Slomczynska U, Leplawy T, Leplawy M T
Institute of Organic Chemistry, Technical University, Lodz, Poland.
Biomed Biochim Acta. 1991;50(10-11):S205-8.
Synthesis of LHRH N-terminal pentapeptide Glp1-His2-Trp3-Ser4-Tyr5-OMe (6) involving 3 + 2 enzymatic coupling has been developed. Synthetic strategy features the formation of one peptide bond (Glp-His) by chemical coupling and three peptide bonds by means of papain (Trp-Ser, Ser-Tyr) or alpha-chymotrypsin (His-Trp). High efficiency of this six-step synthesis is demonstrated by 44% overall yield. Its advantages are the use of inexpensive enzymes, simple isolation of intermediates and final pentapeptide, and easy recovery of substrates.
已开发出涉及3 + 2酶促偶联的促黄体生成素释放激素（LHRH）N端五肽Glp1-His2-Trp3-Ser4-Tyr5-OMe（6）的合成方法。合成策略的特点是通过化学偶联形成一个肽键（Glp-His），并借助木瓜蛋白酶（Trp-Ser、Ser-Tyr）或α-胰凝乳蛋白酶（His-Trp）形成三个肽键。该六步合成法的总产率为44%，证明了其高效性。其优点包括使用廉价的酶、中间体和最终五肽的分离简单以及底物易于回收。
