Dissecting the novel abilities of aripiprazole: The generation of anti-colorectal cancer effects by targeting Gαq via HTR2B
作者机构：College of Pharmaceutical SciencesSouthwest UniversityChongqing 400715China NMPA Key Laboratory for Quality Monitoring of Narcotic Drugs and Psychotropic SubstancesChongqing Institute for Food and Drug ControlChongqing 401121China
出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)
年 卷 期：2023年第13卷第8期
页 面：3400-3413页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学]
基 金：supported by Chongqing basic research and frontier exploration project(cstc2022ycjh-bgzxm0119 China)
主 题：Aripiprazole 5-Hydroxytryptamine receptor 5-Hydroxytryptamine 2B receptor G protein subunit alpha q Colorectal cancer Phosphoinositide 3-kinase/theserine threoninekinaseAKT Extracellularregulated protein kinases
摘 要：Colorectal cancer(CRC)is a type of malignant tumor that seriously threatens human health and life,and its treatment has always been a difficulty and hotspot in ***,this study for the first time reports that antipsychotic aripiprazole(Ari)against the proliferation of CRC cells both in vitro and in vivo,but with less damage in normal colon ***,the results showed that5-hydroxytryptamine 2B receptor(HTR2B)and its coupling protein G protein subunit alpha q(Gaq)were highly distributed in CRC *** had a strong affinity with HTR2B and inhibited HTR2B downstream *** of HTR2B signaling suppressed the growth of CRC cells,but HTR2B was not found to have independent anticancer ***,the binding of Gaq to HTR2B was decreased after Ari *** of Gaq not only restricted CRC cell growth,but also directly affected the antiCRC efficacy of ***,an interaction between Ari and Gaq was found in that the mutation at amino acid 190 of Gaq reduced the efficacy of ***,these results confirm that Gaq coupled to HTR2B was a potential target of Ari in mediating CRC ***,this study provides a novel effective strategy for CRC therapy and favorable evidence for promoting Ari as an anticancer agent.
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