典型文献
The novel BRDT inhibitor NHWD870 shows potential as a male contraceptive in mice
文献摘要：
Small molecule inhibitors of the bromodomain and extraterminal domain(BET)family proteins have emerged as promising options not only for the treatment of multiple cancers but also for disturbing the process of sperm maturation with potential for use as viable contraceptive targets.In this study,we find that the BET family inhibitor NHWD870 and BRDT can bind well in vitro through bioinformatics software prediction and protein binding in-hibition experiments.NHWD870 can produce a good contraceptive effect through animal experiments in vivo,and the fertility can be restored to normal after drug withdrawal.Transcriptomics and proteomics results suggest that NHWD870 affects pathways related to spermatogenesis and maturation,further contributing to the male infertility phenotype.Our results show that NHWD870 can induce a complete and reversible contraceptive effect in mice,which is stronger than that of JQ1 and its synthesized derivatives.This study is expected to eventually lead to clinical trials.
文献关键词：
中图分类号：
作者姓名：
Sixian Wu;Xiaoliang Li;Lijun Shang;Lvying Wu;Tongtong Li;Peiyv Li;Zhiliang Ji;Jianwen Hou;Mingzhu Yin;Wenming Xu
作者机构：
Joint Laboratory of Reproductive Medicine,SCU-CUHK,Key Laboratory of Obstetric,Gynaecologic and Paediatric Diseases and Birth Defects of Ministry of Education,West China Second University Hospital,Sichuan University,Chengdu 610041,China;Reproductive Medical Centre,West China Second University Hospital,Sichuan University,Chengdu 610041,China;School of Human Sciences,London Metropolitan University,London N7 8BD,UK;State Key Laboratory of Cellular Stress Biology,School of Life Sciences,Xiamen University,Xiamen 361102,China;Department of Dermatology,Hunan Engineering Research Center of Skin Heath and Disease,Xiangya Hospital,Central South University,Changsha 410008,China
文献出处：
引用格式：
[1]Sixian Wu;Xiaoliang Li;Lijun Shang;Lvying Wu;Tongtong Li;Peiyv Li;Zhiliang Ji;Jianwen Hou;Mingzhu Yin;Wenming Xu-.The novel BRDT inhibitor NHWD870 shows potential as a male contraceptive in mice)[J].生物化学与生物物理学报（英文版）,2022(12):1789-1800
A类：
BRDT,NHWD870,extraterminal
B类：
novel,shows,potential,as,male,contraceptive,mice,Small,molecule,inhibitors,bromodomain,BET,family,proteins,have,emerged,promising,options,only,treatment,multiple,cancers,also,disturbing,process,maturation,use,viable,targets,In,this,study,find,that,well,vitro,through,bioinformatics,software,prediction,binding,hibition,experiments,produce,good,effect,animal,vivo,be,restored,normal,after,drug,withdrawal,Transcriptomics,proteomics,results,suggest,affects,pathways,related,spermatogenesis,further,contributing,infertility,phenotype,Our,induce,complete,reversible,which,stronger,than,JQ1,its,synthesized,derivatives,This,expected,eventually,lead,clinical,trials
AB值：
0.561774
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