Phosphatidylinositol phosphates (PtdInsPs or simply PIPs) undertake significant roles in biological processes within the cell.1They adopt roles as precursors for secondary messengers by interacting directly with proteins leading to a wide range of intracellular processes: vesicular trafficking, cytokinesis, cell apoptosis, cell proliferation, exocytosis and endocytosis. Deregulation of these processes is associated with disease � cancer, diabetes and Alzheimer's disease. Hence, PIP levels are important from both a biological and pharmaceutical view point. PI(3)P is one of these secondary messengers and is considered an active cellular component of endosomes; adopting a role in membrane trafficking, endocytosis and phagocytosis. Key effector proteins involved in these functions are recruited through specific PI(3)P binding domains such as FYVE, PX (Phagocyte oxidase homology) and PH (Pleckstrin like homology) domains.However, the roles of PI(3)P in cell signalling are not completely understood. We discuss the design and synthesis of PI(3)P derivatives for a range of biological experiments. In particular, discussion will focus on the ?-amino derivative (pictured); from its synthesis2 to its use in affinity pull-down experiments using extracts from a colorectal carcinoma cell line LIM1215. We present our LC/MS/MS proteomic analyses of the proteins bound to PI(3)P.31. Prestwich, G. D. Chem. Biol. 2004  , 11, 619;2. Conway, S. J.; Holmes, A. B., et. al. Org. Biomol. Chem. 2010  , 8, 66.3. Catimel, B., et.al. J. Proteomics, 2013  , 82, 35-51.

Synthesis and biological evaluation of PI(3)P analogs

246th National Meeting (2013)

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