Publications by authors named "J W Kozarich"
The founding of the journal by the American Chemical Society 60 years ago was a highlight of the Society's growing commitment to chemically driven biochemistry. It was a commitment that was nearly an additional 60 years in the making. In that time, biological chemistry was becoming more molecularly focused.
View Article and Find Full Text PDFExpression of human asparagine synthetase (ASNS) promotes metastatic progression and tumor cell invasiveness in colorectal and breast cancer, presumably by altering cellular levels of L-asparagine. Human ASNS is therefore emerging as a drug target for cancer therapy. Here we show that a slow-onset, tight binding inhibitor, which exhibits nanomolar affinity for human ASNS in vitro, exhibits excellent selectivity at 10 μM concentration in HCT-116 cell lysates with almost no off-target binding.
View Article and Find Full Text PDFArticle Synopsis
- Acyl phosphates, like ATPAc, are useful for studying how certain nucleotides bind to proteins by modifying specific lysine residues, which can happen even in proteins without previously identified binding sites.
- The study shows that ATPAc specifically acylates the lysine at position 133 (K133) of procaspase-6 in Jurkat cells, influenced by interactions at the protein's dimer interface involving a conserved tyrosine residue (Y198).
- A mutation (Y198A) that alters this interaction prevents acylation at K133 but does not affect the activity of the active form of caspase-6, suggesting that ATP could play a key role as an endogenous ligand at this previously un