This blog supports the CH795 Special Topics in Chemistry courses taught by Dr. Gavin Williams and Dr. Alex Deiters at North Carolina State University. Please include an illustrative figure when you post a blog entry.
Friday, November 18, 2011
A Small Molecule Mimicking a Phosphatidylinositol (4,5)-Bisphosphate Binding Pleckstrin Homology Domain
Inositol phospholipids are important precursors for signaling molecules involved in a variety of cellular processes. Phosphatidylinositol (4,5)-bisphosphate (PI(4,5)P2) is the most studied of these lipids. Conditional depletion of cellular PI(4,5)P2 has already been accomplished using expression of a Pleckstrin Homology Domain, which binds specifically to these molecules, and will sequester them when overexpressed. This paper demonstrates a chemical alternative to achieve this conditional knock-down of PI(4,5)P2. Their final product is a bis-urea, bis-boronic acid molecule, taking advantage of already-known phosphate - interacting properties of some of these molecules.
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