Meclizine, a piperazine-derivative antihistamine, binds to dimerized translationally controlled tumor protein and attenuates allergic reactions in a mouse model

Eun Hwa Jang, Hae Duck Bae, Yejin Jeon, Dong Hae Shin, Soosung Kang, Kyunglim Lee

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

Translationally controlled tumor protein (TCTP), a highly conserved protein present in most eukaryotes, is involved in numerous biological processes. Only the dimeric form of TCTP (dTCTP) formed during inflammatory conditions exhibits cytokine-like activity. Therefore, dTCTP is considered as a therapeutic target for allergic diseases. Because monomeric TCTP (mTCTP) and dTCTP share a high topological similarity, we hypothesized that small molecules interacting with mTCTP would also bind to dTCTP and interfere with dTCTP-based cellular processes. In this study, nine compounds listed in the literature as interacting with mTCTP were investigated for their ability to suppress the activity of extracellular dTCTP in bronchial epithelial cells. It was found that one of the nine, meclizine, a piperazine-derivative antihistamine, significantly reduced IL-8 release and suppressed the NF-κB pathway. The direct interaction of meclizine with dTCTP was confirmed by surface plasmon resonance (SPR). Also, we found that meclizine can attenuate ovalbumin (OVA)-induced airway inflammation in mice. Therefore, meclizine might be a potential anti-allergic drug as an inhibitor for dTCTP.

Original languageEnglish
Article number114072
JournalBiomedicine and Pharmacotherapy
Volume157
DOIs
StatePublished - Jan 2023

Bibliographical note

Publisher Copyright:
© 2022

Keywords

  • Airway inflammation
  • Antihistamine
  • HRF
  • Meclizine
  • TCTP

Fingerprint

Dive into the research topics of 'Meclizine, a piperazine-derivative antihistamine, binds to dimerized translationally controlled tumor protein and attenuates allergic reactions in a mouse model'. Together they form a unique fingerprint.

Cite this