皮啡肽类似物：额外的D-氨基酸取代并不总是能增强其对体外酶促降解的抗性。
Dermorphin analogs: resistance to in vitro enzymatic degradation is not always increased by additional D-amino acid substitutions.
作者信息
Darlak K, Benovitz D E, Spatola A F, Grzonka Z
机构信息
Institute of Chemistry, University of Gdansk, Poland.
出版信息
Biochem Biophys Res Commun. 1988 Oct 14;156(1):125-30. doi: 10.1016/s0006-291x(88)80813-1.
Dermorphin (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2) and seven analogs were examined for their biostability towards rat brain homogenate; half-lives for the parent were 127 min and 48 min, respectively, with Gly4-Tyr5 cleavage confirmed by collection and identification of the N-terminal fragment. Surprisingly, several analogs with additional D-amino acid substitutions were cleaved more rapidly than the parent, suggesting the importance of remote secondary structural features for differential enzyme susceptibility.
对脑啡肽（H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2）及其七种类似物进行了大鼠脑匀浆生物稳定性检测；母体的半衰期分别为127分钟和48分钟，通过对N端片段的收集和鉴定证实了Gly4-Tyr5的裂解。令人惊讶的是，几种具有额外D-氨基酸取代的类似物比母体裂解得更快，这表明远距离二级结构特征对不同酶敏感性的重要性。
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