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Conomarphins cause paralysis in mollusk: Critical and tunable structural elements for bioactivity.
Journal of Peptide Science ( IF 2.1 ) Pub Date : 2019-07-15 , DOI: 10.1002/psc.3179
Charmaine B Mendoza 1 , Dan Jethro M Masacupan 1 , Dessa Camille R Batoctoy 2 , Eizadora T Yu 2, 3 , Arturo O Lluisma 1, 3 , Lilibeth A Salvador-Reyes 1, 3
Affiliation  

Two conomarphins were purified as the major component of the venom of Conus eburneus. Conomarphins Eb1 and Eb2 showed biological activity in the mollusk Pomacea padulosa, causing sluggishness and retraction of siphon, foot, and cephalic tentacles. To further probe the effects of conserved amino acids and posttranslational modifications in conomarphins, we prepared four synthetic analogues: conomarphin Eb1 Hyp10Pro, Hyp10Ala, d‐Phe13Ala, and l‐Phe13 variants. Structure‐activity relationship analysis indicated that d‐Phe13 is critical to the biological activity of conomarphins. In contrast, amino acid changes at position 10 and removal of posttranslational modification in Hyp10Pro can be tolerated. The high expression level and observed mollusk activity of conomarphins may suggest their potential role as defensive arsenal of Conoidean snails against other predatory gastropods.

中文翻译:

香豆素引起软体动物瘫痪:生物活性的关键和可调结构元素。

二conomarphins作为毒液的主要成分纯化黑星芋螺。香豆素Eb1和Eb2在软体动物Pomacea padulosa中显示出生物活性,导致虹吸管,足管和头触手的呆滞和缩回。为了进一步探究保守氨基酸和conomarphins中翻译后修饰的作用,我们准备了四种合成类似物:conomarphin Eb1 Hyp10Pro,Hyp10Ala,d- Phe13Ala和l- Phe13变体。构效关系分析表明,d‐Phe13对香豆素的生物活性至关重要。相反,Hyp10Pro的10位氨基酸变化和翻译后修饰的去除是可以容忍的。香豆素的高表达水平和观察到的软体动物活性可能表明它们具有潜在的作用,可以作为Conoidean蜗牛的防御性武器库对付其他掠食性腹足类动物。
更新日期:2019-07-15
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