摘要
促黄体生成激素释放激素 (LHRH)激动剂药物已商品化 ,用于治疗性激素依赖的癌症 ,LHRH拮抗剂的研究还处于试验阶段 .近几年 ,在寻找高活性 ,低组胺释放 ,水溶性好 ,稳定性高的拮抗剂研究方面 ,已取得明显进展 .一些较小的环肽及肽模拟物也表现出较好的生物活性 .在十肽拮抗剂分子内 ,中间四肽的 βⅡ
Luteinizing hormone releasing hormone(LHRH) agonists as antitumor agents for hormone dependent tumor have been on the market for about ten years, while the LHRH antagonists that have been developed furthest are still in clinical trial. Significant progress has been made in searching for LHRH antagonists with high activity, low histamine releasing, good aqueous solubility. Smaller linear or cyclic peptides and peptidomimetics showed antagonistic activity both in vitro and in vivo . The βⅡ turn in the central tetrapeptide and the N terminal tripeptide segment of decapeptide LHRH antagonists play an important role in receptor binding.
出处
《生物化学与生物物理进展》
SCIE
CAS
CSCD
北大核心
2000年第5期500-504,共5页
Progress In Biochemistry and Biophysics
