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The Discovery of Novel Protein Tyrosine Phosphatase ε Inhibitors Using a High‐throughput Screening Approach
Author(s) -
Yun HyeYeoung,
Ku Bonsu,
Lee Hye Seon,
Shin HoChul,
Park JunBeom,
Kim Chang Hyen,
Kim Seung Jun
Publication year - 2017
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.11044
Subject(s) - protein tyrosine phosphatase , drug discovery , high throughput screening , chemistry , phosphatase , signal transduction , computational biology , biochemistry , enzyme , biology
Protein tyrosine phosphatase epsilon (PTPε) is important for signal transduction in osteoclasts, and is considered to be an attractive drug target for the treatment of osteoporosis. We identified 11 potent PTPε inhibitors based on three chemical scaffolds through the high‐throughput screening of a chemical library. As these compounds are structurally diverse with high bioavailability, they warrant further investigation in the near future. The discovery of these inhibitors and the relationship between their structure and inhibitory activity toward PTPε is discussed in detail.