吉林大学学报（理学版）2019，Vol.57Issue(3)：696-700,5.DOI:10.13413／j.cnki.jdxblxb.2018207
Exendin-4高活性短肽模拟物的筛选及生物活性
ScreeningandBioactivityofHigh-Activity Short-PeptideMimicsofExendin-4
摘要
Abstract
Usingthetechniqueofphagescreening,weutilizedtheglucagon-likepeptide1receptor (GLP-1R)of RINm-5F cellasthetargettoscreen GLP-1receptoragoniststhroughcompetitive elutionbyExendin-4andobtained12-merpeptidemimicsEPA.Theexperimentalresultsshowthat EPAandExendin-4canpromotetheproliferativeactivityofisletβcells,andtheactivityofEPAis 5%—25% higherthanthatofExendin-4intherangeof40—200μmol／L.EPAinhibitstheapoptosis ofisletβcellsbyinhibitingbaxgeneandup-regulatingbcl-2geneexpression,andinhibitingCaspase-3activityat100 mmol／Lhighconcentrationofglucosetoxicity,EPAisahigh-activityshort-peptide mimicsofExendin-4,whichcaninhibitthe mitochondrialapoptosisthroughbcl-2／bax…Casepase-3 signalingpathway.关键词
肽库筛选/Exendin-4模拟物/生物活性/葡萄糖毒性Key words
peptidelibraryscreening/mimicofExendin-4/bioactivity/glucosetoxicity分类
生物科学引用本文复制引用
宋相伟,王雪丽,王璐璐,楼婉琳,王丽萍,熊新辉,牛建丽,李惟..Exendin-4高活性短肽模拟物的筛选及生物活性[J].吉林大学学报（理学版）,2019,57(3):696-700,5.基金项目
吉林省科技发展计划项目(批准号:20190304051YY)、长春师范大学自然科学基金(批准号:长师大自然合字[2018]第012号)、吉林工商学院科研项目(批准号:院理科合字LB2016004)和吉林省大学生创新创业训练计划项目(批准号:2018100). （批准号:20190304051YY）
