N-TERMINAL ANALOGS OF CECROPIN-A - SYNTHESIS, ANTIBACTERIAL ACTIVITY, AND CONFORMATIONAL PROPERTIES
N-TERMINAL ANALOGS OF CECROPIN-A - SYNTHESIS, ANTIBACTERIAL ACTIVITY, AND CONFORMATIONAL PROPERTIES
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DOI：
10.1021/bi00328a017
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发表时间：
1985-01-01
期刊：
影响因子：
2.9
通讯作者：
BOMAN, HG
中科院分区：
文献类型：
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作者：
ANDREU, D;MERRIFIELD, RB;BOMAN, HG
采用固相法合成了 37 个残基抗菌肽天蚕素 A 的 6 种类似物：天蚕素 A-(2-37)、[Glu2]天蚕素 A、[Pro4]天蚕素 A、[Glu6]天蚕素 A、[Leu6] 天蚕素 A 和 [Pro8]天蚕素 A。测定了它们对 4 种测试生物的抗菌活性，并与在 CD 光谱中观察到的构象变化相关，并基于先前提出的两亲性α-螺旋模型进行了讨论。 2 位芳香族残基对于对抗所有测试细菌的活性都很重要。天蚕素A的高度α-螺旋1-11区域似乎在其对抗大肠杆菌的活性中没有发挥显着作用，但显然参与其对抗铜绿假单胞菌、巨大芽孢杆菌和藤黄微球菌的相互作用。
Six analogs of the 37-residue antibacterial peptide cecropin A were synthesized by the solid-phase method: cecropin A-(2-37), [Glu2]cecropin A [Pro4]cecropin A, [Glu6]cecropin A [Leu6] cecropin A, and [Pro8]cecropin A. Their antibacterial activities against 4 test organisms were determined and related to conformational changes observed in their CD spectra, and were discussed on the basis of a previously proposed amphipathic .alpha.-helix model. An aromatic residue in position 2 was shown to be important for activity against all tested bacteria. The highly .alpha.-helical 1-11 region of cecropin A did not appear to play a significant role in its activity against Escherichia coli, but was clearly involved in its interaction against Pseudomonas aeruginosa, Bacillus megaterium, and Micrococcus luteus.