| 摘要 |
This invention relates to a method for producing an LH-RH derivative, characterized in that a peptide fragment shown by general formula (1): pGlu-His-Trp-OR1 (where R1 denotes a lower alkyl) and a peptide fragment shown by general formula (2): H-Ser-Tyr-X-Leu-Arg-Pro-Y (where X denotes an amino acid selected from the group consisting of D-amino acids such as D-Leu, D-Ser(But), D-Trp, and (2-napthyl)-D-Ala, and Gly, and Y denotes Gly-NH2, Azgly(Azaglycine)-NH2 or NHR2 (R2 is lower alkyl)) are allowed to react in the presence of chymotrypsin or a chymotrypsin-like enzymes, to produce the LH-RH derivative shown by general formula (3): pGlu-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-Y (where X and Y are as defined above). Since the method does not accompany a side reaction such as racemization, it enables simple separation and purification of LH-RH derivatives. Moreover the method enables to provide high yields, as well as recovery and recycling of unreacted peptide fragments, therefore it is valuable in industrial use.
|
