Synthesis and biological evaluation of peptide-derived TSLP inhibitors.

Bioorg Med Chem Lett

College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea. Electronic address:

Published: October 2017

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 (T2) 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.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2017.09.010DOI Listing

Publication Analysis

Top Keywords

tslp inhibitors
8
tslp
6
synthesis biological
4
biological evaluation
4
evaluation peptide-derived
4
peptide-derived tslp
4
inhibitors thymic
4
thymic stromal
4
stromal lymphopoietin
4
lymphopoietin tslp
4

Similar Publications

Cannabichromene (CBC) is one of the main cannabinoids found in the cannabis plant, and although less well known than tetrahydrocannabinol (THC) and cannabidiol (CBD), it is gaining attention for its potential therapeutic benefits. To date, CBC's known mechanisms of action include anti-inflammatory, analgesic, antidepressant, antimicrobial, neuroprotective, and anti-acne effects through TRP channel activation and the inhibition of inflammatory pathways, suggesting that it may have therapeutic potential in the treatment of inflammatory skin diseases, such as atopic dermatitis (AD), but its exact mechanism of action remains unclear. Therefore, in this study, we investigated the effects of CBC on Th2 cytokines along with the Janus kinase (JAK)/signal transducer and activator of transcription (STAT) pathways involved in AD pathogenesis.

View Article and Find Full Text PDF
Article Synopsis
  • The incidence and mortality rates of cutaneous squamous cell carcinoma (cSCC) are increasing, highlighting the urgent need for better prevention methods.
  • Topical treatments like calcipotriol and 5-fluorouracil (5-FU) can eliminate actinic keratosis (AK) lesions, but their exact mechanisms weren't clear until recent research.
  • A study shows that type 2 immunity, specifically the interaction between thymic stromal lymphopoietin (TSLP) and Th2 cells, is crucial for eliminating premalignant cells and could be targeted for cSCC prevention.
View Article and Find Full Text PDF

New insights into the mechanisms of aspirin-exacerbated respiratory disease.

Curr Opin Allergy Clin Immunol

February 2025

Department of Medicine, the Division of Allergy and Clinical Immunology, Brigham and Women's Hospital, Harvard Medical School, Jeff and Penny Vinik Center for Translational Immunology Research, Boston, Massachusetts, USA.

Purpose Of Review: Aspirin-exacerbated respiratory disease (AERD), a syndrome characterized clinically by asthma, chronic rhinosinusitis with nasal polyposis, and respiratory reactions to aspirin and other cyclooxygenase-1 inhibitors, is an inflammatory condition of the respiratory tract that is often severe and challenging to treat. There have been several recent advances in our understanding of the underlying pathology of the disease. These have been paralleled by welcome advances in the availability of targeted treatment options for patients with AERD.

View Article and Find Full Text PDF

Type 2 cytokine-JAK1 signaling is involved in the development of dry skin-induced mechanical alloknesis.

J Dermatol Sci

October 2024

Juntendo Itch Research Center (JIRC), Institute for Environmental and Gender-Specific Medicine, Juntendo University Graduate School of Medicine, Urayasu, Japan; Department of Dermatology, Juntendo University Urayasu Hospital, Urayasu, Japan. Electronic address:

Background: Mechanical alloknesis (m-alloknesis) is itch hypersensitivity induced by normally innocuous stimuli. It is sometimes observed in dry skin based itch-related diseases such as atopic dermatitis (AD), and often triggers the vicious itch-scratch cycle. The acetone-ether and water (AEW) mouse model mimics dry skin-induced m-alloknesis, yet its underlying mechanism remains unclear.

View Article and Find Full Text PDF
Article Synopsis
  • Targeted therapies using biologics for atopic diseases, urticaria, and angioedema are advancing quickly, with several new antibodies developed, tested, and approved for clinical use, like omalizumab and dupilumab.
  • There is ongoing research into combining different biologics for enhanced treatment efficacy, expanding their applications to conditions like food allergies and eosinophilic esophagitis.
  • There are emerging concerns about unexpected side effects and hypersensitivity reactions associated with these therapies, raising important questions about their safety and mechanisms, particularly in specific patient groups like children.
View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!