当前位置: X-MOL 学术Bioorg. Med. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis and biological evaluation of peptide-derived TSLP inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2017-09-07 , DOI: 10.1016/j.bmcl.2017.09.010
Seonghu Park , Yeeun Park , Sang-Hyun Son , Kiho Lee , Yong Woo Jung , Ki Yong Lee , Young Ho Jeon , Youngjoo Byun

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 (68) exhibited >50% inhibition at concentration of 0.3 mM. They can be used as hit compounds for developing peptide-based TSLP inhibitors.



中文翻译:

肽源TSLP抑制剂的合成及生物学评价

胸腺基质淋巴细胞生成素(TSLP)是II型细胞因子,与人类大多数炎症性变态反应有关。它主要由上皮细胞产生,通过激活T型辅助细胞2型(T H 2)途径在慢性炎症性疾病的发展中起重要作用。在这项研究中,基于TSLP和TSLP受体之间界面的氨基酸序列,通过固相肽合成制备了总共16种肽。通过ELISA测定其TSLP抑制活性。其中,三种肽(6 - 8)显示出> 50%的抑制为0.3mM的浓度。它们可用作开发基于肽的TSLP抑制剂的热门化合物。

更新日期:2017-09-07
down
wechat
bug