LIGAND BASED PHARMACOPHORIC DISCOVERY OF NEW CLK1 INHIBITORS
Indian Journal of Chemistry22-37CLK1 has been recognized as an optimistic target against an array of diseases, including cancer due to their pre-mRNA splicing function. In this study, ligand-based pharmacophore approach has been employed to identify new CLK1 inhibitors from ...
Sule, Swapnil Anil +5 more
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Chemical genetics reveals Leishmania KKT2 and CRK9 kinase activity is required for cell cycle progression. [PDF]
PLoS PathogensProtein kinases are key regulators of the eukaryotic cell cycle and have consequently emerged as attractive targets for drug development. Their well-defined active sites make them particularly amenable to inhibition by small molecules, underscoring their
Juliana B T Carnielli +8 more
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Discovery of unique mitotic mechanisms in Paradiplonema papillatum [PDF]
Open BiologyDiplonemids are highly diverse and abundant marine plankton with significant ecological importance. However, little is known about their biology, even in the model diplonemid Paradiplonema papillatum whose genome sequence is available.
Bungo Akiyoshi +2 more
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Targeting the cGAS‐STING Pathway Inhibits Peripheral T‐cell Lymphoma Progression and Enhances the Chemotherapeutic Efficacy [PDF]
Advanced SciencePeripheral T‐cell lymphoma (PTCL) is a highly heterogeneous group of mature T‐cell malignancies. The efficacy of current first‐line treatment is dismal, and novel agents are urgently needed to improve patient outcomes.
Xueying Lu +14 more
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Crystallography Across Temperature Extremes: Insights into the Conformational Landscapes of Human Kinases [PDF]
Structural DynamicsProtein kinases are a large family of enzymes that regulate diverse cellular processes by transferring phosphate groups from ATP to their protein substrates. The enzymatic kinase domain (KD) represents a conserved fold, and KD phosphorylation, as well as
Michael C Thompson
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Targeting the trypanosome kinetochore with CLK1 protein kinase inhibitors [PDF]
Nature Microbiology, 2020 The kinetochore is a macromolecular structure that assembles on the centromeres of chromosomes and provides the major attachment point for spindle microtubules during mitosis. In Trypanosoma brucei, the proteins that make up the kinetochore are highly divergent; the inner kinetochore comprises at least 20 distinct and essential proteins (KKT1-20) that ...
Manuel Saldivia +22 more
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Targeting the splice factor kinase CLK1 in prostate cancer cells
Prostate cancer is the most rampant diagnosed cancer and the second leading cause of cancer related death in men between middle age and old age. There is a need to identify the molecular genetic processes that underpin prostate cancer and to search for new treatments.
Uzor, Simon Ogbonnaya
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Clk/STY (cdc2-like kinase 1) and Akt regulate alternative splicing and adipogenesis in 3T3-L1 pre-adipocytes. [PDF]
PLoS ONE, 2013 The development of adipocytes from their progenitor cells requires the action of growth factors signaling to transcription factors to induce the expression of adipogenic proteins leading to the accumulation of lipid droplets, induction of glucose ...
Pengfei Li +6 more
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Frontiers in Cell and Developmental Biology, 2021 The abnormality of RNA-binding proteins (RBPs) is closely related to the tumorigenesis and development of esophageal squamous cell carcinoma (ESCC), and has been an area of interest for research recently.
Xiuping Yang +9 more
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Cloning of Human PRP4 Reveals Interaction with Clk1 [PDF]
Journal of Biological Chemistry, 2001 Prp4 is a protein kinase of Schizosaccharomyces pombe identified through its role in pre-mRNA splicing, and belongs to a kinase family including mammalian serine/arginine-rich protein-specific kinases and Clks, whose substrates are serine/arginine-rich proteins.
T, Kojima +4 more
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