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

Leilei Zhang; Yu Yan; Zijie Liu; Zeper Abliz; Gang Liu

doi:10.1021/jm9002846

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.

Authors

Leilei Zhang¹, Yu Yan, Zijie Liu, Zeper Abliz, Gang Liu

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amino Acid Sequence
Animals
Biphenyl Compounds / chemistry
Cattle
Chromatography, Liquid
Drug Discovery*
Drug Evaluation, Preclinical
Luminescent Measurements
Mass Spectrometry
Molecular Sequence Data
Peptides / chemistry
Peptides / metabolism*
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / pharmacology*
Protein Serine-Threonine Kinases / antagonists & inhibitors*
Protein Serine-Threonine Kinases / metabolism*
Quinoxalines / chemistry
Quinoxalines / pharmacology
Reproducibility of Results
Small Molecule Libraries / chemistry
Small Molecule Libraries / pharmacology

Substances

Biphenyl Compounds
Peptides
Protein Kinase Inhibitors
Quinoxalines
Small Molecule Libraries
Protein Serine-Threonine Kinases