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差向異構(gòu)化是指在化學(xué)反應(yīng)中，一個(gè)差向異構(gòu)體（epimer）轉(zhuǎn)化為另一個(gè)差向異構(gòu)體或其手性對(duì)映體的過(guò)程。在肽合成中，氨基酸的差向異構(gòu)化是一個(gè)常見(jiàn)的副反應(yīng)，可能導(dǎo)致肽的整體構(gòu)象改變，從而影響其生物活性。差向異構(gòu)化產(chǎn)物與目標(biāo)肽在物理特性上高度相似，增加了純化的難度。在多肽合成及多肽藥物...
INTRODUCTIONTheN-α-Fmoc-α-aminoisobutyricacidderivative（Aib）isadifficultderivativeforcouplinginSPPSduetoitssecondmethylgroupontheα-carbonthatinterfereswiththecouplingreaction（Figure1）.However,itcanbefoundinanumberofbiologicallyrelevantcompo...
查看詳情INTRODUCTIONTheAKR/Grossmurineleukemiaviruses（MuLV）areC-typeretrovirusesthatcausethedevelopmentofleukemiainAKR（H-2k）mice.1Type-specificantiretroviralcytotoxicT-lymphocyte（CTL）responseshavebeenreportedthatallowdifferentiationbetweeninfection...
查看詳情INTRODUCTIONInthedevelopmentofantibodiesdirectedagainstspecificpeptidesequences,T-helperepitopesareoftentaggedontothepeptidesequencetoaidinthestimulationoftheimmuneresponse.OnesuchsequenceistheuniversalPanHLADR-bindingepitope（PADRE）.Synthes...
查看詳情INTRODUCTIONOnechallengefacingpeptidesynthesisisthe-lactamformationofarginine（Figure1）.Theformationof-lactamoccurswhentheinternalnitrogenoftheguanidineattackstheactivatedester,irreversiblyformingthelactamring.Thisreactioniscompetitivewithpe...
查看詳情INTRODUCTIONOnepotentialissueinpeptidesynthesisisracemizationofcysteineａndhistidine.Thisisaconcernformicrowavepeptidesyntheisbecauseoftheelevatedtemperaturesduringdeprotectionａndcoupling.Studieshaveshownthatloweringthetemperatureto50°Cdurin...
查看詳情INTRODUCTIONVIP（vasoactiveintestinalpeptide）,apeptidehormone,hasbeenimplicatedinanumberofbiologicalprocessesincluding:increasingdigestivesystemmotility,stimulatingpepsinogensecretion,controllingthemammaliancircadiantimekeepingmachinery,regu...
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