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Here, Kenakin discusses how the efficacy of drugs that act at seven-transmembrane receptors is linked to the particular pharmacological assay used to observe the effects of the drug, and highlights how a return to whole–system assays is adding value to the drug discovery process.
The phosphoinositide 3-kinase (PI3K) signal transduction pathway is often inappropriately activated in human cancer and is crucial for cancer cell growth and survival. Liu and colleagues discuss key therapeutic targets in the PI3K pathway and agents that are currently in development, and consider the associated challenges and possible approaches to overcome them.
Immune tolerance might be therapeutically manipulated to restore normal immunity in allergic disease. This Review highlights current knowledge of immunomodulatory therapies for the manipulation of immune tolerance and discusses recent approaches to improve allergen-specific immunotherapy.
Cell surface carbohydrates and carbohydrate-binding proteins mediate many key recognition events. This article reviews current progress in the development of glycomimetics and the opportunities and challenges presented by this relatively untapped source of therapeutics.