Results 161 to 170 of about 2,071 (187)
Discovery of unique mitotic mechanisms in Paradiplonema papillatum
Akiyoshi B, Faktorová D, Lukeš J.
europepmc +1 more source
Library-based Discovery of DYRK1A/CLK1 Inhibitors from Natural Product Extracts
Planta Medica, 2012 The dual specificity tyrosine-phosphorylation-regulated kinase DYRK1A possesses diverse roles in neuronal development and adult brain physiology, and increased activity has been linked to neurodegenerative diseases. Very few inhibitors of this kinase have been reported up to now.
Emilie Durieu +2 more
exaly +7 more sources
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European Journal of Medicinal Chemistry, 2023
Clk1 kinase is a key modulator of the pre-mRNA alternative splicing machinery which has been proposed as a promising target for treatment of various tumour types, Duchenne's muscular dystrophy and viral infections such as HIV-1 and influenza. Most reported Clk1 inhibitors showed significant co-inhibition of Clk2 and Clk4 in particular, which limits ...
Dalia S El-Gamil +2 more
exaly +3 more sources
Clk1 kinase is a key modulator of the pre-mRNA alternative splicing machinery which has been proposed as a promising target for treatment of various tumour types, Duchenne's muscular dystrophy and viral infections such as HIV-1 and influenza. Most reported Clk1 inhibitors showed significant co-inhibition of Clk2 and Clk4 in particular, which limits ...
Dalia S El-Gamil +2 more
exaly +3 more sources
Clk1‐regulated aerobic glycolysis is involved in glioma chemoresistance [PDF]
Journal of Neurochemistry, 2017 AbstractChemoresistance remains a major challenge for the treatment of glioma. In this study, we investigated the role of Clock 1 (Clk1), which encodes an enzyme that is necessary for ubiquinone biosynthesis in glioma chemoresistance in vitro. The results showed that Clk1 was highly expressed in GL261 mouse glioma cells which were most sensitive to 1 ...
Wenbin Zhang +2 more
exaly +3 more sources
Dysregulation of iron homeostasis and methamphetamine reward behaviors in Clk1-deficient mice
Acta Pharmacologica Sinica, 2021Chronic administration of methamphetamine (METH) leads to physical and psychological dependence. It is generally accepted that METH exerts rewarding effects via competitive inhibition of the dopamine transporter (DAT), but the molecular mechanism of METH addiction remains largely unknown.
John L Waddington +2 more
exaly +3 more sources
Protein Expression and Purification, 2020
Cdc-like kinase 1 (CLK1) is a dual-specificity kinase capable of autophosphorylation on tyrosine residues and Ser/Thr phosphorylation of its substrates. CLK1 belongs to the CLK kinase family that regulates alternative splicing through phosphorylation of serine-arginine rich (SR) proteins. Recent studies have demonstrated that CLK1 has an important role
Yael Eisenberg-Domovich +2 more
exaly +4 more sources
Cdc-like kinase 1 (CLK1) is a dual-specificity kinase capable of autophosphorylation on tyrosine residues and Ser/Thr phosphorylation of its substrates. CLK1 belongs to the CLK kinase family that regulates alternative splicing through phosphorylation of serine-arginine rich (SR) proteins. Recent studies have demonstrated that CLK1 has an important role
Yael Eisenberg-Domovich +2 more
exaly +4 more sources
An overview of cdc2‐like kinase 1 (Clk1) inhibitors and their therapeutic indications
Medicinal Research Reviews, 2022AbstractOver the past decade, Clk1 has been identified as a promising target for the treatment of various diseases, in which deregulated alternative splicing plays a role. First small molecules targeting Clk1 are in clinical trials for the treatment of solid cancer, where variants of oncogenic proteins derived from alternative splicing promote tumor ...
Ahmed K. ElHady +4 more
openaire +2 more sources
Biochemical characterization and localization of the dual specificity kinase CLK1
Journal of Cell Science, 2000ABSTRACT CLK1 was one of the first identified dual specificity kinases and is the founding member of the ‘LAMMER’ family of kinases. We have established the substrate site specificity of CLK1. We report here that truncation of the N terminus of CLK1 resulted in a dramatic increase in CLK1 enzymatic activity, indicating that the N ...
Harry J Menegay +2 more
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Discovery of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors
Bioorganic and Medicinal Chemistry Letters, 2021Inhibition of cdc2-like kinase1 (CLK1) could efficiently induce autophagy and it has been thought as a potential target for treatment of autophagy-related diseases. Herein we report the discovery of a series of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors.
Yun Zhang, Anjie Xia, Guifeng Lin
exaly +3 more sources
Release of SR Proteins from CLK1 by SRPK1: A Symbiotic Kinase System for Phosphorylation Control of Pre-mRNA Splicing [PDF]
Molecular Cell, 2016 Phosphorylation has been generally thought to activate the SR family of splicing factors for efficient splice-site recognition, but this idea is incompatible with an early observation that overexpression of an SR protein kinase, such as the CDC2-like ...
Brandon E Aubol +2 more
exaly +2 more sources