Ser/Thr Kinase Inhibitor Libra

The Design, Annotation, and Application of a Kinase-Targeted Library

We present here a workflow for designing a kinase-targeted library (KTL) with the goal of capturing known kinase inhibitor chemical space. We validated our design retrospectively using recent, high-throughput screening data

含多个磷酸化位点的多肽的合成

phosphorylation）和单体法（Building block approach），如Figure 2所示。前者是在多肽序列合成结束后再在固相载体上对丝氨酸、苏氨酸或酪氨酸的侧链羟基进行磷酸化，可以在同一次合成中同时得到带有和不带有磷酸化位点的多肽；而后者则将适当保护的磷酸化氨基酸直接引入到多肽序列中，操作较前者更为简单，现已成为磷酸化多肽合成的首选策略。 在采用单体法构建磷酸化多肽时，目前广泛采用的原料为侧链单苄基保护的氨基酸：Fmoc-AA(PO(OBzl)OH)-OH (AA = Ser, Thr

High-Throughput Automated Confocal Microscopy Imaging Screen of a Kinase-Focused Library to Identify p38 Mitogen-Activated Protein Kinase Inhibitors U

generation through preclinical candidate selection. In this chapter we describe the development, validation, and implementation of an HCS assay to screen compounds from a kinase-focused small-molecule library to identify inhibitors of the p38 pathway using