Property Summary

NCBI Gene PubMed Count 36
Grant Count 26
R01 Count 19
Funding $2,056,379.25
PubMed Score 72.18
PubTator Score 54.97

Knowledge Summary

Patent (25,749)

Expression

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.
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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
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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.
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