Identification of peptide substrate and small molecule inhibitors of testis-specific serine/threonine kinase1 (TSSK1) by the developed assays

  • J Med Chem. 2009 Jul 23;52(14):4419-28. doi: 10.1021/jm9002846.
Leilei Zhang  1 ,  Yu Yan ,  Zijie Liu ,  Zeper Abliz ,  Gang Liu
Affiliations
  • 1. Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
PMID: 19530700 DOI: 10.1021/jm9002846
Abstract

In 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.