申请人:MERRELL DOW PHARMACEUTICALS INC.
公开号:EP0297456A2
公开(公告)日:1989-01-04
Novel peptides having a fragment containing 2 or 3 Arg or Lys residues and having a fragment containing 2 or 3 Gly, Leu, Ile, or Thr residues adjacent to the carboxy end of the first fragment and having amino and carboxy tails consisting of chains made up of any amino acids are immunosuppressant agents and can suppress the lymphocyte system by suppressing lymphocyte proliferation.
The formula is as follows:
Tn-A-B-C-D-Tc
wherein
Tn is an amino terminal residue selected from hydrogen, one or two alkyl groups of from 1 to 6 carbon atoms, one or two acyl groups of from 2 to 10 carbon atoms, carbobenzyloxy, and t-butyloxycarbonyl;
A is a peptide fragment containing from 3 to 12 residues of any amino acid;
B is a peptide fragment containing 2 or 3 amino acid residues selected from Arg and Lys;
C is a peptide fragment containing 2 or 3 amino acid residues selected from Gly, Leu, Ile, and Thr;
D is a peptide fragment containing from 1 to 12 residues of any amino acid; and
Tc is a carboxy terminal residue selected from OH, (C₁-C₆)alkoxy, amino, mono- or di-(C₁-C₄)alkyl substituted amino, and benzylamino.
新型多肽具有含有 2 或 3 个 Arg 或 Lys 残基的片段,以及与第一个片段的羧基端相邻的含有 2 或 3 个 Gly、Leu、Ile 或 Thr 残基的片段,并具有由任意氨基酸组成的链的氨基和羧基尾部,是一种免疫抑制剂,可通过抑制淋巴细胞增殖来抑制淋巴细胞系统。
其计算公式如下
Tn-A-B-C-D-Tc
其中
Tn 是氨基末端残基,选自氢、一个或两个 1 至 6 个碳原子的烷基、一个或两个 2 至 10 个碳原子的酰基、苄氧羰基和 t-丁氧羰基;
A 是含有 3 至 12 个氨基酸残基的肽片段;
B 是含有 2 或 3 个选自 Arg 和 Lys 的氨基酸残基的肽片段;
C 是含有 2 或 3 个选自 Gly、Leu、Ile 和 Thr 的氨基酸残基的肽片段;
D 是含有 1 至 12 个任意氨基酸残基的肽片段;以及
Tc 是羧基末端残基,选自 OH、(C₁-C₆)烷氧基、氨基、单-或二-(C₁-C₄)烷基取代的氨基和苄基氨基。