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Xiangyu HONG


Caiyun FU


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Journal of Zhejiang University SCIENCE B

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Advances in the research and application of neurokinin-1 receptor antagonists

Author(s):  Xiangyu HONG, Junjie MA, Shanshan ZHENG, Guangyu ZHAO, Caiyun FU

Affiliation(s):  College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China

Corresponding email(s):  fucy03@zstu.edu.cn

Key Words:  Neurokinin-1 receptor (NK-1R) antagonist; Pathophysiological disorder; Tumor target; Bioavailability; Nanoencapsulation; Synergistic therapy

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Xiangyu HONG, Junjie MA, Shanshan ZHENG, Guangyu ZHAO, Caiyun FU. Advances in the research and application of neurokinin-1 receptor antagonists[J]. Journal of Zhejiang University Science B,in press.Frontiers of Information Technology & Electronic Engineering,in press.https://doi.org/10.1631/jzus.B2300455

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year="in press",
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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.




Darkslateblue:Affiliate; Royal Blue:Author; Turquoise:Article


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