申请人:The Salk Institute For Biological Studies
公开号:US05352796A1
公开(公告)日:1994-10-04
Unnatural amino acids are provided which can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; j=1,2 or 3, and preferably, Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl; or the formula (b): ##STR3## where R.sub.11 is H or acyl and W is as defined in (a), and preferably R.sub.11 is H and W is ##STR4## Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.
提供了可以并入肽中的非天然氨基酸,可以抑制或促进垂体腺分泌促性腺激素,并抑制生殖腺释放类固醇。这些非天然氨基酸在肽的合成中很有用,其化学式为(a):##STR1## 其中,W为(CH.sub.2).sub.n或##STR2## n为1到6的整数;j=1、2或3,最好Y为N-CN,X为NH,R.sub.2为烷基、改性烷基、烯基、炔基、芳基或甲基吡啶基;或者化学式(b):##STR3## 其中R.sub.11为H或酰基,W如(a)中所定义,最好R.sub.11为H,W为##STR4## 揭示了类似于十肽GnRH的肽,其中3、5、6和/或8位置至少有一个非天然氨基酸残基。