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Synthesis and biological evaluation of peptide-derived TSLP inhibitors.

Authors
  • Park, Seonghu1
  • Park, Yeeun1
  • Son, Sang-Hyun1
  • Lee, Kiho1
  • Jung, Yong Woo1
  • Lee, Ki Yong1
  • Jeon, Young Ho2
  • Byun, Youngjoo3
  • 1 College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea. , (North Korea)
  • 2 College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea. Electronic address: [email protected] , (North Korea)
  • 3 College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea. Electronic address: [email protected] , (North Korea)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Oct 15, 2017
Volume
27
Issue
20
Pages
4710–4713
Identifiers
DOI: 10.1016/j.bmcl.2017.09.010
PMID: 28927768
Source
Medline
Keywords
License
Unknown

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.

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