肽合成_多肽_固相肽合成-默克生命科学

肽由两个或多个通过酰胺键连接的氨基酸组成,形成一条通常由2至70个氨基酸组成的氨基酸链。肽与蛋白质的区别在于,其无需折叠即可发挥生物活性。 肽在体内以肽类激素的形式存在,例如血管紧张素、LHRH、脑啡肽等,同时也作为动植物中的毒素存在。肽作为药物研发的先导化合物以及独立的药物本身,备受关注。它们还应用于疫苗、生物材料、组织学探针中,并被大量用作抗原以产生抗体。
肽可通过溶液法或固相法进行化学合成。该过程涉及在N-保护的氨基酸与具有游离氨基及受保护羧基的氨基酸之间,定向且选择性地形成酰胺键。在固相合成中,羧基保护基被连接到聚合物载体上。 键形成后,二肽的氨基保护基被去除,随后与下一个N-保护的氨基酸进行偶联。
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图2用于Boc固相肽合成(SPPS)的侧链保护基

图3。Fmoc固相肽合成(SPPS)中的侧链保护基
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