Identification of peptide substrate and small molecule inhibitors of testis-specific serine/threonine kinase1 (TSSK1) by the developed assays.
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Zhang L, Yan Y, Liu Z, Abliz Z, Liu G
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.
- PubMed ID
- 19530700 [ View in PubMed]
- 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.