Application of PI3K inhibitors in breast cancer treatment: a clinical trial landscape analysis based on clinical trial databases and registries. [PDF]
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Natural products as kinase inhibitors in lung cancer: molecular mechanisms, therapeutic potential, and clinical trials. [PDF]
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Functionalized nanomedicines for co-targeting of multiple pathways to efficiently treat thyroid cancer: prospects and challenges. [PDF]
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Itraconazole in the Treatment of Aberrantly Active Hedgehog and/or PI3K Recurrent Ovarian Cancer. [PDF]
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Translational insights into miR-126 and miR-423: biomarkers and therapeutic targets in cancer, cardiovascular, metabolic and kidney diseases. [PDF]
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Isoform-specific phosphoinositide 3-kinase inhibitors as therapeutic agents
Current Opinion in Pharmacology, 2003The phosphoinositide 3-kinase (PI3K) family of enzymes consists of several closely related isoforms that are thought to have distinct biological roles. Until now, researchers have been frustrated by poor selectivity of the available pharmacological inhibitors, which are unable to distinguish adequately the activities of different PI3K isoforms ...
Stephen G Ward, Peter Finan
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Of the four class I phosphoinositide 3-kinase (PI3K) isoforms, PI3Kα has justly received the most attention for its potential in cancer therapy. Herein we report our successful approaches to achieve PI3Kα vs PI3Kβ selectivity for two chemical series.
Timothy P Heffron +2 more
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Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold.
Bioorganic & Medicinal Chemistry, 2004Phosphoinositide 3-kinases (PI3-Ks) are an ubiquitous class of signaling enzymes that regulate diverse cellular processes including growth, differentiation, and motility. Physiological roles of PI3-Ks have traditionally been assigned using two pharmacological inhibitors, LY294002 and wortmannin. Although these compounds are broadly specific for the PI3-
Zachary A. Knight +7 more
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Therapeutic potential of phosphoinositide 3-kinase inhibitors
Expert Opinion on Therapeutic Patents, 2004Originally discovered as oncogene-associated lipid kinases more than 15 years ago, the family of phosphoinositide 3-kinase (PI 3-K) enzymes has recently emerged as an important therapeutic target in human pathophysiology. After more than a decade with only a few inhibitors with low activity, poor isoform or kinase selectivity or unacceptable ...
B. Drees +3 more
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Development of first lead structures for phosphoinositide 3-kinase-C2γ inhibitors.
Journal of Medicinal Chemistry, 2015The importance of complete elucidation of the biological functions of phosphoinositide 3-kinases (PI3K) was realized years ago. They generate 3-phosphoinositides, which are known to function as important second messengers in many inter- and intracellular signaling pathways. However, the functional role of class II PI3Ks is still unclear.
A. Freitag +8 more
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