Preparation of Luteinizing Hormone-Releasing Hormone Analogue
Taking Rink Amide resin as a solid support,and Fmoc-protected amino acids as raw materials,we prepared a D-cysteine6 substituted analogue([D-Cys6]-LHRH)of luteinizing hormone-releasing hormone(LHRH)by using solid-phase peptide synthesis method.The optimized cleaving reagent is trifluoroacetic acid-H2O-triisopropylsilane(95.0∶2.5∶2.5,volume ratio).The HPLC purity of pure[D-Cys6]-LHRH is 97.8%,and the total yield is 47.5%.This method has the advantages of easy operation,high efficiency,and high total yield,which provides a reference for the preparation of LHRH analogue,and lays a foundation for the construc-tion of LHRH receptor targeted peptide-drug conjugate.