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Identification of novel protein tyrosine phosphatase sigma inhibitors promoting neurite extension

Title
Identification of novel protein tyrosine phosphatase sigma inhibitors promoting neurite extension
Author
류성언
Keywords
Protein tyrosine phosphatase; PTP sigma; Receptor type PTP; Inhibitor; High-throughput screening
Issue Date
2016-01
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v. 26, NO 1, Page. 87-93
Abstract
Protein tyrosine phosphatase sigma (PTP sigma) is a potential target for the therapeutic treatment of neurological deficits associated with impaired neuronal recovery, as this protein is the receptor for chondroitin sulfate proteoglycan (CSPG), which is known to inhibit neuronal regeneration. Through a high-throughput screening approach started from 6400 representative compounds in the Korea Chemical Bank chemical library, we identified 11 novel PTP sigma inhibitors that can be classified as flavonoid derivatives or analogs, with IC50 values ranging from 0.5 to 17.5 mu M. Biochemical assays and structure-based active site-docking simulation indicate that our inhibitors are accommodated at the catalytic active site of PTP sigma as surrogates for the phosphotyrosine group. Treatments of these compounds on PC-12 neuronal cells led to the recovery of neurite extension attenuated by CSPG treatment, demonstrating their potential as antineurodegenerative agents. (C) 2015 Elsevier Ltd. All rights reserved.
URI
http://www.sciencedirect.com/science/article/pii/S0960894X15302341?via%3Dihubhttp://hdl.handle.net/20.500.11754/30528
ISSN
0960-894X; 1464-3405
DOI
10.1016/j.bmcl.2015.11.026
Appears in Collections:
COLLEGE OF ENGINEERING[S](공과대학) > BIOENGINEERING(생명공학과) > Articles
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