Nek2, a Serine/Threonine kinase present at the centrosome of the cell, is essential during mitosis and is greatly over-expressed in many forms of cancer. Nevertheless several of its biological functions remain unknown due to the lack of small molecule substrates and biosensors, which can serve in assaying its intracellular activity. C-Nap1, a known in vivo protein substrate of Nek2, has its phosphorylation sites identified by mass spectrometry, an information utilized to synthesize small peptide substrates of Nek2 and assess their catalytic efficiency via Michaelis-Menten kinetic parameters (high kcat and low Km values). In this project, FMOC-based solid phase peptide synthesis procedure is employed for the development of two potential peptide substrates of Nek2 (NAP-3 and NAP-4) which are purified using Reverse Phase-HPLC, and characterized by ESI-MS. The knowledge gained from these studies could be utilized in the development of Nek2 biosensors and small molecule inhibitors.

Synthesis and characterization of efficient Nek2 substrates employing solid phase synthesis procedures

244th National Meeting (2012)

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