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1、药学学报ActaPharmaceuticaSinica2007,42(2):111-117·111··综述·Recentprogressintheimprovementofthecouplingefficiencyof“difficultsequences”inpeptidesynthesis3HANXiang,WANGDe2xin(InstituteofMateriaMedica,ChineseAcademyofMedicalSciencesandPekingUnionMedicalCollege,Beijing100050,China)Abstr
2、act:Eventhoughchemistryisnowinplacethatpotentiallyallowshighcouplingefficienciestobeattained,successfulcouplingisusuallyachallengewhenso2called“difficultsequences”isencounteredinpeptidesynthesis.Somefactorsthataffectthecouplingefficiencyhavebeendiscussedandrelatedmethodstooverc
3、omethoseobstacleshavebeenintroducedinpresentreview.Allsuggestionsproposedherearevaluableandalsofeasibletoimprovethecouplingcompletenessinbothliquid2phaseorsolid2phasepeptidesynthesis.Keywords:peptidesynthesis;couplingefficiency;difficultsequences;β2structureofpeptideCLCnumber:R
4、916Documentcode:AArticleID:0513-4870(2007)02-0111-07多肽合成中“困难序列”的缩合研究进展3韩香,王德心(中国医学科学院、中国协和医科大学药物研究所,北京100050)摘要:化学学科发展至今拥有极强的能力来获得高的合成效率,但是在多肽合成中“困难序列”的存在仍然成为成功缩合的巨大挑战。本文综述了影响多肽缩合效率的因素以及提高“困难序列”缩合效率的有效方法。所述方法均简便易行,适用于多肽的固相合成或液相合成。关键词:多肽合成;缩合效率;困难序列;β2构象Thephenomenonof“difficult
5、sequences”hasresiduesfromtheresinexistintraorinterchainlongfrustratedchemistsintheireffortstoassembleaggregationduetohydrogenbonds,producingdifficulty[4]peptidescontainingsuchsequencesbysolidorliquidtocouplingreaction.Althoughtheoccurrenceand[1,2]phasesynthesisprotocols.Theconv
6、entionalcouplingseverityof“difficultsequences”cannotbepredictedmethods,suchasactiveesterandacid2anhydridearewithconfidence,itisgenerallythoughtthatarisesfrom[3]sometimesfailedtoovercomethatobstacle.Theusetheintermolecularassociationofresin2boundpeptideofnewcouplingreagentisnota
7、lwaysfruitfulinpeptidechainsintoextendedβ2sheettypestructuresduring[5]synthesis,becausetroublesfromtheinsolubilityofsequentialassembly.SuchstructureledtheN2reactantsorthepoorswellingstateofpolymersupportterminalintoinaccessibletobeacylated.Therefore,inSPPS(solidphasepeptidesynt
8、hesis)gofarbeyondgettingaclearunderstandingofthefactor
