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Therapeutic potential of interfering with apelin signalling

Journal

DRUG DISCOVERY TODAY
Volume 11, Issue 23-24, Pages 1100-1106

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2006.10.011

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The apelin receptor is a G protein-coupled receptor activated by several apelin fragments. Its tissue distribution suggests that apelin signalling is involved in a broad range of physiological functions. Endothelial cells, which express high levels of apelin receptors, respond to apelin through the phosphorylation of key intracellular effectors associated with cell proliferation and migration. In addition, apelin is a mitogen for endothelial cells and exhibits angiogenic properties in matrigel experiments. This review focuses on the therapeutic potential of apelin signalling, which is associated with pathologies that result from decreased vascularisation (ischemias) or neovascularisation (retinopathies and solid tumors).

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