Protein kinases are a class of enzymes that transfer phosphate groups from ATP to specified substrates, resulting in structural and functional modifications to substrate activity.  Cell division, signaling, and metabolism are all affected by the phosphorylation of proteins via post-translational modification by protein kinases.  Within the past few decades, protein kinase research has emerged at the forefront of chemical biology as one of the primary areas of interest in drug development.  An estimated total of 500 protein kinases exist in the human kinome.  However, only a small fraction of these have been subjected to studies regarding biological function and therapeutic targeting.  The impetus to determine the functions of various kinases lies in the potential to modulate them and thus treat various ailments, particularly cancer.<br/>                 A common practice in determining the function and mechanism of a protein kinase is the synthesis and utilization of small-molecule chemical probes.  These inhibitors are targeted towards a specified protein and subsequently elucidate pathways in both healthy and diseased cells. From this verification, the probe can serve as a precursor to a therapeutic drug in combating the disease in question.   Our project focuses on the inhibition of kinase STK-16, an understudied serine-threonine kinase.  Our goal is to synthesize a library of small molecule chemical probes that are both potent and selective inhibitors of STK-16.  Previously conducted research has found that kinase STK-16 inhibition has resulted in increased cell binucleation and reduced total cell number. Considering the relationship between cell binucleation and cancer, it is suspected that STK-16 is associated in some way with cancer cells.  It is our hope that a potent inhibitor may possibly lead to a new chemotherapy agent.<br/>

Synthesis of 2-aminooxazole inhibitors targeting kinase STK-16

ACS Fall 2020 Virtual Meeting

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