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Title 

Identification of novel protein tyrosine phosphatase sigma inhibitors promoting neurite extension

Authors 

Hye Seon LeeBonsu KuT H ParkH ParkJ K ChoiKyu Tae ChangC H KimS E RyuSeung Jun Kim

Publisher 

Elsevier

Issue Date 

2016

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 26, no. 1, pp. 87-93

Keywords 

High-throughput screeningInhibitorProtein tyrosine phosphatasePTPrReceptor type PTP

Abstract 

Protein tyrosine phosphatase sigma (PTPσ) 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 PTPσ inhibitors that can be classified as flavonoid derivatives or analogs, with IC50 values ranging from 0.5 to 17.5 μM. Biochemical assays and structure-based active site-docking simulation indicate that our inhibitors are accommodated at the catalytic active site of PTPσ 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.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2015.11.026

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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