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Bioorg Med Chem Lett. 2017 Oct 15;27(20):4710-4713. doi: 10.1016/j.bmcl.2017.09.010. Epub 2017 Sep 7.

Synthesis and biological evaluation of peptide-derived TSLP inhibitors.

Author information

1
College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea.
2
College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea. Electronic address: yhjeon@korea.ac.kr.
3
College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea. Electronic address: yjbyun1@korea.ac.kr.

Abstract

Thymic stromal lymphopoietin (TSLP) is a type II cytokine which is associated with most inflammatory allergic disorders in humans. It is produced mainly by epithelial cells with important role in the development of chronic inflammatory diseases by activating T-helper cell type-2 (TH2) pathways. In this study, a total of 16 peptides were prepared by solid phase peptide synthesis based on amino acid sequences of the interface between TSLP and TSLP receptor. Their TSLP inhibition activities were determined by ELISA assay. Among them, three peptides (6-8) exhibited >50% inhibition at concentration of 0.3mM. They can be used as hit compounds for developing peptide-based TSLP inhibitors.

KEYWORDS:

Allergic disease; Peptides; TSLP inhibitors; TSLP receptors

PMID:
28927768
DOI:
10.1016/j.bmcl.2017.09.010
[Indexed for MEDLINE]

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