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Updated: May 18, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
Discovery of potent inhibitors of receptor protein tyrosine phosphatase sigma through the structure-based virtual
Hwangseo Park1, Pham Ngoc Chien, Seong Eon Ryu
1Department of Bioscience and Biotechnology, Sejong University, Seoul, Republic of Korea. hspark@sejong.ac.kr
Abstract:
Receptor protein tyrosine phosphatase sigma (PTPσ) has proved to be a promising target for the development of therapeutics for the treatment of neurological diseases. Here, we report the first example for a successful application of the structure-based virtual screening to identify the novel small-molecule inhibitors of PTPσ. These inhibitors revealed high potencies with the associated IC(50) values ranging from 0.1 to 1.3 μM and were also screened for having desirable physicochemical properties as a drug candidate. Therefore, they deserve consideration for further development by structure-activity relationship studies to develop therapeutics for neurological diseases. Structural features relevant to the stabilization of the newly identified inhibitors in the active site of PTPσ are discussed in detail.
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