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对一个具有很强的抑制豆蔻酰转移酶(NMT)活性的抑制肽噬菌体所展示的随机区15肽序列TW-PVVHGACRAHGHC进行关键氨基酸残基的单点、双点和缺失等一系列突变研究,以确定其功能区段。结果显示W2A、H6N和H6R突变使抑制活性明显下降,P3A、V4V5→A4A5双点突变对活性也有一定的影响,而V4V5→W4W5、H12N、H14N、C9S、C15S、ΔC15、ΔH14C15和ΔC9~C15等突变则基本上不影响抑制作用。表明W2、P3和H6在该抑制肽与NMT的作用中是重要的,而且P3与H6之间的氨基酸倾向于带较大侧链基团的残基。C9~C15间的序列在抑制作用中无明显贡献。提示该抑制肽功能区域位于N端的8个氨基酸残基中。
A series of mutation studies of single point, double point and deletion of the key amino acid residues in a randomized 15-terminal peptide sequence TW-PVVHGACRAHGHC displayed by an inhibitory peptide phage possessing strong inhibitory myristoyl transferase (NMT) activity were carried out with Determine its functional section. The results showed that the W2A, H6N and H6R mutations significantly decreased the inhibitory activity, while the P3A and V4V5 → A4A5 double-point mutations also had some effects on the activity. However, V4V5 → W4W5, H12N, H14N, C9S, C15S, ΔC15, ΔH14C15 and ΔC9-C15 Mutations do not substantially affect the inhibitory effect. Suggesting that W2, P3 and H6 are important in this inhibitory effect of peptides on NMT, and the amino acids between P3 and H6 tend to favor residues with larger side chain groups. The sequence between C9 and C15 showed no significant contribution to the inhibition. Suggesting that the inhibitory peptide functional region is located in the N terminal 8 amino acid residues.