Synthesis and biological evaluation of peptide-derived TSLP inhibitors

Seonghu Park; Yeeun Park; Sang Hyun Son; Kiho Lee; Yong Woo Jung; Ki Yong Lee; Young Ho Jeon; Youngjoo Byun

doi:10.1016/j.bmcl.2017.09.010

Synthesis and biological evaluation of peptide-derived TSLP inhibitors

Seonghu Park
, Yeeun Park
, Sang Hyun Son
, Kiho Lee
, Yong Woo Jung
, Ki Yong Lee
, Young Ho Jeon^*
, Youngjoo Byun

^*Corresponding author for this work

Korea University (SEJONG)

Research output: Contribution to journal › Article › peer-review

15 Citations (Scopus)

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 (T_H2) 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 0.3 mM. They can be used as hit compounds for developing peptide-based TSLP inhibitors.

Original language	English
Pages (from-to)	4710-4713
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	27
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2017.09.010
Publication status	Published - 2017

Bibliographical note

Publisher Copyright:
© 2017 Elsevier Ltd

Keywords

Allergic disease
Peptides
TSLP inhibitors
TSLP receptors

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2017.09.010

Cite this

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title = "Synthesis and biological evaluation of peptide-derived TSLP inhibitors",

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 0.3 mM. They can be used as hit compounds for developing peptide-based TSLP inhibitors.",

keywords = "Allergic disease, Peptides, TSLP inhibitors, TSLP receptors",

author = "Seonghu Park and Yeeun Park and Son, \{Sang Hyun\} and Kiho Lee and Jung, \{Yong Woo\} and Lee, \{Ki Yong\} and Jeon, \{Young Ho\} and Youngjoo Byun",

note = "Publisher Copyright: {\textcopyright} 2017 Elsevier Ltd",

year = "2017",

doi = "10.1016/j.bmcl.2017.09.010",

language = "English",

volume = "27",

pages = "4710--4713",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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}

TY - JOUR

T1 - Synthesis and biological evaluation of peptide-derived TSLP inhibitors

AU - Park, Seonghu

AU - Park, Yeeun

AU - Son, Sang Hyun

AU - Lee, Kiho

AU - Jung, Yong Woo

AU - Lee, Ki Yong

AU - Jeon, Young Ho

AU - Byun, Youngjoo

PY - 2017

Y1 - 2017

N2 - 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 0.3 mM. They can be used as hit compounds for developing peptide-based TSLP inhibitors.

AB - 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 0.3 mM. They can be used as hit compounds for developing peptide-based TSLP inhibitors.

KW - Allergic disease

KW - Peptides

KW - TSLP inhibitors

KW - TSLP receptors

UR - https://www.scopus.com/pages/publications/85029547109

U2 - 10.1016/j.bmcl.2017.09.010

DO - 10.1016/j.bmcl.2017.09.010

M3 - Article

C2 - 28927768

AN - SCOPUS:85029547109

SN - 0960-894X

VL - 27

SP - 4710

EP - 4713

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

Synthesis and biological evaluation of peptide-derived TSLP inhibitors

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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