Identification of Peptide Substrate and Small Molecule Inhibitors of Testis-Specific Serine/Threonine Kinase1 (TSSK1) By the Developed Assays.

J Med Chem. 2009 Jun 16; Zhang L, Yan Y, Liu Z, Abliz Z, Liu GIn this paper, a peptide substrate (Pep8) of TSSK1 is identified. Using Pep8 as a substrate, two homogeneous and efficient assays for TSSK1 inhibitors screening have been developed, including luminescent kinase assay and LC-MS-based high-throughput assay. Two classes of compounds were identified that are able to efficiently inhibit phosphorylation catalyzed by TSSK1.