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自从1954年第一次合成具有生物活性的多肽-催产素,至今将近20年中,随着医学事业及分子生物学研究的需要,多肽合成有了飞跃的发展。一系列的多肽及蛋白质,如促肾上腺皮质激素(39肽),胰岛素(两条肽链共51个氨基酸残基),增血糖素(29肽),调血钙激素(32肽)和它们的类似物以及一些蛋白质的较大片段,如核糖核酸酶 T_1的氨端47肽等均已合成。这些产物都是用发展较早的所谓经典法合成的,它的特点是反应物在有机溶剂中均相进行缩合。随着肽链的延长,反应物在有机溶剂中的溶解度将显著下降,它们的有效缩合和最终产物的分离提纯都发生很大困难。近年来虽然在保护基及缩合剂的选用和分离方法的革新等方面取得了很大的发展,但目前用经典法合成大肽仍停留在四、五十肽水平。Hirschmann 在1969年用均相法合成核糖核酸酶 S-蛋白(104肽)的报导中,虽利用尽量减少侧链保护基
For the first time in 1954, a bioactive polypeptide called oxytocin has been synthesized, and for nearly 20 years, with the needs of medical research and molecular biology research, peptide synthesis has made a leap forward. A series of polypeptides and proteins such as adrenocorticotropic hormone (39 peptide), insulin (51 amino acid residues in two peptide chains), glucagon (29 peptide), calmodulin (32 peptide) and their Analogues, as well as larger fragments of some proteins, such as the amino terminal 47 peptide of ribonuclease T_1, have been synthesized. These products are synthesized with the so-called classical method of the earlier development, which features the homogeneous condensation of reactants in organic solvents. With the extension of the peptide chain, the solubility of the reactants in the organic solvent will be significantly reduced, and both their effective condensation and the separation and purification of the final product will be very difficult. In recent years, although the protection of the base and condensing agent selection and separation methods and other aspects of the innovation has made great progress, but now using the classic method of synthesis of large peptides still remain in the four, fifty peptide levels. Hirschmann in the homogeneous phase synthesis of ribonuclease S-protein (104 peptides) in 1969 reported the use of minimized side chain protecting groups