Advances in the research and application of neurokinin-1 receptor antagonists
作者机构：College of Life Sciences and MedicineZhejiang Sci-Tech UniversityHangzhou310018China
出 版 物：《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》 (浙江大学学报（英文版）B辑（生物医学与生物技术）)
年 卷 期：2024年第25卷第2期
页 面：91-105页
核心收录：
学科分类：0831[工学-生物医学工程（可授工学、理学、医学学位）] 0710[理学-生物学] 1001[医学-基础医学(可授医学、理学学位)] 08[工学] 0836[工学-生物工程]
基 金：This work was supported by the Zhejiang Provincial Natural Science Foundation of China(No.LD22H310004) the“Pioneer”and“Leading Goose”R&D Program of Zhejiang(No.2022C03005),China.
主 题：Neurokinin-1 receptor(NK-1R)antagonist Pathophysiological disorder Tumor target Bioavailability Nanoencapsulation Synergistic therapy
摘 要：Recently,the substance P(SP)/neurokinin-1 receptor(NK-1R)system has been found to be involved in various human pathophysiological disorders including the symptoms of coronavirus disease 2019(COVID-19).Besides,studies in the oncological field have demonstrated an intricate correlation between the upregulation of NK-1R and the activation of SP/NK-1R system with the progression of multiple carcinoma types and poor clinical prognosis.These findings indicate that the modulation of SP/NK-1R system with NK-1R antagonists can be a potential broad-spectrum antitumor strategy.This review updates the latest potential and applications of NK-1R antagonists in the treatment of human diseases and cancers,as well as the underlying mechanisms.Furthermore,the strategies to improve the bioavailability and efficacy of NK-1R antagonist drugs are summarized,such as solid dispersion systems,nanonization,and nanoencapsulation.As a radiopharmaceutical therapeutic,the NK-1R antagonist aprepitant was originally developed as radioligand receptor to target NK-1R-overexpressing tumors.However,combining NK-1R antagonists with other drugs can produce a synergistic effect,thereby enhancing the therapeutic effect,alleviating the symptoms,and improving patients’quality of life in several diseases and cancers.
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