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Identification of CLK1 Inhibitors by a Fragment–linking Based Virtual Screening
Molecular Informatics, 2016AbstractAlternative splicing plays an important role in the regulation of protein biosynthesis. CDC2‐like kinases (CLKs) phosphorylate splicing factors rendering them a potential target for treating diseases caused by splicing dysregulation. As selective and potent inhibitors of CLK1 are still lacking, a fragment‐linking based virtual screening ...
Walter +8 more
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CLK1 Activates YAP to Promote Intrahepatic Cholangiocarcinogenesis
Cancer ResearchAbstract Cdc2-like kinase 1 (CLK1) has dual-specificity kinase ability to phosphorylate tyrosine and serine/threonine protein residues. CLK1 regulates many physiologic processes and has been shown to contribute to multiple types of cancer.
Shuai Xue +12 more
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Human CDC2-Like Kinase 1 (CLK1): A Novel Target for Alzheimer’s Disease
Current Drug Targets, 2014The cdc2-like kinases (CLKs) are an evolutionarily conserved group of dual specificity kinases belonging to the CMGC (cyclin-dependent kinases (CDKs), mitogen-activated protein kinases (MAP kinases), glycogen synthase kinases (GSK) and CDK-like kinases). The CLK family consists of four isoforms namely CLK1, CLK2, CLK3 and CLK4.
Princi, Jain +5 more
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Acta Pharmacologica SinicaMitochondria are not only the most important organelles in eukaryotic cells that participate in energy metabolism, signal transduction, cell apoptosis and other physiological processes, but also essential regulators of neurodevelopment, neuroplasticity, survival and adult neurogenesis.
John L Waddington +2 more
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Development of Selective Clk1 and -4 Inhibitors for Cellular Depletion of Cancer-Relevant Proteins
Journal of Medicinal Chemistry, 2017In cancer cells, kinases of the Clk family control the supply of full-length, functional mRNAs coding for a variety of proteins essential to cell growth and survival. Thus, inhibition of Clks might become a novel anticancer strategy, leading to a selective depletion of cancer-relevant proteins after turnover.
Ahmed K. ElHady +3 more
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Characterisation of the murine CLK1 dual-specificity kinase.
2009Murine Clk1 (also known as Sty) was identified as a dual-specificity kinase capable of phosphorylating serine, threonine and tyrosine residues when expressed in bacteria. Expression of Clk1 is deveolpmentally regulated at the level of RNA expression. Embryonic cells express two mRNAs of similar size, whereas differentiated cells express two additional ...
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An overview of cdc2‐like kinase 1 (Clk1) inhibitors and their therapeutic indications
Medicinal Research Reviews, 2023Ahmed K Elhady +2 more
exaly