Screening for small molecule inhibitors of B. burgdorferi HtrA

在本报告所述期间，合作团队开始在重组BbHtrA蛋白期间进行初步检测开发，并正在用红移荧光团标记的酪蛋白衍生物完成酶表征。使用BbHtrA和酪蛋白底物进行的验证筛选已证明了试验的耐用性，可进行更大规模的筛选。酶特异性的进一步表征正在使用FRET肽筛选方法进行，以便向筛选抑制剂所需的表征FRET底物移动。

During the reporting period, the collaborative team began initial assay development during recombinant BbHtrA protein, and enzyme characterization is being completed with a casein derivative labeled with a red-shifted fluorophore. Validation screens with BbHtrA and the casein substrate have demonstrated assay robustness to enable larger-scale screening. Further characterization of enzyme specificity is being conducted using a FRET peptide screening approach in order to move towards a characterized FRET substrate necessary for screening for inhibitors.