Results 41 to 50 of about 2,078,396 (299)
FEBS Open Bio, 2018 Many clinically approved protein kinase inhibitors stabilize an inactive conformation of their kinase target. Such inhibitors are generally highly selective compared to active conformation inhibitors, and consequently, general methods to identify ...
Yoshiji Hantani +8 more
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Folia Biologica, 2006 Since protein kinases have been found to be implicated in many diseases, first of all malignancies, they are considered as promising therapeutic targets. Many protein kinase inhibitors have been designed by now. These molecules have a low molecular weight and most of them bind to protein kinases competing with ATP for the ATP-binding site. Some protein
I, Shchemelinin, L, Sefc, E, Necas
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Targeting mTOR for cancer therapy
Journal of Hematology & Oncology, 2019 Mechanistic target of rapamycin (mTOR) is a protein kinase regulating cell growth, survival, metabolism, and immunity. mTOR is usually assembled into several complexes such as mTOR complex 1/2 (mTORC1/2).
Hui Hua +5 more
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Targeting the trypanosome kinetochore with CLK1 protein kinase inhibitors
bioRxiv, 2019 The kinetochore is a macromolecular structure that assembles on the centromeres of chromosomes and provides the major attachment point for spindle microtubules during mitosis.
Manuel Saldivia +21 more
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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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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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DeepPurpose-based drug discovery in chondrosarcoma
Chinese Journal of Plastic and Reconstructive Surgery, 2022 Background: Chondrosarcoma (CS) is the second most common primary bone tumor, accounting for approximately 30% of all malignant bone tumors. Unfortunately, the efficacy of currently available drug therapies is limited.
Jianrui Li +3 more
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Mediators of Inflammation, 2000 The effect of various phospholipase A2 and protein kinase inhibitors on the arachidonic acid liberation in bovine platelets induced by the protein kinase activator 12-O-tetradecanoylphorbol–13-acetate (TPA) was studied.
M. Lehr, K. Griessbach
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Kinase-targeted cancer therapies: progress, challenges and future directions
Molecular Cancer, 2018 The human genome encodes 538 protein kinases that transfer a γ-phosphate group from ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with human cancer initiation and progression.
Khushwant S. Bhullar +6 more
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Properties of FDA-approved small molecule protein kinase inhibitors: a 2025 update.
Pharmacological ResearchBecause of the deregulation of protein kinase action in many inflammatory diseases and cancer, the protein kinase family has become one of the most significant drug targets in the 21st century.
Robert Roskoski
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