Hudson D, Kenner G W, Sharpe R, Szelke M
Int J Pept Protein Res. 1979;14(3):177-85. doi: 10.1111/j.1399-3011.1979.tb01923.x.
An efficient synthesis of methionine enkephalin using a phenolic resin support is described. Analogues modified at their C-termini, such as peptide acids, amides, methyl esters and compounds formed by their reduction, were prepared conveniently from common peptide phenyl ester resins. The resin was used in the synthesis of complex isosterically modified analogues designed to investigate the role of peptide backbone plays in receptor interaction. Free hexapeptide phenyl ester resins underwent intramolecular aminolysis liberating the corresponding cyclic peptides.
描述了一种使用酚醛树脂载体高效合成甲硫氨酸脑啡肽的方法。从常见的肽苯基酯树脂方便地制备了在其C末端修饰的类似物,如肽酸、酰胺、甲酯及其还原形成的化合物。该树脂用于合成复杂的等排修饰类似物,以研究肽主链在受体相互作用中的作用。游离的六肽苯基酯树脂进行分子内氨解,释放出相应的环肽。