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文献和实验为缩合剂,保持pH 8.5~9,反应4天,得到相应的环六肽和环五肽,收率在15%~50%之间。生物活性实验表明所有的环六肽对细胞粘附的抑制作用均明显低于线性肽GRGDS。环五肽中也只有Cyclo(RGDdFV)和Cyclo(RGDFd-V)对Laminin P1的细胞粘附具有明显的抑制作用。 对于某些在碱性条件下易分解的目的物,反应过程当中应用惰性气体进行保护,例如,线性多肽H-Asp(Fmoc)- d-Ser-Phe- D-Phe- Arg- Gly - OH在无水DMF中,加入5倍量NaHCO
Synthesis of Cyclopropane-Containing Leu-Enkephalin Analogs
of this chapter is to describe the preparation of a novel cyclopropane-containing cis -substituted (-Glyψ[CHOH-cp-CONH]-) subunit, which replaces Gly 2 -Gly 3 subunit of the Leu-enkephalin (Tyr-Gly-Gly-Phe-Leu) framework shown in Fig. 1 . Fig
, RocheBenzamidine-AgaroseEnterokinase Asp-Asp-Asp-Asp-Lys�New England Biolabs, Novagen, RocheTrypsin Inhibitor-AgaroseTEV protease Glu-Asn-Leu-Tyr-Phe-Gln�GlyInvitrogen – Life Technologies Ni-NTA (6His recomb. TEV)PreScission Leu-Glu-Val-Leu-Phe-Gln�Gly-ProAmersham
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