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脂肪族氨基二酸天冬氨酸在昆虫中对促肌收缩和食物摄入抑制活性方面可有效模拟速激肽中的酪氨酸(磺酸)。

Aliphatic amino diacid Asu functions as an effective mimic of Tyr(SO3H) in sulfakinins for myotropic and food intake-inhibition activity in insects.

作者信息

Nachman Ronald J, Vercammen Tom, Williams Howard, Kaczmarek Krzysztof, Zabrocki Janusz, Schoofs Liliane

机构信息

Areawide Pest Management Research, Southern Plains Agricultural Research Center, USDA, 2881 F/B Road, College Station, TX 77845, USA.

出版信息

Peptides. 2005 Jan;26(1):115-20. doi: 10.1016/j.peptides.2004.07.018.

Abstract

The aliphatic amino diacid alpha-aminosuberic acid can function as an effective, stable mimic of the hydrolysis-susceptible Tyr(SO3H) group in sulfakinin neuropeptide analogs for both hindgut contractile activity in cockroach and food intake-inhibition activity in the desert locust. In the analog, the acidic sulfate group is replaced with an acidic carboxyl group. The degree of activity of sulfakinin analogs is correlated with the carboxyl/alpha-carbon distance in the cockroach hindgut contractile assay. The results represent an important step in the design and synthesis of biostable, sulfakinin analogs that could potentially suppress the feeding behavior of destructive insect pests of agricultural importance.

摘要

脂肪族氨基二羧酸α-氨基辛二酸可作为一种有效、稳定的模拟物,用于模拟速激肽神经肽类似物中易水解的Tyr(SO3H)基团,对蟑螂后肠收缩活性和沙漠蝗的食物摄入抑制活性均有效。在该类似物中,酸性硫酸基团被酸性羧基取代。在蟑螂后肠收缩试验中,速激肽类似物的活性程度与羧基/α-碳距离相关。这些结果代表了设计和合成具有生物稳定性的速激肽类似物的重要一步,这类类似物可能潜在地抑制对农业具有重要意义的破坏性害虫的取食行为。

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