具有非肼连接基的新型双氢吗啡酮类似物的合成与生物学评价
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.
作者信息
Mollica Adriano, Davis Peg, Ma Shou-Wu, Lai Josephine, Porreca Frank, Hruby Victor J
机构信息
Department of Chemistry, University of Arizona, Tucson, Arizona 85721, USA.
出版信息
Bioorg Med Chem Lett. 2005 May 16;15(10):2471-5. doi: 10.1016/j.bmcl.2005.03.067.
Biphalin is a potent opioid peptide agonist, with a palandromic structure, composed of two enkephalin-like active fragments connected tail to tail by a hydrazine linker (Tyr-D-Ala-Gly-Phe-NH-NH<-Phe<-Gly<-D-Ala<-Tyr). This study presents the synthesis and in vitro bioassays of six new biphalin analogues with three different non-hydrazine linkers, some of which have higher binding affinity and bioactivity than biphalin.
双啡肽是一种强效阿片肽激动剂，具有回文结构，由两个脑啡肽样活性片段通过肼连接子尾对尾相连组成（酪氨酰-D-丙氨酰-甘氨酰-苯丙氨酰-氨-氨-苯丙氨酰-甘氨酰-D-丙氨酰-酪氨酰）。本研究展示了六种带有三种不同非肼连接子的新型双啡肽类似物的合成及体外生物活性测定，其中一些类似物比双啡肽具有更高的结合亲和力和生物活性。
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