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内皮素是重要的缩血管因子。内皮素和内皮素受体具有很强的广泛的生物学效应 ,但它们之间三维结合机制并不十分清楚。截取内皮素肽链的有效片段 ,或根据天然肽类提取物 ,利用 D-型天然或特殊氨基酸 ,进行结构改造 ,获得重要的内皮素受体拮抗剂线性六肽、线性三肽和环三肽等。特殊氨基酸的空间限制性构象、芳环的脂溶性等 ,在肽类拮抗剂与内皮素受体结合时有重要作用。另外 ,末端的羧基、可形成氢键的官能团或原子 ,是构效关系研究中的重要因素。
Endothelin is an important vasoconstrictor factor. Endothelin and endothelin receptors have a very wide range of biological effects, but the three-dimensional binding mechanism between them is not very clear. Effective fragments of the endothelin chain are intercepted, or structurally engineered from native peptide extracts using D-type native or specific amino acids to obtain important endothelin receptor antagonist linear hexapeptides, linear tripeptides, and cyclic tripeptides Wait. The space-restricted conformation of special amino acids, the lipophilicity of aromatic rings and the like play an important role in the binding of peptide antagonists to endothelin receptors. In addition, the terminal carboxyl groups, hydrogen bondable functional groups or atoms, is an important factor in the study of the structure-activity relationship.