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dc.contributor.author류성언-
dc.date.accessioned2017-11-07T04:43:33Z-
dc.date.available2017-11-07T04:43:33Z-
dc.date.issued2016-01-
dc.identifier.citationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v. 26, NO 1, Page. 87-93en_US
dc.identifier.issn0960-894X-
dc.identifier.issn1464-3405-
dc.identifier.urihttp://www.sciencedirect.com/science/article/pii/S0960894X15302341?via%3Dihub-
dc.identifier.urihttp://hdl.handle.net/20.500.11754/30528-
dc.description.abstractProtein 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.en_US
dc.description.sponsorshipThe authors appreciate the staff of the Korean Chemical Bank for providing the chemical library. This work was supported by the Bio & Medical Technology Development Programs of the National Research Foundation, funded by the Korean Government (20110030027 and 2014M3A9B6070243) and the Korea Research Institute of Bioscience and Biotechnology Research Initiative Program.en_US
dc.language.isoenen_US
dc.publisherPERGAMON-ELSEVIER SCIENCE LTDen_US
dc.subjectProtein tyrosine phosphataseen_US
dc.subjectPTP sigmaen_US
dc.subjectReceptor type PTPen_US
dc.subjectInhibitoren_US
dc.subjectHigh-throughput screeningen_US
dc.titleIdentification of novel protein tyrosine phosphatase sigma inhibitors promoting neurite extensionen_US
dc.typeArticleen_US
dc.relation.no1-
dc.relation.volume26-
dc.identifier.doi10.1016/j.bmcl.2015.11.026-
dc.relation.page87-93-
dc.relation.journalBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.contributor.googleauthorLee, Hye Seon-
dc.contributor.googleauthorKu, Bonsu-
dc.contributor.googleauthorPark, Tae Hyun-
dc.contributor.googleauthorPark, Hwangseo-
dc.contributor.googleauthorChoi, Joong-Kwon-
dc.contributor.googleauthorChang, Kyu-Tae-
dc.contributor.googleauthorKim, Cheol-Hee-
dc.contributor.googleauthorRyu, Seong Eon-
dc.contributor.googleauthorKim, Seung Jun-
dc.relation.code2016000607-
dc.sector.campusS-
dc.sector.daehakCOLLEGE OF ENGINEERING[S]-
dc.sector.departmentDEPARTMENT OF BIOENGINEERING-
dc.identifier.pidryuse-
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COLLEGE OF ENGINEERING[S](공과대학) > BIOENGINEERING(생명공학과) > Articles
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