061 a critical role for MELK in the proliferation of brain tumors, including their stem cells, and suggest that MELK may be a compelling molecular target for treatment of high-grade brain tumors.
17280616 the kinase activity of MELK is likely to affect mammary carcinogenesis through inhibition of the pro-apoptotic function of Bcl-GL
16216881 analysis of MELK substrate specificity and activity regulation
12400006 pEg3 is a potential regulator of the G2/M progression and may act antagonistically to the CDC25B phosphatase,pEg3 kinase is able to specifically phosphorylate CDC25B in vitro. One phosphorylation site was identified and corresponded to serine 323

AA Sequence

MKDYDELLKYYELHETIGTGGFAKVKLACHILTGEMVAIKIMDKNTLGSDLPRIKTEIEALKNLRHQHIC      1 - 70
QLYHVLETANKIFMVLEYCPGGELFDYIISQDRLSEEETRVVFRQIVSAVAYVHSQGYAHRDLKPENLLF     71 - 140
DEYHKLKLIDFGLCAKPKGNKDYHLQTCCGSLAYAAPELIQGKSYLGSEADVWSMGILLYVLMCGFLPFD    141 - 210
DDNVMALYKKIMRGKYDVPKWLSPSSILLLQQMLQVDPKKRISMKNLLNHPWIMQDYNYPVEWQSKNPFI    211 - 280
HLDDDCVTELSVHHRNNRQTMEDLISLWQYDHLTATYLLLLAKKARGKPVRLRLSSFSCGQASATPFTDI    281 - 350
KSNNWSLEDVTASDKNYVAGLIDYDWCEDDLSTGAATPRTSQFTKYWTESNGVESKSLTPALCRTPANKL    351 - 420
KNKENVYTPKSAVKNEEYFMFPEPKTPVNKNQHKREILTTPNRYTTPSKARNQCLKETPIKIPVNSTGTD    421 - 490
KLMTGVISPERRCRSVELDLNQAHMEETPKRKGAKVFGSLERGLDKVITVLTRSKRKGSARDGPRRLKLH    491 - 560
YNVTTTRLVNPDQLLNEIMSILPKKHVDFVQKGYTLKCQTQSDFGKVTMQFELEVCQLQKPDVVGIRRQR    561 - 630
LKGDAWVYKRLVEDILSSCKV                                                     631 - 651
//

Text Mined References (49)

PMID Year Title
26431963 2015 MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells.
25601206 2015 EZH2 protects glioma stem cells from radiation-induced cell death in a MELK/FOXM1-dependent manner.
25365263 2014 Preclinical efficacy of maternal embryonic leucine-zipper kinase (MELK) inhibition in acute myeloid leukemia.
25017123 2014 Transcription factors as master regulator for cancer stemness: remove milk from fox?
24885567 2014 Maternal embryonic leucine zipper kinase enhances gastric cancer progression via the FAK/Paxillin pathway.
24844244 2014 MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.
24795222 2014 Maternal embryonic leucine zipper kinase: key kinase for stem cell phenotype in glioma and other cancers.
24185907 2013 Maternal embryonic leucine zipper kinase (MELK): a novel regulator in cell cycle control, embryonic development, and cancer.
23922895 2013 Structural basis for the regulation of maternal embryonic leucine zipper kinase.
23836907 2013 Maternal embryonic leucine zipper kinase (MELK) reduces replication stress in glioblastoma cells.
23357462 2013 Network-based approach identified cell cycle genes as predictor of overall survival in lung adenocarcinoma patients.
23283305 2012 Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer.
23186163 2013 Toward a comprehensive characterization of a human cancer cell phosphoproteome.
22945237 2013 The maternal embryonic leucine zipper kinase (MELK) is upregulated in high-grade prostate cancer.
21806965 2011 Resistance of colorectal cancer cells to radiation and 5-FU is associated with MELK expression.
21558073 2011 Siomycin A targets brain tumor stem cells partially through a MELK-mediated pathway.
21145462 2010 Kinase associated-1 domains drive MARK/PAR1 kinases to membrane targets by binding acidic phospholipids.
20861186 2010 Maternal embryonic leucine zipper kinase is upregulated and required in mammary tumor-initiating cells in vivo.
20420823 2010 Maternal embryonic leucine zipper kinase is stabilized in mitosis by phosphorylation and is partially degraded upon mitotic exit.
19946888 2010 Defining the membrane proteome of NK cells.
19690332 2009 Quantitative phosphoproteomic analysis of T cell receptor signaling reveals system-wide modulation of protein-protein interactions.
19671159 2009 Dysregulated expression of Fau and MELK is associated with poor prognosis in breast cancer.
19369195 2009 Large-scale proteomics analysis of the human kinome.
18691976 2008 Kinase-selective enrichment enables quantitative phosphoproteomics of the kinome across the cell cycle.
18669648 2008 A quantitative atlas of mitotic phosphorylation.
17960622 2008 Maternal embryonic leucine zipper kinase transcript abundance correlates with malignancy grade in human astrocytomas.
17722061 2008 Maternal embryonic leucine zipper kinase is a key regulator of the proliferation of malignant brain tumors, including brain tumor stem cells.
17344846 2007 Patterns of somatic mutation in human cancer genomes.
17280616 2007 Involvement of maternal embryonic leucine zipper kinase (MELK) in mammary carcinogenesis through interaction with Bcl-G, a pro-apoptotic member of the Bcl-2 family.
17081983 2006 Global, in vivo, and site-specific phosphorylation dynamics in signaling networks.
16628004 2006 M-phase MELK activity is regulated by MPF and MAPK.
16344560 2006 Diversification of transcriptional modulation: large-scale identification and characterization of putative alternative promoters of human genes.
16266996 2005 Maternal embryonic leucine zipper kinase/murine protein serine-threonine kinase 38 is a promising therapeutic target for multiple cancers.
16216881 2005 Substrate specificity and activity regulation of protein kinase MELK.
16159311 2006 Cell-cycle-dependent cortical localization of pEg3 protein kinase in Xenopus and human cells.
15908796 2005 CDC25B phosphorylated by pEg3 localizes to the centrosome and the spindle poles at mitosis.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
15342556 2004 Sequence comparison of human and mouse genes reveals a homologous block structure in the promoter regions.
15164053 2004 DNA sequence and analysis of human chromosome 9.
14976552 2004 LKB1 is a master kinase that activates 13 kinases of the AMPK subfamily, including MARK/PAR-1.
14702039 2004 Complete sequencing and characterization of 21,243 full-length human cDNAs.
14699119 2004 Inhibition of spliceosome assembly by the cell cycle-regulated protein kinase MELK and involvement of splicing factor NIPP1.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12400006 2002 Human pEg3 kinase associates with and phosphorylates CDC25B phosphatase: a potential role for pEg3 in cell cycle regulation.
11802789 2002 Phosphorylation of a novel zinc-finger-like protein, ZPR9, by murine protein serine/threonine kinase 38 (MPK38).
9305775 1997 Cloning and expression of a cDNA encoding a novel protein serine/threonine kinase predominantly expressed in hematopoietic cells.
9136115 1997 New member of the Snf1/AMPK kinase family, Melk, is expressed in the mouse egg and preimplantation embryo.
8724849 1996 Prediction of the coding sequences of unidentified human genes. V. The coding sequences of 40 new genes (KIAA0161-KIAA0200) deduced by analysis of cDNA clones from human cell line KG-1.
8125298 1994 Oligo-capping: a simple method to replace the cap structure of eukaryotic mRNAs with oligoribonucleotides.