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Protein kinase inhibitors for acute leukemia [PDF]
Biomarker Research, 2018 Conventional treatments for acute leukemia include chemotherapy, radiation therapy, and intensive combined treatments (including bone marrow transplant or stem cell transplants). Novel treatment approaches are in active development. Recently, protein kinase inhibitors are on clinical trials and offer hope as new drugs for acute leukemia treatment. This
Qing Xie +3 more
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The Kinase Specificity of Protein Kinase Inhibitor Peptide [PDF]
Frontiers in Pharmacology, 2021 G-protein-coupled-receptor (GPCR) signaling is exquisitely controlled to achieve spatial and temporal specificity. The endogenous protein kinase inhibitor peptide (PKI) confines the spatial and temporal spread of the activity of protein kinase A (PKA), which integrates inputs from three major types of GPCRs.
Yao Chen, Yao Chen, Bernardo L. Sabatini
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Bivalent inhibitors of protein kinases [PDF]
Critical Reviews in Biochemistry and Molecular Biology, 2014 Protein kinases are key players in a large number of cellular signaling pathways. Dysregulated kinase activity has been implicated in a number of diseases, and members of this enzyme family are of therapeutic interest. However, due to the fact that most inhibitors interact with the highly conserved ATP-binding sites of kinases, it is a significant ...
Carrie M. Gower +2 more
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Pharmacology and pharmacovigilance of protein kinase inhibitors
Therapies, 2022 Protein kinase inhibitors experienced their advent in the 2000s. Their market introduction made it possible to constitute a class of targeted therapies administered orally. This name was chosen to mark a break with conventional chemotherapy drugs, but it is important to stress that these are multi-target drugs with complex affinity profiles.
Khouri, Charles +4 more
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Deactivatable Bisubstrate Inhibitors of Protein Kinases
Molecules, 2022 Bivalent ligands, including bisubstrate inhibitors, are conjugates of pharmacophores, which simultaneously target two binding sites of the biomolecule. Such structures offer attainable means for the development of compounds whose ability to bind to the biological target could be modulated by an external trigger.
Tanel Sõrmus +4 more
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Protein Kinase CK2 Is an Inhibitor of the Neuronal Cdk5 Kinase [PDF]
Journal of Biological Chemistry, 2004 The complex of Cdk5 and its neuronal activator p35 is a proline-directed Ser/Thr kinase that plays an important role in various neuronal functions. Deregulation of the Cdk5 enzymatic activity was found to associate with a number of neurodegenerative diseases.
Zhibo Hou +4 more
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Inhibitors of protein kinase C [PDF]
Chinese Science Bulletin, 2005 Protein kinase catalyzes the transfer of the γ-phosphoryl group from ATP to the hydroxyl groups of protein side chains, which plays critical roles in signal transduction pathways by transmitting extracellular signals across the plasma membrane and nuclear membrane to the destination sites in the cytoplasm and the nucleus.
Jian Cao +6 more
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Protein Kinase Inhibitors as a Therapeutic Modality [PDF]
Accounts of Chemical Research, 2003 AbstractFor Abstract see ChemInform Abstract in Full Text.
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Protein Kinase Inhibitors in Rheumatology
Journal of Autoimmune Diseases and Rheumatology, 2014 Protein kinases have multiple roles in cell biology, many of which are deeply involved in inflammation and immunity. There are currently many treatment options for patients with autoimmune disease, but none that is completely effective. Protein kinase inhibitors are becoming one of the most promising therapeutic groups, not only for the treatment of ...
Gloria Vásquez +1 more
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A protein kinase inhibitor as an antimycobacterial agent [PDF]
FEMS Microbiology Letters, 2001 The protein kinase inhibitor 1-(5-isoquinolinesulfonyl)-2-methylpiperazine (H7) was found to inhibit the growth of two different mycobacterial strains, the slow-growing Mycobacterium bovis Bacille Calmette Guerin (BCG) and the fast-growing saprophyte Mycobacterium smegmatis mc2 155, in a dose-dependent manner.
Yossef Av-Gay +2 more
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