Minting a new class of Polo-like-kinase inhibitors
نویسندگان
چکیده
منابع مشابه
Linear Regression QSAR Models for Polo-Like Kinase-1 Inhibitors
A structurally diverse dataset of 530 polo-like kinase-1 (PLK1) inhibitors is compiled from the ChEMBL database and studied by means of a conformation-independent quantitative structure-activity relationship (QSAR) approach. A large number (26,761) of molecular descriptors are explored with the main intention of capturing the most relevant structural characteristics affecting the bioactivity. T...
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Metastatic triple negative breast cancer (TNBC) is an incurable disease with limited therapeutic options, and no targeted therapies available. Triple negative tumors and the basal-like genomic subtype, are both characterized by a high proliferation rate and an increase in cell division. In this context, protein kinases involved in the mitotic formation have a relevant role in this tumor subtype...
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The Polo-like protein kinases (Plks) are a conserved family of enzymes that play a variety of roles in the passage of cells through M phase (for reviews see Glover et al., 1998; Nigg, 1998). Named after the Drosophila polo gene originally identified through a recessive maternal effect lethal mutation, conserved Plk homologues have been identified in yeast, Xenopus, C. elegans and mammals. The i...
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Polo-like kinase 1 (Plk1) plays several roles in cell division and it is a recognized cancer drug target. Plk1 levels are elevated in cancer and several types of cancer cells are hypersensitive to Plk1 inhibition. Small molecule inhibitors of the kinase domain (KD) of Plk1 have been developed. Their selectivity is limited, which likely contributes to their toxicity. Polo-like kinases are charac...
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The outlook for patients with rheumatoid arthritis has improved significantly over the last three decades with the use of disease-modifying antirheumatic drugs. However, despite the use of methotrexate, cytokine inhibitors, and molecules targeting T and B cells, a percentage of patients do not respond or lose their response over time. The autoimmune process in rheumatoid arthritis depends on ac...
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ژورنال
عنوان ژورنال: Cancer Biology & Therapy
سال: 2009
ISSN: 1538-4047,1555-8576
DOI: 10.4161/cbt.8.24.10389