The Hybrid Pyrroloisoindolone-Dehydropyrrolizine Alkaloid (-)-Chlorizidine A Targets Proteins within the Glycolytic Pathway.
The Hybrid Pyrroloisoindolone-Dehydropyrrolizine Alkaloid (-)-Chlorizidine A Targets Proteins within the Glycolytic Pathway.
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DOI：
10.1002/cbic.201500229
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发表时间：
2015-09-21
期刊：
影响因子：
--
通讯作者：
Fenical W
中科院分区：
文献类型：
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作者：
Álvarez-Micó X;Rocha DD;Guimarães LA;Ambrose A;Chapman E;Costa-Lotufo LV;La Clair JJ;Fenical W
(-)-氯西啶 A 是一种海洋生物碱，含有吡咯异吲哚酮和脱氢吡咯嗪的独特融合物，其细胞毒性活性通过细胞和分子方法的组合进行了探索。我们的研究首先应用从半合成生物活性评估中收集的初步 SAR 证据来制备主动免疫亲和荧光 (IAF) 探针。然后使用该探针来鉴定两种胞质蛋白 GAPDH 和 hENO1，作为 (-)-Chlorizidine A 的靶标。
The cytotoxic activity of (-)-chlorizidine A, a marine alkaloid containing a unique fusion between a pyrroloisoindolone and dehydropyrrolizine, was explored using a combination of cellular and molecular methods. Our studies began by applying preliminary SAR evidence gathered from semisynthetic bioactivity evaluations, to prepare an active immunoaffinity fluorescent (IAF) probe. This probe was then used to identify two cytosolic proteins, GAPDH and hENO1, as the targets of (-)-chlorizidine A.