![]() Based on our results, we have identified specific, high affinity The compounds on cell growth in a yeast cell-based assay. Screening (HTS) format and validated the hits utilizing an orthogonal gel-based assay. We identifiedĬompounds that inhibited Erf2 auto-palmitoylation activity using a fluorescence-based, coupled assay in a high throughput Here, we present the analysis of one of the scaffold backbones, bis-cyclic piperazine. This approach to identify and characterize several scaffold backbones and R-groups that reduce or eliminate the activity ofĮrf2 in vitro. Molecular scaffolds that are systematically arranged into positional scanning and scaffold ranking formats. The Torrey Pines Institute for Molecular Studies consists of more than 30 million compounds designed around 68 Erf2 is the Saccharomyces cerevisiae PAT responsible forĬatalyzing the palmitoylation of Ras2, an ortholog of the human Ras oncogene proteins. ![]() Screening approach to identify inhibitors of Erf2 activity. The need for screening campaigns to identify new specific, high affinity modulators. ![]() However, current chemical modulators of zDHHC PAT enzymes lack specificity and affinity, underscoring Neurological disorders, implying these enzymes and substrates are valid targets for pharmaceutical Dysregulation of the enzymes which catalyzed the palmitoylĪddition and/or the substrates of these enzymes have been linked to cancer, cardiovascular, and The addition of palmitoyl moieties to proteins regulates their membrane targeting, ![]()
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