Identification of peptide substrate and small molecule inhibitors of testis-specific serine/threonine kinase1 (TSSK1) by the developed assays.
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.
Zhang
Leilei
L
Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
Yan
Yu
Y
Liu
Zijie
Z
Abliz
Zeper
Z
Liu
Gang
G
D000595:Amino Acid Sequence; D000818:Animals; D001713:Biphenyl Compounds / Q000737:chemistry; D002417:Cattle; D002853:Chromatography, Liquid; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D008163:Luminescent Measurements; D013058:Mass Spectrometry; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D011810:Quinoxalines / Q000737:chemistry / Q000494:pharmacology; D015203:Reproducibility of Results; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology
D001713:Biphenyl Compounds; D010455:Peptides; D047428:Protein Kinase Inhibitors; D011810:Quinoxalines; D054852:Small Molecule Libraries; D017346:Protein Serine-Threonine Kinases